BML-277 - CAS 516480-79-8
Catalog number:
516480-79-8
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H14ClN3O2
Molecular Weight:
363.80
COA:
Inquire
Targets:
Checkpoint Kinase (Chk)
Description:
BML-277 is a selective APT-competitive inhibitor of the DNA damage response signaling enzyme CHK2 ( IC50 =15 nM).
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Purity:
≥98%
Appearance:
Off-white solid
Synonyms:
Chk2 Inhibitor II; 2-[4-(4-chlorophenoxy)phenyl]-3H-benzimidazole-5-carboxamide;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
A selective APT-competitive inhibitor
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
UXGJAOIJSROTTN-UHFFFAOYSA-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)
Canonical SMILES:
C1=CC(=CC=C1C2=NC3=C(N2)C=C(C=C3)C(=O)N)OC4=CC=C(C=C4)Cl
1.The checkpoint 1 kinase inhibitor LY2603618 induces cell cycle arrest, DNA damage response and autophagy in cancer cells.
Wang FZ1, Fei HR, Cui YJ, Sun YK, Li ZM, Wang XY, Yang XY, Zhang JG, Sun BL. Apoptosis. 2014 Sep;19(9):1389-98. doi: 10.1007/s10495-014-1010-3.
Chemotherapy- or radiotherapy-induced DNA damage activates the Chk1-dependent DNA damage response (DDR) and cell cycle checkpoints to facilitate cell survival. Numerous attempts have been made to identify specific Chk1 inhibitors to enhance the efficiency of chemotherapy or radiotherapy. In this study, we investigated the molecular mechanisms underlying the antitumor activity of LY2603618, a potent and selective small molecule inhibitor of Chk1 protein kinase, in human lung cancer cells. Treatment of cancer cells with LY2603618 caused cell cycle arrest in the G2/M phase. A marked induction of DDR, including the phosphorylation of ATM, Chk2, p53 and histone H2AX, was observed after LY2603618 treatment. LY2603618 inhibited Chk1 autophosphorylation (S296 Chk1) and increased DNA damage-mediated Chk1 phosphorylation (S345 Chk1). In addition, LY2603618-treated lung cancer cells transitioned from LC3-I to LC3-II, a hallmark of autophagy. Blocking autophagy with chloroquine (CQ) further enhanced LY2603618's inhibitory effect on cell viability/proliferation.
2.The catalytic topoisomerase II inhibitor dexrazoxane induces DNA breaks, ATF3 and the DNA damage response in cancer cells.
Deng S1, Yan T, Nikolova T, Fuhrmann D, Nemecek A, Gödtel-Armbrust U, Kaina B, Wojnowski L. Br J Pharmacol. 2015 May;172(9):2246-57. doi: 10.1111/bph.13046. Epub 2015 Feb 27.
BACKGROUND AND PURPOSE: The catalytic topoisomerase II inhibitor dexrazoxane has been associated not only with improved cancer patient survival but also with secondary malignancies and reduced tumour response.
3.Targeting of Chk2 as a countermeasure to dose-limiting toxicity triggered by topoisomerase-II (TOP2) poisons.
Gokare P1,2, Navaraj A2, Zhang S1,2, Motoyama N3, Sung SS4, Finnberg NK1,2. Oncotarget. 2016 Apr 18. doi: 10.18632/oncotarget.8790. [Epub ahead of print]
The DNA damage response (DDR) gene cell cycle checkpoint kinase 2 (Chk2) triggers programmed cell death and lethal radiation-induced toxicity in mice in vivo. However, it is not well established to what extent targeting of Chk2 may protect from dose-limiting toxicities (DLT) inflicted by mainstay cancer chemotherapy. We screened different classes of chemotherapy in wild type and Chk2-deficient cells. Here we show that loss of Chk2 protect from cell death in vitro and lethal toxicity in vivo following treatment with topoisomerase II (TOP2)-inhibitors whereas no such protection was observed following treatment with topoisomerase I (TOP1) inhibitors. Furthermore, through combined in silico and functional screens of the Diversity Set II (NCI/NTP) chemical library we identified the carbanilide-derivative NSC105171, also known as ptu-23, as a novel Chk2 inhibitor (Chk2i). Indeed, NSC105171 can be administered safely to mice to countermeasure etoposide-induced toxicity.
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CAS 516480-79-8 BML-277

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