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C3742

Sigma-Aldrich

Chk2 Inhibitor II hydrate

≥98% (HPLC)

Synonyme(s) :

2-(4-(4-Chlorophenoxy)phenyl)-1H-benzimidazole-5-carboxamide hydrate

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About This Item

Formule empirique (notation de Hill):
C20H14ClN3O2 · xH2O
Numéro CAS:
516480-79-8
Poids moléculaire :
363.80 (anhydrous basis)
Numéro MDL:
MFCD08276917
Code UNSPSC :
12352200
ID de substance PubChem :
24724438
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

solid

Couleur

off-white to tan

Solubilité

DMSO: ≥2 mg/mL (warmed)

Auteur

Johnson & Johnson

Température de stockage

2-8°C

Chaîne SMILES 

O=C(C1=CC=C2C(N=C(C3=CC=C(OC4=CC=C(Cl)C=C4)C=C3)N2)=C1)N

InChI

1S/C20H14ClN3O2/c21-14-4-8-16(9-5-14)26-15-6-1-12(2-7-15)20-23-17-10-3-13(19(22)25)11-18(17)24-20/h1-11H,(H2,22,25)(H,23,24)

Clé InChI

UXGJAOIJSROTTN-UHFFFAOYSA-N

Informations sur le gène

human ... CHEK2(11200)

Actions biochimiques/physiologiques

Chk2 Inhibitor II is a checkpoint kinase 2 inhibitor, which controls the p53 response to DNA breaks induced by radiation, leading to apoptosis. Protection of T-cells from apoptosis implies use as an adjuvant for radiation therapy in cancer. IC50 = 15 nM; Ki = 37 nM. Chk2 Inhibitor II shows 1000-fold greater selectivity for the Chk2 serine/threonine kinase than for the Cdk1/B and CK1 kinases (for which IC50 = 12 μM and 17 μM, respectively). Chk2 Inhibitor II weakly inhibits a panel of 31 other kinases (<25% inhibition at a concentration of 10 μM and prevents apoptosis of human CD4+ and CD8+ T-cells subjected to ionizing radiation (EC50 = 3 μM and 7.6 μM, respectively).

Caractéristiques et avantages

This compound was developed by Johnson & Johnson. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Ran Guo et al.
Antioxidants (Basel, Switzerland), 11(6) (2022-06-25)
Reactive oxygen species (ROS) act as a signaling intermediate to promote cellular adaptation to maintain homeostasis by regulating autophagy during pathophysiological stress. However, the mechanism by which ROS promotes autophagy is still largely unknown. Here, we show that the ATM/CHK2/ULK1
Wenyu Zhang et al.
Cell death and differentiation, 27(2), 482-496 (2019-06-19)
Both the stress-response protein, SIRT1, and the cell cycle checkpoint kinase, CHK2, play critical roles in aging and cancer via the modulation of cellular homeostasis and the maintenance of genomic integrity. However, the underlying mechanism linking the two pathways remains
Lauren E Williamson et al.
Cell, 183(7), 1884-1900 (2020-12-11)
Eastern equine encephalitis virus (EEEV) is one of the most virulent viruses endemic to North America. No licensed vaccines or antiviral therapeutics are available to combat this infection, which has recently shown an increase in human cases. Here, we characterize
Michael P Doyle et al.
Cell reports, 36(9), 109628-109628 (2021-09-02)
Hendra virus and Nipah virus (NiV), members of the Henipavirus (HNV) genus, are zoonotic paramyxoviruses known to cause severe disease across six mammalian orders, including humans. We isolated a panel of human monoclonal antibodies (mAbs) from the B cells of
Sandhya Bangaru et al.
Cell, 177(5), 1136-1152 (2019-05-18)
Here, we describe the discovery of a naturally occurring human antibody (Ab), FluA-20, that recognizes a new site of vulnerability on the hemagglutinin (HA) head domain and reacts with most influenza A viruses. Structural characterization of FluA-20 with H1 and
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