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BML-277 (Chk2 Inhibitor II) Chk inhibitor

Name: BML-277 (Chk2 Inhibitor II)
Brand: Selleck Chemicals
SKU: S8632
Availability: InStock
Rating: 5 (17 reviews)

Cat.No.S8632

BML-277 (Chk2 Inhibitor II) is an ATP-competitive inhibitor of Chk2 with IC50 of 15 nM, and it is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases. This compound dose dependently protects human CD4(+) and CD8(+) T-cells from apoptosis due to ionizing radiation.

Chemical Structure

Molecular Weight: 363.80

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Quality Control

Batch: S863201 DMSO]72 mg/mL]false]Ethanol]21 mg/mL]false]Water]Insoluble]false Purity: 99.17%

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.17

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase
Other Chk Inhibitors	Prexasertib (LY2606368) Dihydrochloride CCT245737 (SRA737) AZD7762 Rabusertib (LY2603618) MK-8776 (SCH 900776) CHIR-124 PF-477736 Prexasertib (LY2606368) GDC-0575 BBI-355

Solubility

In vitro
Batch:

DMSO : 72 mg/mL (197.91 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 21 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.600mg/ml (9.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 72 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.600mg/ml (9.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 72 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	363.80	Formula	C₂₀H₁₄ClN₃O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	516480-79-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC(=CC=C1C2=NC3=C(N2)C=C(C=C3)C(=O)N)OC4=CC=C(C=C4)Cl

Mechanism of Action

Targets/IC₅₀/Ki	Chk2 (Cell-free assay) 15 nM
In vitro	BML-277 (Chk2 Inhibitor II) shows 1,000-fold greater selectivity for the CHK2 serine/threonine kinase than for the Cdk1/B and CK1 kinases and was first discovered to be a potent, selective small molecule showing radioprotection towards human T cells. Different doses of this compound specifically inhibit CHK2 phosphorylation at Thr68 at different time course, but not CHK1 phosphorylation. Treatment with combination of it and ERK inhibitor results in substantially more apoptosis compared with treatment of either drug alone.
In vivo	SUDHL6 DLBCL xenografts mice treated every other day intraperitoneally with either vehicle, ERK inhibitor (5 mg kg−1), BML-277 (Chk2 Inhibitor II) (1 mg kg−1), or both ERK inhibitor and this compound for 20 days show no lethal toxicity, significant weight loss or any gross abnormalities. Both 5 mg/kg ERK inhibitor and 1 mg/kg of it modestly inhibit tumour growth but combined treatment with ERK inhibitor and BML-277 results in a statistically significant suppression of tumour growth.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15771432/ [2] https://pubmed.ncbi.nlm.nih.gov/21772273/

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