详情描述
CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Kiapp) of 330 nM.
Product information
CAS Number: 41179-33-3
Molecular Weight: 349.40
Formula: C22H20FNO2
Chemical Name: 4-{2'-fluoro-[1, 1'-biphenyl]-4-yl}-N-(4-hydroxyphenyl)butanamide
Smiles: OC1C=CC(=CC=1)NC(=O)CCCC1C=CC(=CC=1)C1=CC=CC=C1F
InChiKey: ODYAQBDIXCVKAE-UHFFFAOYSA-N
InChi: InChI=1S/C22H20FNO2/c23-21-6-2-1-5-20(21)17-10-8-16(9-11-17)4-3-7-22(26)24-18-12-14-19(25)15-13-18/h1-2,5-6,8-15,25H,3-4,7H2,(H,24,26)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (286.20 mM; Need ultrasonic)
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: ≥360 days 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:
CMPD1 does not inhibit p38 MAPK-mediated phosphorylation of other two substrates, MBP and ATF2. CMPD1 induced mitotic arrest and apoptosis in U87 cells. CMPD1 inhibits tubulin polymerisation in glioblastoma cells.
References:
- Gurgis F, et al. Cytotoxic activity of the MK2 inhibitor CMPD1 in glioblastoma cells is independent of MK2. Cell Death Discov. 2015 Sep 7;1:15028.
- Davidson W, er al. Discovery and characterization of a substrate selective p38alpha inhibitor. Biochemistry. 2004 Sep 21;43(37):11658-71.
- Phoa AF, et al. Pharmacology of novel small-molecule tubulin inhibitors in glioblastoma cells with enhanced EGFR signalling. Biochem Pharmacol. 2015 Dec 15;98(4):587-601.
Products are for research use only. Not for human use.