WM-3835

SKU: orb1218406

Description

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.

Key Properties

• CAS Number: 2229025-70-9
• MW: 400
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₇FN₂O₄S
• SMILES: CC1=CC(C2=CC=CC=C2)=CC(C(NNS(=O)(C3=CC(O)=CC=C3)=O)=O)=C1F
• Target: Apoptosis
• Solubility: DMSO:250 mg/mL (624.34 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  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 days. Result: Potently inhibited pOS-1 xenograft growth.
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• In Vitro:
  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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Apoptosis