1. Cell Cycle/DNA Damage
    Apoptosis
  2. Checkpoint Kinase (Chk)
    Apoptosis
  3. BML-277

BML-277 (Synonyms: Chk2 Inhibitor II)

Cat. No.: HY-13946 Purity: 98.02%
Handling Instructions

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.

BML-277 Chemical Structure

BML-277 Chemical Structure

CAS No. : 516480-79-8

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
50 mg USD 384 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target[1]

Chk2

15 nM (IC50)

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 theKm of ATP for Chk2 is determined to be 99 μM and the Ki 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].

Molecular Weight

363.80

Formula

C₂₀H₁₄ClN₃O₂

CAS No.

516480-79-8

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 22.22 mg/mL (61.08 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (4.59 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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 (102.5 nM, 1 μM, 100.5 μM, 10 μM, and 101.5 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

Purity: 98.02%

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Keywords:

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

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