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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,630 | 8-10 weeks | |
50 mg | $2,120 | 8-10 weeks | |
100 mg | $3,100 | 8-10 weeks |
Description | 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. |
Targets&IC50 | BRD4:2.7 nM |
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[1]. |
In vivo | NHWD-870 (0.75-3 mg/kg; p.o.) reduces tumor-associated macrophages (TAMs) in subcutaneous H526 and A2780 tumors by downregulating CSF1 expression in tumor cells, thereby inhibiting TAM proliferation[1]. |
Molecular Weight | 491.59 |
Formula | C29H29N7O |
Cas No. | 2115742-03-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 60 mg/mL (122.05 mM), Sonication and heating to 60℃ are recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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