A BET family protein inhibitor; binds to BD1 in BRD2

PLX51107 – 5 mg

Brand:
Cayman
CAS:
1627929-55-8
Storage:
-20
UN-No:
Non-Hazardous - /

PLX51107 is a bromodomain and extra terminal domain (BET) family protein inhibitor.{61018} It binds to bromodomain 1 (BD1) in bromodomain-containing protein 2 (BRD2), BRD3, BRD4, and BRDT (Kds = 1.6, 2.1, 1.7, and 5 nM, respectively), as well as BD2 (Kds = 5.9, 6.2, 6.1, and 120 nM, respectively). It also binds to the bromodomains of CBP and p300 (Kds = ~100 nM for both). PLX51107 (0.1-10 µM) inhibits CpG-induced proliferation of primary chronic lymphocytic leukemia (CLL) cells. In vivo, PLX51107 (0.5-10 mg/kg) inhibits Ba/F3 cell-induced splenomegaly in mice. It also reduces tumor volume and increases survival in YUMM3.3 and D4M3.A mouse syngeneic B-RAFV600E mutant melanoma models.{61019}  

 

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SKU: 30742 - 5 mg Category:

Description

A BET family protein inhibitor; binds to BD1 in BRD2, BRD3, BRD4, and BRDT (Kds = 1.6, 2.1, 1.7, and 5 nM, respectively), as well as BD2 (Kds = 5.9, 6.2, 6.1, and 120 nM, respectively); binds to bromodomains of CBP and p300 (Kds = ~100 nM for both); inhibits CpG-induced proliferation of primary CLL cells from 0.1-10 µM; inhibits Ba/F3 cell-induced splenomegaly in mice from 0.5-10 mg/kg; reduces tumor volume and increases survival in YUMM3.3 and D4M3.A mouse syngeneic B-RAFV600E mutant melanoma models

Formal name: 4-[6-(3,5-dimethyl-4-isoxazolyl)-1-[(1S)-1-(2-pyridinyl)ethyl]-1H-pyrrolo[3,2-b]pyridin-3-yl]-benzoic acid

Synonyms: 

Molecular weight: 438.5

CAS: 1627929-55-8

Purity: ≥98%

Formulation: A solid

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