I-BET762

SKU: orb1307159

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Description

Molibresib (GSK525762) is a potent and selective BET bromodomain inhibitor with an IC50 of approximately 35 nM. It is widely used in cancer research, demonstrating activity in both in vitro assays and in vivo models for studying oncology and transcriptional regulation.

Research Area

Epigenetics & Chromatin, Immunology & Inflammation

Images & Validation

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Key Properties

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CAS Number	1260907-17-2
MW	423.90
Purity	>98%
Formula	C₂₂H₂₂ClN₅O₂
SMILES	CCNC(=O)C[C@@H]1N=C(c2ccc(Cl)cc2)c2cc(OC)ccc2-n2c(C)nnc12
Target	Bromodomain
Solubility	Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml)

Bioactivity

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Target IC50	BET proteins:35 nM
In Vivo	At day 2 of differentiation, I-BET-762 treatment altered cytokine production in CD4+ T cells, up-regulating the expression of some anti-inflammatory gene products and down-regulating the expression of some pro-inflammatory cytokines.I-BET-762 inhibited the binding of bromodomain and additional terminal domain proteins and BRD2/3/4 to the tandem bromodomain of the BET (Kd: 50.5-61.3 nM). In FRET analysis, displacement of the BET tandem bromodomain a tetraacetylated H4 peptide (IC50: 32.5-42.5 nM). Read more...
In Vitro	At day 2 of differentiation, I-BET-762 treatment altered cytokine production in CD4+ T cells, up-regulating the expression of some anti-inflammatory gene products and down-regulating the expression of some pro-inflammatory cytokines.I-BET-762 inhibited the binding of bromodomain and additional terminal domain proteins and BRD2/3/4 to the tandem bromodomain of the BET (Kd: 50.5-61.3 nM). In FRET analysis, displacement of the BET tandem bromodomain a tetraacetylated H4 peptide (IC50: 32.5-42.5 nM). Read more...
Cell Research	CD4+ T cells are isolated from lymph nodes and spleens of 10- to 12-wk old mice and activated with plate bound anti-CD3 and anti-CD28 antibodies in the presence of indicated cytokines. I-BET-762 compounds is included during the 60–72 h of initial activation. Over the course of 5 d of T-cell culture and expansion, the compounds is diluted 12-fold relative to the starting concentrations.(Only for Reference) Read more...

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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GSK525762

Quality Guarantee

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Compound Identifiers

PubChem CID

46943432 ↗

Key Properties

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No computed properties available.

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I-BET762 (orb1307159)

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CAS Number:	1300019-38-8
MW:	396.83
Formula:	C₂₀H₁₇ClN₄O₃

CAS Number:	1260530-25-3
MW:	423.9
Formula:	C₂₂H₂₂ClN₅O₂

Purity:	>98% (HPLC)
CAS Number:	1260907-17-2
MW:	423.8954
Formula:	C₂₂H₂₂ClN₅O₂

I-BET762

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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I-BET762 (orb1307159)

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