9 BRD: BAZ2A/2B: BAZ2-ICR. Where indicated, 1 μm GSK778 or GSK046 or carrier (DMSO) were added at the same time as LPS. Copy Link. Copy Link. ≥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. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Their affinities for the individual bromodomains of the BET family were initially determined by TR-FRET (Fig. Iniciar Sessão; Criar uma conta ()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. GSK778 phenocopied the effects of pan-BET inhibitors in cancer models. 3 Details of the supplier of the safety data sheet; Company: Abmole Bioscience Inc. First of all, GSK778 (iBET-BD1) is a potent and selective inhibitor of bromodomain (BRD) BD1. Copy Link. GSK778 Hydrochloride. Compounds GSK778 (5) and GSK046 (6) are recently reported BET BD1-selective and BET BD2-selective small molecule inhibitors with >130-fold and >300-fold selectivity over the other corresponding bromodomains, respectively, as determined by surface plasmon resonance (SPR) assays. GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). The addition of olinone to oligodendrocyte progenitor cells demonstrated biological effects divergent from pan-BET inhibition. . GSK778 hydrochloride | C30H34ClN5O3 | CID 168013350 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological. 11 - Combustible Solids. ≥98% (HPLC)MOscan analysis of GSK778 indicated the binding of this compound only to BET bromodomains with strong binding to BET BD1 domains while weakly binding to BET BD2 domains. 1B and fig. The BD1-selective inhibitor GSK778 exhibited similar transcriptional effects compared to pan-BET inhibitors in cancer cells, consistent with previous studies showing that BD1 plays the dominant role in maintaining established transcriptional programs (Picaud et al. ≥98% (HPLC)Comparison of the binding modes of CDD-956 with BD1, CDD-1302 with BRDT-BD2 , and iBET-BD1 (GSK778) with BRD4-BD1 (Fig. View and buy high purity iBET-BD1 | GSK778 from AOBIOUS, the leading supplier of life science reagents. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models[1]. 4. If not otherwise indicated, cells were pretreated with I-BET151, iBET-BD1,. Copy Link. 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. Your information is safe with us. MR EN. In contrast to other reported domain selective molecules, these compounds showed little binding to bromodomains outside the BET fam-GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Applications Products Services Documents Support. Copy Link. Serum alanine aminotransferase (ALT)/aspartate aminotransferase (AST) < 2. Email. 1. SML3234. 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]. 8902. 33DFTG (TD139) $21. WGK 3. Available to order from Sigma-Aldrich. 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. Available to order from Sigma-Aldrich. toronto@thesgc. Email. Available to order from Sigma-Aldrich. Supplementary Materials for - Europe PMC. 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. GSK789 was derived from a series of naphthyridone ATAD2 inhibitors. GSK778 Hydrochloride. 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]). S1F, and table S1). 1. WGK 3. Applications Products Services Documents Support. Chemical Structure. GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. 9. In addition, while GSK778 phenocopied I-BET151 in terms of antiproliferative effects on a range of human cancer cells, GSK046 was less effective. Catalog No. 7 GSK046 (BD2) pIC50 = 7. INTRODUCTION. SML3234. In almost half of hepatocellular carcinoma (HCC) cases, the Akt pathway is activated. A panel of biocatalytic systems was tested to identify biocatalysts suitable for milligram scale production of metabolite M4. 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. All products from TargetMol are for Research Use Only. 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. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. Copy Link. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. All Photos (1) Documents. 2451862-42-1. But, how does GSK778 work on the target? Let’s discuss it in detail. 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). GlaxoSmithKline; BRD2, BRD3, BRD4, BRDT (BD2) GSK046; pIC50 = 7. 33DFTG (TD139) $21. GSK778: CAS Registry Number: 2451862-42-1: Molecular Weight: 511. HK EN. SML3234. GSK778 Hydrochloride. Fig. , 2016). SML3234. Membranes were blocked with 5% milk in Tris-buffered saline (TBS) with 0. GSK778 Hydrochloride. 09-Sep-2023. Description: GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). 2h 04m. PK EN. All Photos (1) Documents. 2451862-42-1: Formula: C 30 H 33 N 5 O 3: Formula Wt. 1. Safety Information. