详情描述
Potent and selective lysine acetyltransferase KAT6A and KAT6B inhibitor (IC50 values are 8 and 28 nM, respectively). Exhibits > 10-fold selectivity for KAT6A/B over KAT7 and KAT5, and no significant activity against KAT8, KAT2A/2B, and KAT3A/B. Induces cell cycle arrest in G1/G0 in MEFs and inhibits proliferation of lymphoma cells in vitro. Cell permeant. Suitable for use in vitro.
Product information
CAS Number: 2055397-18-5
Molecular Weight: 384.42
Formula: C20H17FN2O3S
Synonym:
WM-8014
WM8014
MOZ-IN-3
MOZ-IN 3
MOZ-IN3
Chemical Name: [1,1'-Biphenyl]-3-carboxylic acid, 4-fluoro-5-methyl-, 2-(phenylsulfonyl)hydrazide
Smiles: CC1=CC(=CC(=C1F)C(=O)NNS(=O)(=O)C1=CC=CC=C1)C1=CC=CC=C1
InChiKey: PHHZKBMVRPULAW-UHFFFAOYSA-N
InChi: InChI=1S/C20H17FN2O3S/c1-14-12-16(15-8-4-2-5-9-15)13-18(19(14)21)20(24)22-23-27(25,26)17-10-6-3-7-11-17/h2-13,23H,1H3,(H,22,24)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 77 mg/mL(200.3 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
WM-8014 induces cell cycle arrest in embryonic day (E)14.5 mouse embryonic fibroblasts.Cells treated with WM-8014 failed to proliferate after ten days of treatment (IC50 2.4 μM). Higher doses of WM-8014 (up to 40 μM) did not accelerate growth arrest, which after eight days of treatment was irreversible.
In Vivo:
WM-8014 potentiates oncogene-induced senescence in a zebrafish model of hepatocellular carcinoma.
References:
- Baell JB,et al.Nature.2018;560(7717):253-257.
- Leaver DJ,et al.J Med Chem. 2019 8;62(15):7146-7159.
Products are for research use only. Not for human use.