I-BET762 (Molibresib) (GSK525762) - Chemietek

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Home > Epigenetics Resch Products > BET Family Protein Inhibitors > I-BET762 (Molibresib) (GSK525762)

I-BET762 (Molibresib) (GSK525762)

I-BET762 (Molibresib) (GSK525762) is a cell-permeable benzodiazepine-based inhibitor of BET (bromodomain and extra terminal domain) proteins, BRD2, BRD3 and BRD4, binds to the tandem bromodomains of BET with Kd of 50.5–61.3 nM, displacing a tetra-acetylated H4 peptide prebound to tandem bromodomains of BET with IC50 of 32.5–42.5 nM in FRET analysis. I-BET-762 occupies the acetyl-lysine binding pocket of BET proteins and inhibits binding of BET proteins to acetylated histones, thus disrupts the formation of the chromatin complexes essential for expression of inflammatory genes.

Catalog NO:	CT-BET762
Synonym:	Molibresib, GSK525762
CAS NO:	1260907-17-2
Mol. Formula:	C₂₂H₂₂ClN₅O₂ ∙ 0.2H₂O
MW:	427.5

** in vivo Quality material. Optically Pure Source (ref 3). 99.6-100% by achiral and chiral HPLCs. A recrystallized powder, with quantitative elemental analysis. Bulk stock! Prompt.

Pricing and OrderingTechnical Data

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NO	Size	Price	In Stock	Quantity
1	10 mg	$100.00	YES
2	50 mg	$300.00	YES
3	100 mg	$490.00	YES
4	200 mg	$850.00	YES

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Solubility : Soluble in DMSO, Ethanol

Storage : Store at 0°C (short term), -20°C (long term), desiccated

Purity : ≥99.5% (HPLC at 214 and 254 nm), 100% optical purity (Chiral HPLC)

Original QC Data : HPLC-MS, ¹HNMR, Chiral HPLC, and Quantitative Elemental Analysis

Please Pick Batch NO:

I-BET762, Current Lot, Certificate of Analysis
I-BET762, lot 01, Appearance (color).pdf
C_K, I-BET762, Lot 01, HPLC-MS.pdf
C_K, I-BET762, Lot 01, Chiral HPLC.pdf
C_K, I-BET762, Lot 01, NMR in DMSO.pdf

1. Olivier Mirguet, et al., Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains, J. Med. Chem., 2013, 56 (19), pp 7501–7515

2. A. Chaidos, et al., Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762, Blood, 2014, vol. 123 no. 5, 697-705;

3. A product with the highest standard in every aspect, manifested by HPLC-MS, Chiral HPLC, NMR and Quantitative Elemental Analysis.

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