In Vivo (Add solvents to the product individually and in order.)
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
40%PEG300
5%Tween80
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
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.
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
Biological Activity
Description
BML-277 (Chk2 Inhibitor II) is an 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.
Targets
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.
Single-cell suspensions are obtained from lymph node biopsies of patients diagnosed with DLBCL and are treated with DMSO, ERK inhibitor and BML-277 (Chk2 Inhibitor II) alone or in combination for 48 h after which the percentage of apoptotic cells is determined by Annexin V analysis.
CEP-1347 Boosts Chk2-Mediated p53 Activation by Ionizing Radiation to Inhibit the Growth of Malignant Brain Tumor Cells
[ Int J Mol Sci, 2024, 25(17)9473]
Mild replication stress causes premature centriole disengagement via a sub-critical Plk1 activity under the control of ATR-Chk1
[ Nat Commun, 2023, 14(1):6088]
Suppression of TREX1 deficiency-induced cellular senescence and interferonopathies by inhibition of DNA damage response
[ iScience, 2023, 26(7):107090]
Cannabidiol Enhances Cabozantinib-Induced Apoptotic Cell Death via Phosphorylation of p53 Regulated by ER Stress in Hepatocellular Carcinoma
[ Cancers (Basel), 2023, 15(15)3987]
ATM Regulates Differentiation of Myofibroblastic Cancer-Associated Fibroblasts and Can Be Targeted to Overcome Immunotherapy Resistance
[ Cancer Res, 2022, 82(24):4571-4585.]
Wwox Binding to the Murine Brca1-BRCT Domain Regulates Timing of Brip1 and CtIP Phospho-Protein Interactions with This Domain at DNA Double-Strand Breaks, and Repair Pathway Choice
[ Int J Mol Sci, 2022, 23(7)3729]
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.
