BML-277Chk2 inhibitor,potent and highly selective CAS# 516480-79-8 |
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Quality Control & MSDS
3D structure
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| Cas No. | 516480-79-8 | SDF | Download SDF |
| PubChem ID | 9969021 | Appearance | Powder |
| Formula | C20H14ClN3O2 | M.Wt | 363.8 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Chk2 Inhibitor II; C 3742 | ||
| Solubility | DMSO : 22.22 mg/mL (61.08 mM; Need ultrasonic) | ||
| Chemical Name | 2-[4-(4-chlorophenoxy)phenyl]-3H-benzimidazole-5-carboxamide | ||
| SMILES | C1=CC(=CC=C1C2=NC3=C(N2)C=C(C=C3)C(=O)N)OC4=CC=C(C=C4)Cl | ||
| Standard InChIKey | UXGJAOIJSROTTN-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C20H14ClN3O2/c21-14-4-8-16(9-5-14)26-15-6-1-12(2-7-15)20-23-17-10-3-13(19(22)25)11-18(17)24-20/h1-11H,(H2,22,25)(H,23,24) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM.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]. References: | |||||
BML-277 Dilution Calculator
BML-277 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.7488 mL | 13.7438 mL | 27.4876 mL | 54.9753 mL | 68.7191 mL |
| 5 mM | 0.5498 mL | 2.7488 mL | 5.4975 mL | 10.9951 mL | 13.7438 mL |
| 10 mM | 0.2749 mL | 1.3744 mL | 2.7488 mL | 5.4975 mL | 6.8719 mL |
| 50 mM | 0.055 mL | 0.2749 mL | 0.5498 mL | 1.0995 mL | 1.3744 mL |
| 100 mM | 0.0275 mL | 0.1374 mL | 0.2749 mL | 0.5498 mL | 0.6872 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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BML-277 is novel, potent and highly selective inhibitor of the chk2 with the IC50 value of 15±6.9nM [1].
BML-277 has shown the ATP-competitive inhibition of chk2 with the Ki value of 37nM. BML-277 has also been exhibited to be a chk2 inhibitor with the IC50 value of 15±6.9nM and efficiently rescue T-cell populations from the apoptosis of radiation-induced in a concentration-dependent fashion with the EC50 of 3~7.6μM. The Km of ATP for chk2 is 99μM and assuming that intracellular ATP concentration is 10mM. Apart from these, BML-277 has shown the inhibition through docking into a homology model of chk2 ATP binging site [1].
References:
[1]Arienti KL1, Brunmark A, Axe FU, McClure K, Lee A, Blevitt J, Neff DK, Huang L, Crawford S, Pandit CR, Karlsson L, Breitenbucher JG. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85.
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BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM.
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