VE-821 - Moligand™, 10mM in DMSO , Inhibitor of ATR serine/threonine kinase, CAS No.1232410-49-9, Inhibitor of ATR serine/threonine kinase

CAS: 1232410-49-9 Cat. No.: V408304 Molecular Weight: 368.41 PubChem CID: 51000408

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

2-Pyrazinecarboxamide, 3-amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

VE-821 is a potent and selective ATP competitive inhibitor ofATRwithKi/IC50of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.
In vitro

VE-821 shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-PK, mTOR and PI3K (K_is of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively. VE-821 alone commits a large fraction of cancer cell populations to death, but it only reversibly limits cell cycle progression in normal cells, with minimal death or long-term detrimental effects. VE-821 along with cisplatin treatment shows the most marked synergy. VE-821 inhibits H2AX cell growth with IC50 of 800 nM.

In vivo

Cell Data

cell lines：

Concentrations：--

Incubation Time：96 hours

Powder Purity:≥99%

Specifications

Synonyms

2-Pyrazinecarboxamide, 3-amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

VE-821 is a potent and selective ATP competitive inhibitor of ATR with K_i/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of ATR serine/threonine kinase

Names and Identifiers

• Isomeric SMILES: CS(=O)(=O)C1=CC=C(C=C1)C2=CN=C(C(=N2)C(=O)NC3=CC=CC=C3)N
• PubChem CID: 51000408
• Molecular Weight: 368.41

Associated Targets(Human)

PRKDC Tchem DNA-dependent protein kinase catalytic subunit (1 Activities)

Discover Target: PRKDC

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ATR Tchem Serine/threonine-protein kinase ATR (2 Activities)

Discover Target: ATR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 56 mg/mL (201.62 mM); Ethanol: 8 mg/mL (28.8 mM); Water: Insoluble

References

1. Zhao Mengjie, Li Yanhui, Lu Chenfei, Ding Fangshu, Xu Miao, Ge Xin, Li Mengdie, Wang Zhen, Yin Jianxing, Zhang Junxia, Wang Xiefeng, Ge Zehe, Xiao Hong, Xiao Yong, Liu Hongyi, Liu Wentao, Cao Yuandong, Wang Qianghu, You Yongping, Wang Xiuxing, Yang Kun, Shi Zhumei, Qian Xu.  (2023)  PGC1α Degradation Suppresses Mitochondrial Biogenesis to Confer Radiation Resistance in Glioma.  CANCER RESEARCH,  83  (7): (1094-1110).  [PMID:36696363] [10.1158/0008-5472.CAN-22-3083]