Description
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
Product information
Molecular Weight: 419.89
Formula: C18H18ClN5O3S
Chemical Name: (5E)-5-{[2-oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl]methylidene}-1,3-thiazolidine-2,4-dione hydrochloride
Smiles: Cl.O=C1NC=C(/C=C2/SC(=O)NC/2=O)C=C1C1C=NC(=CC=1)N1CCNCC1
InChiKey: PSLSZGRUEDWPNC-XHIXCECLSA-N
InChi: InChI=1S/C18H17N5O3S.ClH/c24-16-13(7-11(9-21-16)8-14-17(25)22-18(26)27-14)12-1-2-15(20-10-12)23-5-3-19-4-6-23;/h1-2,7-10,19H,3-6H2,(H,21,24)(H,22,25,26);1H/b14-8+;
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 8.33 mg/mL (19.84 mM; Need ultrasonic). H2O : 9.09 mg/mL (21.65 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: ≥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:
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2. Protein kinase inhibitors 1 (Compound A64) is not an effective Cdk1 inhibitor (IC50 > 10 μM). A64 is moderately selective across a panel of kinases, with Kds of 3.7 nM (PIM3), 6.1 nM (CSNK2A2), 6.1 nM (CSNK2A2), 8.8 nM (DYRK1A), 9.5 nM (DAPK1), 31 nM (CSNK2A1), 37 nM (PIM1), 130 nM (DRAK2), 150 nM (CLK2), 190 nM (DRAK1), 220 nM (ULK2), 240 nM (CLK1), 250 nM (DYRK2), and 390 nM (ERK8) and IC50s of 19 nM (DYRK1A), 62 nM (DYRK1B), and 74 nM (HIPK2).
Products are for research use only. Not for human use.
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