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. T9703 CAS 2451862-42-1. CAS Number: 2451862-42-1. To explore the individual functional. GD EN. Copy Link. You can also browse global suppliers,vendor,prices,Price,manufacturers of GSK484(1652591-81-5). GSK778 phenocopies the effects of pan- BET inhibitors in cancer models. GSK778 Hydrochloride. Email. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 00. 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 bromodomain (BD) is a ~110 amino acid motif that binds to acetyl-lysine modifications on histone and non-histone proteins (Dhalluin et al. 22 Early preclinical results demonstrate different phenotypic responses from domain-selective BET inhibitors and reduced toxicity when using pan-BET BD2 selective inhibitors. Available to order from Sigma-Aldrich. Applications Products Services Documents Support. Molecular Formula: C30H33N5O3. It achieves this complex task by recruiting BRD4, via a pan-BET ligand (JQ1), to the GAA repeats by using a sequence-selective DNA-binding polyamide. 0. This approachGSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. WGK. Download scientific diagram | Inhibition of CDK6 confers drug sensitivity to AKTi. First of all,. Applications Products Services Documents Support. GSK778 phenotyping the role of pan-BET inhibitors in cancer models. This approach implicates the use of. 1 μg/mL, which we determined was the equivalent of 1000 units/mL (U/mL) via in-house Griess assay. In addition, while GSK778 phenocopied I-BET151 in terms of antiproliferative effects on a range of human cancer cells, GSK046 was less effective. We do not sell to patients. All Photos (1) Documents. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. MS40229, and GSK77830. 999. Preis und Verfügbarkeit anzeigen. Primary Citation of Related Structures: 6SWN, 6SWO, 6SWP, 6SWQ. Copy Link. E-newsletter Get updates ,discounts and special offers. GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). GSK778 phenocopies the. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. K. IQ EN. BG EN. Selectivity profile of I-BET151, iBET-BD1 (GSK778), and iBET-BD2 (GSK046). GSK778 reduces the production of anti-keyhole limpet. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. PubMed Abstract: The two tandem bromodomains of the BET (bromodomain and extraterminal domain) proteins enable chromatin binding to facilitate transcription. ≥98% (HPLC)Shop Medchemexpress LLC HY-136570 5mg , GSK778 CAS:2451862-42-1 Purity:>98% at Fishersci. SML3234. Buy Epigenetic Reader Domain inhibitor GSK778 (iBET-BD1) from. and GSK778 (iBET-BD1), a BD1-selective in-hibitor (see the figure). Email. S1F, and table S1). 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. MOscan analysis of GSK778 indicated the binding of this compound only to BET bromodomains with strong binding to BET BD1 domains while weakly binding to BET BD2 domains. 61 bulk manufacturing, sourcing and procurement. Applications Products Services Documents Support. GSK778 Hydrochloride. Saturday. Resolution:Description 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. CAS: 2451862-42-1 (free base) Chemical Name: GSK778 2HCl; 4-(2-(Methoxymethyl)-1-((R)-1-phenylethyl)-8-(((S)-pyrrolidin-3-yl)methoxy)-1H. 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. Dagrocorat. Lymphoma Non. 53 reported the development route of iBET-BD1 from a pan-BET imidazoquinolinone-based inhibitor with a slight BD1-bias, iBET151. COO/ COA. 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. Despite their profound preclinical efficacy, the clinical utility of pan-inhibitors is limited due to observed cytotoxicicities. I-BET151, GSK778, GSK046 and GSK620 are available from R. Available to order from Sigma-Aldrich. SML3234. (C) X-ray crystal structure of I-BET151 in. PubMed Abstract: The two tandem bromodomains of the BET (bromodomain and extraterminal domain) proteins enable chromatin binding to facilitate transcription. 14 GSK778, another pan-D1-selective inhibitor (Figure 1A), was recently reported. 11 - Combustible Solids. Open in a separate window. Fig. Applications Products Services Documents Support. The two. (a) Phylogenetic tree of bromodomains, with available chemical probes noted; the BET subfamily and the divergence of its first and second bromodomains, BD1 and BD2, are highlighted (adapted from chromohub. Available to order from Sigma-Aldrich. ≥98% (HPLC) All Photos (1)MS40224, and GSK77825. The BD2 selective inhibitor RVX-208 could significantly decrease atherosclerosis in hyperlipidemic apolipoprotein E-deficient mice 14 , and increase high-density lipoprotein cholesterol as well as apolipoprotein A-1 in monkeys 15 . 