In humans, 61 bromodomains, each composed of ∼110 amino acids forming four antiparallel α helices (αZ, αA, αB, and αC) and two hydrophobic (ZA and BC) loops, in 46 different proteins have been described. Indeed, in the last 30 years a limited progress has been made in GBM treatment with current first-line standards-of-care. VU0469650 hydrochloride. GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. 5 gsk778 (pan-bd2) ↓mcp-1 in lps-stimulated pbmcs: 1000 <10 gsk791 32193360 6 brd: baz2a/2b baz2-icr frap, baz2a: 1000 1 - 25719566 7 gsk2801 frap, baz2b: 1000 3 gsk8573 25799074 8 brd: brd9/7 bi-9564 frap, brd9/7: 100/1000 1 - 26914985 9 tp-472 nanobret, brd9: 323 (ec 50) 1 tp-472n 10 brd: brd9 i-brd9 nanobret, brd9: 159 1 - 25856009 11 brd. GSK778 phenotyping the role of pan-BET inhibitors in cancer models. Open in a. BA EN. 1. WGK. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. At. Miransertib is an Orally Active Akt Inhibitor for Cancer and Infection Research. Storage Class Code. orgGSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. S9684: GSK046Visit ChemicalBook To find more GSK778(2451862-42-1) information like chemical properties,Structure,melting point,boiling point,density,molecular formula,molecular weight, physical properties,toxicity information,customs codes. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Saturday. Its mechanism of action is not fully understood. 999. Find (s)-1-phenylethyl (r)-acetoxyphenylacetate and related products for scientific research at MilliporeSigma GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Structural Genomics Consortium MaRS Centre, South Tower 101 College St. Preis und Verfügbarkeit anzeigen. Applications Products Services Documents Support. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 Hydrochloride. WGK. 125 nM (MV-4−11 cells) ≤. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. COO/ COA. 0; BRD4 (BD2) pKd = 5. 5. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. GlaxoSmithKline; BRD2, BRD3, BRD4, BRDT (BD2) GSK046; pIC50 = 7. Available to order from Sigma-Aldrich. Instruction. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. 1% Tween-20 and incubated with. g ABBV-744, Fig. Dagrocorat. rednibar) and I. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Email. CAS No. No; GlaxoSmithKline The mammalian bromodomain and extra-terminal domain (BET) family of proteins consists of four conserved members (Brd2, Brd3, Brd4, and Brdt) that regulate numerous cancer-related and immunity-associated genes. BROMODOMAIN AND EXTRA‐TERMINAL (BET) PROTEINS. 2451862-42-1 GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). Request PDF | A Simple Electrostatic Model for the Hard-Sphere Solute Component of Nonpolar Solvation | We propose a new model for estimating the free energy of forming a molecular cavity in a. GSK778 Hydrochloride. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models [1]. GSK778 (iBET-BD1) is a potent and selective inhibitor of the BD1 bromine domain of the BET protein,IC50 The values are 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1). Safety Information. All Photos (1) SML3234. Here, two unexpected findings are reported: (1) SynGRs bearing pan-BET or BD2-selective ligands license transcription at the FXN locus, whereas those bearing BD1-selective ligands do not, and (2) rather than being neutral or inhibitory, an untethered BD1-selective ligand (GSK778) substantively enhances the activity of all active SynGRs. P (moc. All Photos (1) Documents. Pharmacological inhibition of BET BDs using the chemical probes JQ1 (Filippakopoulos et al. GSK778 : Catalog Number: M10828: CAS Number: 2451862-42-1: 1. The two tandem bromodomains of the BET proteins enable chromatin binding to facilitate transcription. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. GSK778 Hydrochloride. Figure 4. Phylogenetic tree of the human bromodomain-containing protein subgroups. Recent clinical studies have shown that BRD4 expression in glioma is significantly higher than in the adjacent normal brain tissue. Applications Products Services Documents Support. Copy Link. To explore the individual functional. Storage Class Code. 00. ID EN. WGK. While GSK789 was less selective (TAF1-BD2 K d = 50 nM and TAF1L-BD2 K d = 398 nM), it. All Photos (1) Documents. The two tandem. 4 D and E) shows that our BD1-selective and BD2-selective DECL-derived inhibitors each occupy the same KAc pocket as GSK778 but also access adjacent grooves that differ between the two domain types. All Photos (1) Documents. ([email protected]) and I. Copy Link. But, how does GSK778 work on the target? Let’s discuss it in detail. