WM-3835

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

WM-3835 是一种新型、高特异性的赖氨酸乙酰转移酶 7 (KAT7、MYST2、HBO1) 小分子抑制剂，能够有效抑制 OS 细胞增殖和迁移，并导致细胞凋亡激活。

WM-3835 is a novel and high-specific small molecule?inhibitor of Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1)?, able to potently suppressed OS cell proliferation and migration, and leads to?apoptosis?activation.

WM-3835 (1-25 uM; 24-96 hours) inhibits pOS-1 cell viability in a concentration-dependent manner. WM-3835 (5 uM; 72 h) activates cell apoptosis and significantly increases TUNEL-positive nuclei in pOS-1 cells. WM-3835 (5 μM; 24 hours) downregulates MYLK-HOXA9 mRNA expression in pOS-1 cells. WM-3835 (1-25 uM) suppresses H4K12ac-H3K14ac in a dose-dependent manner. WM-3835 does not alter the expressions of HBO1 protein and total H3, H4 histones. WM-3835 (5 μM) fails to induce apoptosis and reduction of viability in HBO1-KO pOS-1 cells, koHBO1-1 and koHBO1-2, HBO1-low human osteoblasts. Cell Viability Assay Cell Line:Primary human OS (pOS-1) cells Concentration:1, 5, 10, 25 uM Incubation Time:24, 48, 72, 96 hours Result:Inhibited pOS-1 cell viability in a concentration-dependent manner. Exerted a significant anti-survival activity at least 48 h, displaying a time-dependent manner.Apoptosis Analysis Cell Line:pOS-1 cells Concentration:5 uM Incubation Time:72 hours Result:Activated cell apoptosis and significantly increases TUNEL-positive nuclei.RT-PCR Cell Line:pOS-1 cells Concentration:5 uM Incubation Time:24 hours Result:Downregulated MYLK-HOXA9 mRNA expression.

WM-3835 (10 mg/kg/day; ip; for21 days) potently inhibits pOS-1 xenograft growth in SCID mice. Animal Model:SCID mice (18-19 g, female) with pOS1 cells Dosage:10 mg/kg Administration:IP; daily; for 21 daysResult:Potently inhibited pOS-1 xenograft growth.

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Apoptosis

Apoptosis

apoptosis|Lysine Acetyltransferase 7

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2229025-70-9

400

C20H17FN2O4S

>98% (HPLC)

DMSO:250 mg/mL (624.34 mM; Need ultrasonic)

CC1=CC(C2=CC=CC=C2)=CC(C(NNS(=O)(C3=CC(O)=CC=C3)=O)=O)=C1F

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(-20℃)

With Ice Pack

≥ 2 years