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. Available to order from Sigma-Aldrich. 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. Solubility: Soluble in DMSO. ≥98% (HPLC)Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Apart from BRDs, YEATS family members have been. (B) Compound binding to the individual bromodomains of BD1 (orange) and BD2 (cyan) of BET tandem bromodomains in TR-FRET assays. GSK778 inhibits proliferation, induces a cell cycle arrest and Apoptosis . iBET-BD1 phenocopies the effects of pan-BET inhibitors in cancer models, whereas iBET-BD2 is predominantly effective in. 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. their selectivity. Preis und Verfügbarkeit anzeigen. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 27,42 The second-generation BRD4 inhibitors are mainly synthesized by proteolysis targeting chimera (PROTAC) technology. GSK778. Applications Products Services Documents Support. We would like to show you a description here but the site won’t allow us. Applications Products Services Documents Support. M28749 CAS No. Storage Class Code. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. GSK778 Hydrochloride. GSK778 phenocopies the. Well-characterized small molecules are essential tools for studying the biology and therapeutic relevance of a target protein. GSK778 : Catalog Number: M10828: CAS Number: 2451862-42-1: 1. WGK. (B) Compound binding to the individual bromodomains of BD1 (orange) and BD2 (cyan) of BET tandem bromodomains in TR-FRET assays. (B). 14 Whereas a pan-BET inhibitor impeded differentiation of oligodendrocytes, olinone induced this process. GSK778 Hydrochloride. 5. 11 - Combustible Solids. SynTEF1, a prototype synthetic genome reader/regulator (SynGR), was designed to target GAA triplet repeats and restore the expression of frataxin (FXN) in Friedreich’s ataxia patients. 125 nM (MV-4−11 cells) ≤. comThe 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. COO/ COA. 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). GSK778 is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). GSK778 (iBET-BD1) is a strong BD1 bromodomain inhibitor of the BET proteins, with IC50 value of 75 nM for BRD2 BD1, 41 nM for BRD3 BD1, 41 nM for BRD4 BD1, and 143 nM for BRDT BD1. 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. (B) Compound binding to the individual bromodomains of BD1 (orange) and BD2 (cyan) of BET tandem bromodomains in TR-FRET assays. Chemical probes are cell-active, selective, highly validated research tools that can be used to decipher the biology of their target. Coordinates and structure factors have been deposited in the Protein Data Bank (PDB) with identification code 6SWN, 6SWO, 6SWP and 6SWQ. Domain-Selective Targeting (BD1 or BD2 Targeting) The BET protein family of BCPs comprise the ubiquitously expressed BRD2, BRD3, and BRD4 and the testis-restricted BRDT, all of which harbor two highly conserved tandem bromodomains, BD1 and BD2,. GSK778 phenotyping the role of pan-BET inhibitors in cancer models. Available to order from Sigma-Aldrich. CA EN. COO/ COA. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. 1. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. BRD4 inhibitors effectively penetrate the blood-brain barrier and target glioma tumor tissues but have little effect on normal brain tissues. Email. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. AU EN. 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. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Copy Link. Les inhibiteurs spécifiques du. To explore the individual functional contributions of BD1 and BD2 in biology and therapy, selective BD1 and BD2 inhibitors have been developed: GSK778 and GSK046 (termed iBET-BD1 and iBET-BD2, respectively) . 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. Structural Genomics Consortium MaRS Centre, South Tower 101 College St. Before sharing sensitive information, make sure you’re on a federal government site. Miransertib is a highly selective, orally active, pan-Akt inhibitor. GM6001. Email. , 1999). ZA EN. 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. • (+)-JQ1 has 45–50 times more binding capabilities to BD1 compared with BD2 (Chen et al. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. SML3234. GSK778 phenocopies the. ≥98% (HPLC)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. M28843 CAS No. GSK778 (iBET-BD1) potently inhibits numerous cancer cells proliferation, inducing cell cycle arrest and apoptosis. , 2013). Copy Link. 65 In turn, pan-BD2 inhibitors (which have higher inhibitory activity for BD2 than BD1 of BET family members) are. 00. All Photos (1) Documents. Solubility: Soluble in DMSO. We would like to show you a description here but the site won’t allow us. Email. Storage Class Code. