1. Protein Tyrosine Kinase/RTK
  2. DYRK
  3. Protein kinase inhibitors 1 hydrochloride

Protein kinase inhibitors 1 hydrochloride (Synonyms: (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride)

Cat. No.: HY-U00439A Purity: >98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

Protein kinase inhibitors 1 hydrochloride Chemical Structure

Protein kinase inhibitors 1 hydrochloride Chemical Structure

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 88 In-stock
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5 mg USD 80 In-stock
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10 mg USD 140 In-stock
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25 mg USD 310 In-stock
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50 mg USD 550 In-stock
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100 mg USD 990 In-stock
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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.

IC50 & Target

IC50: 74 nM (HIPK2), 136 nM (HIPK1)[1]
Kd: 9.5 nM (HIPK2)[1]

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)[1].

Molecular Weight

419.89

Formula

C₁₈H₁₈ClN₅O₃S

SMILES

O=C(NC/1=O)SC1=C\C2=CNC(C(C3=CC=C(N4CCNCC4)N=C3)=C2)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (71.45 mM; Need ultrasonic)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
References
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Protein kinase inhibitors 1 hydrochloride
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HY-U00439A
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