BML-277 (Synonyms: Chk2 Inhibitor II)

Name: BML-277
Brand: MedChemExpress
SKU: HY-13946
Rating: 5.0 (9 reviews)

Cat. No.: HY-13946 Purity: 99.67%: Data Sheet
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BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC₅₀ of 15 nM.

For research use only. We do not sell to patients.

CAS No. : 516480-79-8

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
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Customer Review

Based on 9 publication(s) in Google Scholar

9 Publications Citing Use of MCE BML-277

Cell Proliferation/Viability Assay

Flow Cytometry

Histological Imaging/Staining

In Vivo Imaging

: BML-277 purchased from MedChemExpress. Usage Cited in: Mol Med. 2025 May 29;31(1):211. [Abstract]; Representative images of mtROS levels in BMDMs infected with S. aureus for 12 h and treated with GDC-0973 or LY3214996 and BML-277 (10 µM). Scale bars, 5 μm.

: BML-277 purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2024 Oct 30;23(1):242. [Abstract]; MTT viability of 4T1 and ID8agg cells treated with vehicle or 2.5 μM BML-277 ± rabuserib for 96 hours. MTT viability of 4T1 and ID8agg cells treated with BML-277 as above ± ATRi for 96 hours.

: BML-277 purchased from MedChemExpress. Usage Cited in: Hum Reprod. 2023 Sep 5;38(9):1769-1783. [Abstract]; H&E staining and the ratio of apoptotic primordial oocytes in human foetal ovaries treated with cisplatin alone or along with CHEK1 inhibitor (CK1) or CHEK2 inhibitor (CK2) (BML-277) (25 µM; 26 h). Red arrows indicate healthy primordial follicles, and yellow arrows indicate apoptotic primordial follicles.

: BML-277 purchased from MedChemExpress. Usage Cited in: Hum Reprod. 2023 Sep 5;38(9):1769-1783. [Abstract]; BML-277 (CK2) (25 µM; 26 h). Analysis of apoptosis-related proteins (BAX, BCL2, γH2AX, NOXA, and PUMA) in each group. Western blot analysis of human foetal ovaries treated with cisplatin or CHEK1/CHEK2 inhibitors showed decreased expression of apoptosis-associated proteins upon exposure to CK1 or CK2.

: BML-277 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2022 Jan 21;8(3):eabj8357. [Abstract]; Representative cell viability upon the treatment of 2 nM E7107, 50 μM BML277, or 2 nM E7107 + 50 μM BML277 (BML-277) in patient samples for 24 hours.

: BML-277 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2022 Jan 21;8(3):eabj8357. [Abstract]; Luciferase-expressing CUTLL1 cells were injected into immunocompromised mice via tail vein coupled to mouse treated with E7107 (at 5 mg/kg per day), BML277 (BML-277) (at 1 mg/kg per day), or E7107 and BML277 (“Comb”). Leukemic burden was assessed via blast detection in mouse body using bioluminescence and in vivo imaging system equipment twice per week.

: BML-277 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Jun 15;11(6):464. [Abstract]; MCF7, 10AKRAS, 7E6 and MDA-MB-231 cell lines are treated with increasing concentration of CHEK2 inhibitor BML (BML-277) (1.25-5 nM) for 24 h and followed with a 24 h treatment of Eto at 5 μg/ml. Cells are harvested to stain with PI followed with FACS analysis.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC₅₀ of 15 nM.

IC₅₀ & Target^[1]

Chk2

15 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
T-cell	EC₅₀	7600 nM Compound: K00247, Benzimidazol1	Effect of gamma irradiation-induced apoptosis in human CD8+ T cells Effect of gamma irradiation-induced apoptosis in human CD8+ T cells	[PMID: 18077363]
T-cell	EC₅₀	3 μM Compound: K00247, Benzimidazol1	Effect of gamma irradiation-induced apoptosis in human CD4+ T cells Effect of gamma irradiation-induced apoptosis in human CD4+ T cells	[PMID: 18077363]

In Vitro

BML-277 is an ATP-competitive inhibitor of Chk2 that dose dependently protects human CD4⁺ and CD8⁺ T-cells from apoptosis due to ionizing radiation. BML-277 efficiently rescues both T-cell populations from radiation-induced apoptosis in a dose-dependent manner with an observed EC₅₀ of 3 7.6 μM. The concentration of BML-277 required for radioprotection is consistent with the biochemical measurement of chk2 inhibition. Providing theK_m of ATP for Chk2 is determined to be 99 μM and the K_i for BML-277 is 37 nM, and assuming that the intracellular ATP concentration is 10 mM, a 5 μM concentration of BML-277 would be expected to produce 42% inhibition of intracellular chk2^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

363.80

Formula

C₂₀H₁₄ClN₃O₂

CAS No.

