[CAS NO. 2321337-71-5] Protein kinase inhibitor 1 hydrochloride
PRODUCTS SPECIFICATIONS [2321337-71-5]
DESCRIPTION [2321337-71-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 419.89 |
| Molecular Formula | C18H18ClN5O3S |
| SMILES | O=C(NC/1=O)SC1=C\C2=CNC(C(C3=CC=C(N4CCNCC4)N=C3)=C2)=O.[H]Cl |
3 Publications Citing Use of MCE
Summary
Protein kinase inhibitor 1 hydrochloride is a potent HIPK2 inhibitor, with IC 50 s of 136 and 74 nM for HIPK1 and HIPK2, and a K d of 9.5 nM for HIPK2.
IC50 & Target
|
DYRK1 |
DYRK2 |
In Vitro
Protein kinase inhibitor 1 hydrochloride is a potent HIPK2 inhibitor, with IC 50 s of 136 and 74 nM for HIPK1 and HIPK2, and a K d of 9.5 nM for HIPK2. Protein kinase inhibitor 1 (Compound A64) is not an effective Cdk1 inhibitor (IC 50 > 10 μM). A64 is moderately selective across a panel of kinases, with K d s 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 IC 50 s of 19 nM (DYRK1A), 62 nM (DYRK1B), and 74 nM (HIPK2) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 9.09 mg/mL ( 21.65 mM ; Need ultrasonic)
DMSO : 8.33 mg/mL ( 19.84 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3816 mL | 11.9079 mL | 23.8158 mL |
| 5 mM | 0.4763 mL | 2.3816 mL | 4.7632 mL |
| 10 mM | 0.2382 mL | 1.1908 mL | 2.3816 mL |
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1.
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Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.83 mg/mL (1.98 mM); Clear solution