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CPI-637 - CAS# 1884712-47-3 60010 Binding of >50% probe displacement

SKU: 10274133793

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Description

Binding of >50% probe displacement is detected for 10 kinases and of >65% for only LRRK2

Metcalf JP

32)33)34-18-26-29-30-27(35-23-7-3-4-8-23)31(26)21-6-5-15-28-17-21/h5-6

which targets only mTORC1

32)44-25(4)38)20-26(22-37)21-34(41)28(35)19-23(2)31(34)40/h19-20

CPI-637 - CAS# 1884712-47-3 60010 Binding of >50% probe displacementCPI 637, CAS No. 1884712 47 3, is a potent and selective CBP EP300 bromodomain inhibitor. The biochemical potency of CPI 637 translated well into cells (CBP BRET EC50 = 0. 3 M). CPI 637 demonstrated a >700 fold selectivity over the BET family of bromodomains (BRD4 IC50 = 11. 0 0. 6 M). CPI 637 inhibits MYC expression in AMO 1 cells (EC50 = 0. 60 M). CBP and EP300 are highly homologous, bromodomain containing transcription coactivators involved in

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