| Bioactivity | INCB-057643 is a novel, orally bioavailable BET inhibitor. | ||||||||||||
| Invitro | INCB-057643 is a novel, orally bioavailable BET inhibitor. INCB-057643 inhibits binding of BRD2/BRD3/BRD4 to an acetylated histone H4 peptide in the low nM range, and is selective against other bromodomain containing proteins. In vitro analyses show that INCB-057643 inhibits proliferation of human AML, DLBCL, and multiple myeloma cell lines, with a corresponding decrease in MYC protein levels. Cell cycle analyses indicate that G1 arrest and a concentration-dependent increase in apoptosis are seen within 48 hours of treatment with INCB-057643[1]. | ||||||||||||
| Name | INCB-057643 | ||||||||||||
| CAS | 1820889-23-3 | ||||||||||||
| Formula | C20H21N3O5S | ||||||||||||
| Molar Mass | 415.46 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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