BT2

SKU: orb1219700

Description

BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC).BT2 treatment reduces the protein levels of BDK in kidneys and heart[1]. 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; intraperitoneal injection; 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.

Key Properties

• CAS Number: 34576-94-8
• MW: 247.1
• Purity: >98% (HPLC)
• Formula: C₉H₄Cl₂O₂S
• SMILES: OC(=O)c1sc2cc(Cl)ccc2c1Cl
• Target: Bcl-2
• Solubility: DMSO:83.33 mg/mL (337.23 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  BT2 (20 mg/kg/day; intraperitoneal injection; 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. 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 treatment reduces the protein levels of BDK in kidneys and heart. Animal model: C57BL/6J male mice (8-10-week-old). Dosage: 20 mg/kg/day. Administration: Intraperitoneal injection; daily; for 1 week. Result: BCKDC activity was robustly (12.3-fold) enhanced in the heart compared with the vehicle-treated animals. Less activation was obtained in muscle and kidney at 3.6-and 3.8-fold, respectively. The protein levels of BDK in kidneys and heart were reduced to averages of 39 and 24%, respectively.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Bcl-2