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Código de clase de almacenamiento. 1. BET proteins are linked to cancer progression. Copy Link. 14 GSK778, another pan-D1-selective inhibitor (Figure 1A), was recently reported. rednibar) and I. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Not for human use. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. The calculations of the energy contributions of individual residues demonstrate that residues corresponding to (BD1, BD2) generate significant energy difference in binding of SG3-179, GSK778, and. Of these, only ABBV-744 and two molecules described within the article, GSK778 (iBET-BD1) and GSK046 (iBET-BD2) showed appreciable selectivity. 3; Cell proliferation assay with the AML cell line MV-4−11 that has a MLL-AF4 rearrangement (3 days): growth inhibition with pIC50 = 7. Available to order from Sigma-Aldrich. ≥98% (HPLC)Shop Medchemexpress LLC HY-136570 5mg , GSK778 CAS:2451862-42-1 Purity:>98% at Fishersci. 12:01PM IST Vir Savarkar (Port Blair) - IXZ. Chemical probes are cell-active, selective, highly validated research tools that can be used to decipher the biology of their target. Available to order from Sigma-Aldrich. BRD3 (BD1) pIC. Chemical structures of the BD1/BD2-selective BET inhibitors discussed: (A) GSK778, (B) GSK046, (C) ABBV-744, and (D) SJ432. 3 Details of the supplier of the safety data sheet; Company: Abmole Bioscience Inc. GSK778 Hydrochloride. Copy Link. Not for human use. The . WGK. ([email protected]) under a material transfer agreement with GSK. 9 BRD: BAZ2A/2B: BAZ2-ICR. 65 ABBV-744 shows potent anti-proliferative effects against. ≥98% (HPLC)We would like to show you a description here but the site won’t allow us. PubMed Abstract: The two tandem bromodomains of the BET (bromodomain and extraterminal domain) proteins enable chromatin binding to facilitate transcription. Preis und Verfügbarkeit anzeigen. Louis Gilman November 13, 2023. 00. Applications Products Services Documents Support. GSK778 reduces the production of anti-keyhole limpet. Forodesine hydrochloride ≥98% (HPLC); Synonyms: 7-[(2S,3S,4R,5R)-3,4-Dihydroxy-5-(hydroxymethyl)-2-pyrrolidinyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one, hydrochloride salt,BCX-1777 HCl,ImmH HCl,Immucillin-H HCl; find Sigma-Aldrich-SML3378 MSDS, related peer-reviewed papers, technical documents, similar products & more at Sigma-Aldrich We would like to show you a description here but the site won’t allow us. Many reports have shown that pan BETis, such as JQ1 and iBET762, exhibited no selectivity between BD1 and BD2, but BD1-selective (GSK778) or BD2-selective (GSK046 and ABBV-744) BETis showed. However, many compounds reported in the literature and routinely. GSK778 Hydrochloride. This approachGSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. M28749 CAS No. CA EN. Related Post. All Photos (1) Documents. GSK778 (iBET-BD1) is an analogue of I-BET151 with good potency against BET BD1 (IC 50 = 40 nM) and similar selectivity to LT052 (150-fold) over BD2 [48]. MM EN. SML3234. 4 D and E) shows that our BD1-selective and BD2-selective DECL-derived inhibitors each occupy the same KAc pocket as GSK778 but also access adjacent grooves that differ between the two domain types. 5 upper limit of normal (ULN) Total bilirubin < 1. AR EN. In contrast to other reported domain-selective molecules, these compounds showed little binding to bromodomains. Synonym(s): 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5-dimethylisoxazole Hydrochloride, iBET-BD1. Available to order from Sigma-Aldrich. S1F. A320. Introduction. Applications Products Services Documents Support. 1B, fig. MX EN. Meanwhile, GSK778 has IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. COO/ COA. Catalog No. Instead, a unique effect of BD2-selective antagonism was revealed with GSK046, affecting the induction of gene expression more so than the expression of steady-state genes, in contrast to GSK778 [28]. All Photos (1) Documents. Buy Epigenetic Reader Domain inhibitor GSK778 (iBET-BD1) from. Applications Products Services Documents Support. Developing BDII selective compounds was far more challenging, and only a handful of BDII selective inhibitors have been developed to date (Figure 1). ≥98% (HPLC)We used the BD1-selective small molecule inhibitor GSK778, which largely phenocopies pan-BET inhibitors, as well as the