516480-79-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC(C=C1)=CC=C1OC(C=C2)=CC=C2C3=NC4=CC(C(N)=O)=CC=C4N3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 22.22 mg/mL (61.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7488 mL	13.7438 mL	27.4876 mL
5 mM	0.5498 mL	2.7488 mL	5.4975 mL
10 mM	0.2749 mL	1.3744 mL	2.7488 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (4.59 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (4.59 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.67 mg/mL (4.59 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.67%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (246 KB) HNMR (265 KB) RP-HPLC (222 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Arienti KL, et al. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85. [Content Brief]

Kinase Assay ^[1]	Activity of inhibitors of chk2 is determined by incubating inhibitory compounds with recombinant full-length chk2: 5 nM recombinant human Chk2, 50 mM HEPES (pH 7.4), 100 mM NaCl, 10 mM MgCl₂, 25 μM synthetic peptide substrate (biotin-SGLYRSPSMPENLNRPR, 1 μM ATP, 50 μCi/mL [γ-³³P] ATP, and a protease inhibitor mixture. The reaction mixtures are incubated at 37°C for 3 h, and the peptide substrate is captured on streptavidin conjugated to agarose beads. The agarose beads are washed repeatedly with a 0.1% solution of Tween-20 in phosphate-buffered saline, pH 7.4. Enzyme activity at different BML-277 concentrations (6.25, 12.5, 25, 50, 100, and 200 nM) is determined by measuring the amount of radioactive phosphate bound to the substrate peptide by scintillation counting. In kinetic experiments ATP concentration is varied while the ratio between unlabeled and [γ-³³P] labeled ATP is kept constant. Reactions are stopped at different time points by addition of 50 mM cold ATP and samples are kept on ice during further processing^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	To determine the radioprotective effect of Chk2 inhibitors, purified T-cells are incubated at 100 000 cells per well in BML-277 (10^2.5 nM, 1 μM, 10^0.5 μM, 10 μM, and 10^1.5 μM) or vehicle (DMSO) at varying concentrations in 96-well stripwells for 1 h. Cells are then exposed to a dose of 0 or 10 Gy gamma irradiation from a ¹³⁷Cs source at a dose rate of 3.65 Gy/min and then returned to the incubator for a further 24 h. Cells are stained with Annexin V-FITC and propidium iodide, according to the manufacturers protocol. Apoptotic and surviving cells are quantitated with a FACSCalibur FACS machine. Data are reported as percent recovery-or the number of survivors from treatment groups minus the number of cells surviving in the irradiated control group divided by the number of surviving cells in the untreated control groups^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Arienti KL, et al. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7488 mL	13.7438 mL	27.4876 mL	68.7191 mL
	5 mM	0.5498 mL	2.7488 mL	5.4975 mL	13.7438 mL
	10 mM	0.2749 mL	1.3744 mL	2.7488 mL	6.8719 mL
	15 mM	0.1833 mL	0.9163 mL	1.8325 mL	4.5813 mL
	20 mM	0.1374 mL	0.6872 mL	1.3744 mL	3.4360 mL
	25 mM	0.1100 mL	0.5498 mL	1.0995 mL	2.7488 mL
	30 mM	0.0916 mL	0.4581 mL	0.9163 mL	2.2906 mL
	40 mM	0.0687 mL	0.3436 mL	0.6872 mL	1.7180 mL
	50 mM	0.0550 mL	0.2749 mL	0.5498 mL	1.3744 mL
	60 mM	0.0458 mL	0.2291 mL	0.4581 mL	1.1453 mL

BML-277 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BML-277516480-79-8Chk2 Inhibitor IIBML277BML 277Checkpoint Kinase (Chk)ApoptosisInhibitorinhibitorinhibit

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BML-277 (Synonyms: Chk2 Inhibitor II)

Customer Review

BML-277 Related Antibodies

9 Publications Citing Use of MCE BML-277

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•Related Small Molecules:

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View All Checkpoint Kinase (Chk) Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

BML-277 Related Antibodies

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Complete Stock Solution Preparation Table

BML-277 Related Classifications

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