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. 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]. Louis Gilman November 13, 2023. Safety Information. Despite their profound preclinical efficacy, the clinical utility of pan-inhibitors is limited due to observed cytotoxicicities. 6147. Email: Sales@ChemShuttle. 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. Get latest info on GSK778, suppliers, manufacturers, wholesalers, traders with GSK778 prices for buying. GSK778 (iBET-BD1) 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). Applications Products Services Documents Support. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Copy Link. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. Applications Products Services Documents Support. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. LY EN. GSK778. Safety Information. Available to order from Sigma-Aldrich. GSK778 Hydrochloride. GSK778 (iBET-BD1) is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. WGK 3. Comprar GSK778 hydrochloride na CymitQuimica a partir de 181,0 € Iniciar Sessão Criar uma conta. GSK778 was found as a BD1 selective inhibitor with 130 times higher affinity for BD1 than BD2 5. , 2020; Gilan et al. Applications Products Services Documents Support. Guanidine hydrochloride; Useful for denaturing proteins and solubilization of inclusion bodies. Available to order from Sigma-Aldrich. K. ≥98% (HPLC) All Photos (1)GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Shelf Life: >3 years if stored properly. Endoplasmic Reticulum Stress Modulator (ERSM) Epigenetics Resch Products. RVX-297 is a 4-quinazolinone derivative related to RVX-208 with an alkylpyrrolidine side chain off the di-methyl substituted phenyl ring (Fig. Inhibitor/agonist potency: goal is < 50 nM (IC 50, K D) Surpasses criterion: :BET mutant TR-FRET assay: BRD2 (BD1) pIC 50 = 7. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. SignificanceBET bromodomain inhibition is therapeutic in multiple diseases; however, pan-BET inhibitors have induced significant myelosuppression and gastrointestinal toxicity, perhaps due to inhib. GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Available to order from Sigma-Aldrich. Comprar GSK778 na CymitQuimica. PL EN. All Photos (1) Documents. CAS Number: 2451862-42-1. 5 upper limit of normal (ULN) Total bilirubin < 1. Email. I-BET151, GSK778, GSK046 and GSK620 are available from R. Their affinities for the individual bromodomains of the BET family were initially determined by TR-FRET (Fig. P (moc. ≥98% (HPLC) All Photos (1)GSK778 (iBET-BD1) هو مثبط قوي وانتقائي BD1 bromodomain لبروتينات BET ، مع IC50s 75 نانومتر (BRD2 BD1) ، 41 نانومتر (BRD3 BD1) ، 41 نانومتر (BRD4 BD1) ، و 143 نانومتر (BRDT BD1) ، على التوالى. 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. Description: GSK778, also known as iBET-BD1, is a potent and selective inhibitor of bromodomain (BRD) BD1, with IC50s of 75 nM (BRD2 BD1). org); (b) BET BD1-selective GSK778 bound to BRD4-BD1 (in cyan,. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Available to order from Sigma-Aldrich. GSK778 Hydrochloride. Copy Link. Email. Applications Products Services Documents Support. , 2010), I-BET762 (Nicodeme et al. GSK778 Hydrochloride. Contains a pharmaceutically active ingredient. 1 Selectivity profile of I-BET151, iBET-BD1 (GSK778), and iBET-BD2 (GSK046). All Photos (1) Documents. No; GlaxoSmithKlineBy surface plasmon resonance binding assay, GSK778 is > 130-fold selective for BD1, whereas GSK046 is > 300-fold selective for BD2 . Applications Products Services Documents Support. The . R. Available to order from Sigma-Aldrich. 27, 42. GSK778 (iBET-BD1) is a potent and selective inhibitor of bromodomain (BRD) BD1. WGK. Copy Link. Applications Products Services Documents Support. They are epigenetic readers of histone acetylation with broad specificity. , Suite 700 Toronto, ON, M5G 1L7 Canada +1 416-946-0237. Safety Information. The two tandem bromodomains of the BET proteins enable chromatin binding to facilitate transcription. GSK778 Hydrochloride. JP EN. Some, such as ABBV-744 and GSK778, are optimized for greater selectivity for one of two distinct BET protein bromodomains in an effort to improve therapeutic indices [55, 56]. We would like to show you a description here but the site won’t allow us. GSK778 Hydrochloride is a potent and highly selective inhibitor of bromodomain BD1 of BRD2, BDR3, BRD4, BRDT. Last but not the least, GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model.