BD2-selective inhibitor GSK046, which has more limited effects on steady. For research use only. 999. Find (s)-1-phenylethyl (r)-acetoxyphenylacetate and related products for scientific research at MilliporeSigmaI-BET151 (GSK1210151A), iBET-BD1 (GSK778) and iBET-BD2 (GSK046) were provided by GlaxoSmithKline plc (GSK, London, UK). TC EN. MR EN. HY-136570 25mg GSK778 CAS: 2451862-42-1 GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Thus, BRD4 is a target for the treatment of glioma. GSK778. The second-generation BRD4 inhibitors are mainly synthesized by proteolysis targeting chimera (PROTAC) technology. CAS#: 2451862-42-1. Copy Link. Modukuri a,1, Zhifeng Yu , Zhi Tan , Hai Minh Tab,1, Melek Nihan Ucisik a. All Photos (1) SML3234. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Selectivity profile of I-BET151, iBET-BD1 (GSK778), and iBET-BD2 (GSK046). 1A). Available to order from Sigma-Aldrich. Pan-BD1 inhibitors (which have higher inhibitory activity for BD1 than BD2 of BET proteins) are comparable to pan-BD inhibitors, such as MS436, 59 Olinone, 60 MS402, 61 3U, 62 GSK778, 19 ZL0516. Additionally, while GSK778 phenocopied I-BET151 in terms of anti-proliferative effects on a range of human cancer cells, GSK046 was less effective. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. ≥98% (HPLC) All Photos (1)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Email. Available to order from Sigma-Aldrich. Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months). 10 µM; GSK791. Solubility: Soluble in DMSO. GSK778 Hydrochloride. ChemicalBook 致力于为化学行业用户提供FREEBASE的性质、化学式、分子式、比重、密度,同时也包括FREEBASE的沸点、熔点、MSDS、用途、作用、毒性、价格、生产厂家、用途、上游原料、下游产品等信息。 Recently, Gilan et al. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. A concentration of 1-2 µM of I-BET151, GSK778, GSK789, or GSK046 was used for cell culture treatments as recommended by our collaborators at GlaxoSmithKline (54–56). Email. 포함:구조식 이미지,카스 번호(CAS),분자식,녹는점,끓는 점,밀도. Email. The authors report the development of GSK046 (iBET-BD2), a potent BD2-selective inhibitor with >1000-fold selectivity over BD1. WGK. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and. ≥98% (HPLC) All Photos (1)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 2 (LPS-PBMC assay) <10. 4. Applications Products Services Documents Support. GSK778 (iBET-BD1) is a potent and selective inhibitor of bromodomain (BRD) BD1. Applications Products Services Documents Support. Molecular Formula: C30H33N5O3. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Email. We do not sell to patients. Applications Products Services Documents Support. GSK778 has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells, GSK778 reduces the clonogenic capacity of primary human AML cells. BET BD1 related products. • (+)-JQ1 has 45–50 times more binding capabilities to BD1 compared with BD2 (Chen et al. But, how does GSK778 work on the target? Let’s discuss it in detail. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Hazard identification. Safety Information. Description: GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). WGK 3. If not otherwise indicated, cells were pretreated with I-BET151, iBET-BD1, iBET-BD2 or vehicle (DMSO) for 48 hours, irradiated with 0 or 6 Gy, and incubated for additional time intervals with concurrent drug. , 2010), BD1-specific GSK778 and BD2-specific ABBV-774 and GSK046 (Faivre et al. Miransertib target all three Akt isoforms by blocking…. Preis und Verfügbarkeit anzeigen. 6SWO: C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH iBET-BD1 (GSK778) PDB ID: 6SWO Download: MMDB ID: 192698: PDB Deposition Date: 2019/9/22: Updated in MMDB: 2021/02: Experimental Method: x-ray diffraction. BD1-selective tool (GSK778) BD2-selective tool (GSK046) BRD4 BD1 IC 50: >50000 nM BRD4 BD2 IC 50: 50 nM BRD4 BD1 IC50: 40 nM BRD4 BD2 IC50: 6300 nM Reduced off-target binding Ph. Catalog Number: AA01KEG7. Particularly, GSK778 has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells. Applications Products Services Documents Support. The subsequent development and application of GSK778 (BD1 selective) and GSK046 (BD2 selective) revealed that inhibition of BD2 was ineffective in displacing BET proteins from chromatin. No; GlaxoSmithKlineBy surface plasmon resonance binding assay, GSK778 is > 130-fold selective for BD1, whereas GSK046 is > 300-fold selective for BD2 . Selectivity profile of I-BET151, iBET-BD1 (GSK778) and iBET-BD2 (GSK046). K. Safety Information. GSK778 phenocopies the. Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification code 6SWN, 6SWO, 6SWP and 6SWQ. Drugs that inhibit both bromodomains equally have shown efficacy in certain malignant and inflammatory conditions. (C) X-ray crystal structure of I-BET151 in. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. They are useful assets for example, in phenotypic assays, or as a starting point for medicinal chemistry campaigns. A concentration of 1-2 µM of I-BET151, GSK778, GSK789, or GSK046 was used for cell culture treatments as recommended by our collaborators at GlaxoSmithKline (54–56). T9703 CAS 2451862-42-1. All Photos (1) SML3234. Address: 1633 Old Bayshore Highway Suite 280 Burlingame, CA 94010. 06 (n = 8); (BD2) 5. 11 - Combustible Solids. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. All Photos (1) SML3234. Glioblastoma multiforme (GBM) is the most common and aggressive malignant primary brain tumor in adult humans, characterized by a poor prognosis despite the existence of multimodal therapy []. It reduces relapse rate and disease progression in Multiple Sclerosis. GSK778 and GSK046 are termed iBET-BD1 and iBET-BD2 respectively. Among this class, RVX-208 mainly blocks BD2 function [99], whereas GSK778 is a BD1 selective inhibitor [99]. 53 reported the development route of iBET-BD1 from a pan-BET imidazoquinolinone-based inhibitor with a slight BD1-bias, iBET151. SML3234. Available to order from Sigma-Aldrich. GSK778 Hydrochloride. Primary Citation of Related Structures: 6SWN, 6SWO, 6SWP, 6SWQ. The two. The two tandem bromodomains of the BET. Available to order from Sigma-Aldrich. Applications Products Services Documents Support. In recent years, members of the bromodomain and. Available to order from Sigma-Aldrich. Figure 5. Copy Link. Not for human use. Applications Products Services Documents Support. Storage Class Code. Available to order from Sigma-Aldrich. However, recent reports of potent and selective pan-BET BD1 and pan-BET BD2 inhibitors have been reported including ABBV-744, 21 GSK778, and GSK046. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. 27,42 The second-generation BRD4 inhibitors are mainly synthesized by proteolysis targeting chimera (PROTAC) technology. GSK778 (iBET-BD1) is a potent and selective inhibitor of the BD1 bromine domain of the BET protein,IC50 The values are 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4. their selectivity. GSK778 has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells, GSK778 reduces the clonogenic capacity of primary human AML cells. Drug Formulation: This drug may be formulated in DMSO. Find (s)-1-phenylethyl (r)-acetoxyphenylacetate and related products for scientific research at MilliporeSigmaGSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Drug Formulation: This drug may be formulated in DMSO. SML3234. We do not sell to patients. Available to order from Sigma-Aldrich. PK EN. COO/ COA. Available to order from Sigma-Aldrich. They are epigenetic readers of histone acetylation with broad specificity. Recombinant IL-1β (Peprotech, Cranbury, NJ) was reconstituted RPMI at 0. Phylogenetic tree of the human bromodomain-containing protein subgroups. nM, SPR BRD4 (BD1): pKd= 8. All Photos (1) Documents. Guanidine hydrochloride; Useful for denaturing proteins and solubilization of inclusion bodies. However, distinct from BD1-selective and pan-BET inhibitors, the BD2. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 8905. All Photos (1) SML3234. In addition, recent studies have shown that selective. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. 5 (LPS-PBMC assay) ≤ 10 µM. FRAP, BAZ2B: 1000 3:. Of these, only ABBV-744 and two molecules described within the article, GSK778 (iBET-BD1) and GSK046 (iBET-BD2) showed appreciable selectivity. Available to order from Sigma-Aldrich. Comparison of the binding modes of CDD-956 with BD1, CDD-1302 with BRDT-BD2 , and iBET-BD1 (GSK778) with BRD4-BD1 (Fig. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. MedKoo CAT#: 408120. All Photos (1) Documents. GSK778. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Available to order from Sigma-Aldrich. 5 upper limit of normal (ULN) Total bilirubin < 1. The authors found that in mouse models of various cancers, BD1 inhibition is. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. GSK778 (iBET-BD1) ist ein potenter und selektiver BD1-BromodomÄnen-Inhibitor der BET-Proteine mit IC50-Werten von 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1) und 143 nM (BRDT BD1) , beziehungsweise. To date, 61 bromodomains have been identified in 46 diverse proteins in human cells (Filippakopoulos et al. Available to order from Sigma-Aldrich. 