BML-277A checkpoint kinase 2 inhibitor that inhibits T cell apoptosis

BML-277 (CAS 516480-79-8)

BML-277 | CAS 516480-79-8 is rated 4.0 out of 5 by 1.
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Application: A checkpoint kinase 2 inhibitor that inhibits T cell apoptosis
CAS Number: 516480-79-8
Purity: ≥98%
Molecular Weight: 363.8
Molecular Formula: C20H14ClN3O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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BML-277 (Chk2 Inhibitor II) is a Chk2 (checkpoint kinase 2) inhibitor. BML-277 protects T cells from apoptosis by controlling the response of p53 to radiation-induced DNA breaks. This is suggestive of BML-277's use as an adjuvant for radiation therapy in cancer. BML-277 is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases. It has also been found to weakly inhibit 31 other kinases.


References

1. Arienti, K.L. 2005. J. Med. Chem. 48(6): 1873-1885. PMID: 15771432

Physical State :
Solid
Solubility :
Soluble in DMSO (20 mg/ml), and ethanol (20 mg/ml).
Storage :
Store at -20° C
Boiling Point :
637.1° C at 760 mmHg
Density :
1.39 g/cm3
Refractive Index :
n20D 1.70
IC50 :
Chk2: IC50 = 15 nM; 35 other kinases: IC50 = 10 µM; Cdk1/B: IC50 = 12 µM; CK1: IC50 = 17 µM; Serine/threonine-protein kinase Chk2: IC50 = 16 nM (Homo sapiens); T cells subjected to ionizing radiation: EC5050 = 3-7.6µM (human)
Ki Data :
Chk2: Ki= 37 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
9969021
MDL Number :
MFCD08276917
SMILES :
C1=CC(=CC=C1C2=NC3=C(N2)C=C(C=C3)C(=O)N)OC4=CC=C(C=C4)Cl

Download SDS (MSDS)

Certificate of Analysis

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Rated 4 out of 5 by from It is reliable and be helpful in our experiment It is reliable and be helpful in our experiment.
Date published: 2015-10-16
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