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BT2, a BCKDC kinase (BDK) inhibitor, exhibits an IC50 of 3.19 μM and functions as a potent, selective Mcl-1 inhibitor with a Ki value of 59 μM. Its interaction with BDK induces helix movements in the N-terminal domain, leading to BDK's dissociation from the branched-chain α-ketoacid dehydrogenase complex (BCKDC).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $39 | In Stock | |
25 mg | $58 | In Stock | |
50 mg | $72 | In Stock | |
100 mg | $105 | In Stock | |
500 mg | $256 | In Stock | |
1 mL x 10 mM (in DMSO) | $38 | In Stock |
Description | BT2, a BCKDC kinase (BDK) inhibitor, exhibits an IC50 of 3.19 μM and functions as a potent, selective Mcl-1 inhibitor with a Ki value of 59 μM. Its interaction with BDK induces helix movements in the N-terminal domain, leading to BDK's dissociation from the branched-chain α-ketoacid dehydrogenase complex (BCKDC). |
Targets&IC50 | BDK:3.19 μM (IC50), MCL1:59 μM (Ki) |
In vivo | BT2 treatment reduces the protein levels of BDK in kidneys and heart. The -fold activation of BCKDC activity in the above tissues correlates with decreased phosphorylation in heart, muscle, and kidney after the long term BT2 treatment. BT2 (20 mg/kg/day; i.p.; daily; for 7 days; C57BL/6J male mice) treatment robustly enhances BCKDC activity in the heart (12.3-fold) compared with the vehicle-treated animals. Less activation is obtained in muscle and kidney at 3.6- and 3.8-fold, respectively [1]. |
Molecular Weight | 247.1 |
Formula | C9H4Cl2O2S |
Cas No. | 34576-94-8 |
Smiles | OC(=O)c1sc2cc(Cl)ccc2c1Cl |
Relative Density. | 1.653 g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 83.33 mg/mL (337.23 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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