2. Available to order from Sigma-Aldrich. Applications Products Services Documents Support. Miransertib is a highly selective, orally active, pan-Akt inhibitor. All products from TargetMol are for Research Use. Recently, inhibitors were developed that selectively target the first (BD1) and second (BD2) bromodomain of the BET proteins (iBET-BD1 [GSK778] and iBET-BD2 [GSK046]). Endoplasmic Reticulum Stress Modulator (ERSM) Epigenetics Resch Products. Copy Link. GSK778 Hydrochloride. 11 - Combustible Solids. Hazard Description: Toxic. GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. The bromodomain (BD) is a ~110 amino acid motif that binds to acetyl-lysine modifications on histone and non-histone proteins (Dhalluin et al. All Photos (1) SML3234. Email. 2451862-42-1 related products. , 2021). Available to order from Sigma-Aldrich. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. In almost half of hepatocellular carcinoma (HCC) cases, the Akt pathway is activated. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Pan-BD1 inhibitors (which have higher inhibitory activity for BD1 than BD2 of BET proteins) are comparable to pan-BD inhibitors, such as MS436, 59 Olinone, 60 MS402, 61 3U, 62 GSK778, 19 ZL0516. GSK778: CAS Registry Number: 2451862-42-1: Molecular Weight: 511. GSK778 Hydrochloride. K. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Buy Epigenetic Reader Domain inhibitor GSK778 (iBET-BD1) from AbMole BioScience. GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75. Copy Link. Biological Activity：GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. Copy Link. 125 nM (MV-4−11 cells) ≤. GSK778 (iBET-BD1) potently inhibits numerous cancer cells. toronto@thesgc. LY EN. SML3234. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. Email. View and buy high purity iBET-BD1 | GSK778 from AOBIOUS, the leading supplier of life science reagents. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. SML3234. Copy Link. (A) Schematic of the BET Bromodomain proteins and chemical structures. 5. All Photos (1) Documents. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. COO/ COA. ksg@ahjnirp. All. CAS Number: 2451862-42-1. 00. CAS: 2451862-42-1 (free base) Chemical Name: GSK778 2HCl; 4-(2-(Methoxymethyl)-1-((R)-1-phenylethyl)-8-(((S)-pyrrolidin-3-yl)methoxy)-1H. 6SWN: N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH iBET-BD1 (GSK778) PDB ID: 6SWN Download: MMDB ID: 192697: PDB Deposition Date: 2019/9/22: Updated in MMDB: 2021/02: Experimental Method: x-ray diffraction. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification code 6SWN, 6SWO, 6SWP and 6SWQ. GSK778 Hydrochloride. WGK. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. $79. 511. Applications Products Services Documents Support. 1B, fig. SML3234. The two novel ‘iBET’ molecules display the. Adequate renal, hepatic, pulmonary and cardiac function defined as: Creatinine clearance (as estimated by Cockcroft Gault) > 60 mL/min. 2′,3′-Didesoxycytidin. S9683 Synonyms: iBET-BD1. WGK 3. 00. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Copy Link. 1 in RR-multiple myeloma CC-94280 HIGHLIGHTS FROM DRUG DISCOVERY ARTICLES PUBLISHED ONLINE | MAR. GSK778 inhibits proliferation, induces a cell cycle arrest and Apoptosis . Applications Products Services Documents Support. ChemScene Provide GSK778(CAS 2451862-42-1)In-stock or Backordered impurities,Bulk custom synthesis,Formular C30H33N5O3,MW 511. 11 - Combustible Solids. Recently, inhibitors were developed that selectively target the first (BD1) and second (BD2) bromodomain of the BET proteins (iBET‐BD1 (GSK778) and iBET‐BD2 (GSK046)). R3653. COO/ COA. Email. E-newsletter Get updates ,discounts and special offers. COO/ COA. (B) Compound binding to the individual bromodomains of BD1 (orange) and BD2 (cyan) of BET tandem bromodomains in TR-FRET assays. The addition of olinone to oligodendrocyte progenitor cells demonstrated biological effects divergent from pan-BET inhibition. Available to order from Sigma-Aldrich. org); (b) BET BD1-selective GSK778 bound to BRD4-BD1 (in cyan,. GSK778 Hydrochloride ≥98% (HPLC); Synonyms: 4-{2-(Methoxymethyl)-1-[(R)-1-phenylethyl]-8-[(S)-pyrrolidin-3-ylmethoxy]-1H-imidazo[4,5-c]quinolin-7-yl}-3,5. The imidazoquinolinone 8-position of iBET151 was identified as orienting towards the. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. COO/ COA. 6SWN, 6SWO, 6SWP, 6SWQ.