NHWD-870

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NHWD-870 is an effective and selective inhibitor of BET family bromodomain only binding to BRD2, BRD3, BRD4 (IC50 = 2.7 nM), and BRDT.

NHWD-870 is an effective and selective inhibitor of BET family bromodomain only binding to BRD2, BRD3, BRD4 (IC50 = 2.7 nM), and BRDT. NHWD-870 exhibits potent anti-tumor efficacies and suppresses cancer cell-macrophage interaction through the increase of tumor apoptosis and inhibition of tumor proliferation.(In Vitro):NHWD-870 exhibits mild inhibition of the hERG channel (IC50?=?5.4?μM). NHWD-870 shows robust activities inducing apoptosis and suppressing cell proliferation. NHWD-870 (0.01-10000 nM) inhibits melanoma cells (A375) with an IC50 of 2.46 nM. In H526, A2780, ES-2, and MDA-MB231 cells, NHWD-870 (0-10000 nM; 5 days) suppressed cell growth. NHWD-870 (0-50 nM; 24?hours) inhibits BRD4 phosphorylation and c-MYC expression in H526, A2780, ES-2, and MDA-MB231 cells.(In Vivo):NHWD-870 (0.75-3 mg/kg; p.o.) reduces the number of tumor associated macrophages (TAMs) in subcutaneously implanted H526 and A2780 tumors. NHWD-870 downregulated CSF1 expression in tumor cells to inhibit TAM proliferation.

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Apoptosis

Apoptosis

KLF5

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2115742-03-3

491.6

C29H29N7O

>98% (HPLC)

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N/A

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(-20℃)

With Ice Pack

≥ 2 years