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Chemical Structure| 34576-94-8 Chemical Structure| 34576-94-8

Structure of BT2
CAS No.: 34576-94-8

Chemical Structure| 34576-94-8

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BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 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 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM.

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Product Details of BT2

CAS No. :34576-94-8
Formula : C9H4Cl2O2S
M.W : 247.10
SMILES Code : O=C(C1=C(Cl)C2=CC=C(Cl)C=C2S1)O
MDL No. :MFCD00781745
InChI Key :AAHPIJMQJAZYTM-UHFFFAOYSA-N
Pubchem ID :739884

Safety of BT2

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P233-P260-P261-P264-P271-P280-P302+P352-P304-P304+P340-P305+P351+P338-P312-P321-P332+P313-P337+P313-P340-P362-P403-P403+P233-P405-P501

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2 cells 200 μM 6 h BT2 promoted FOXO1 protein ubiquitination and degradation Cell Death Dis. 2024 Oct 10;15(10):736
bovine aortic endothelial cells (BAECs) 1 μM 24 h BT2 inhibited VEGF-A165-induced migration Sci Adv. 2020 Jul 29;6(31):eaaz7815
Primary cortical neurons 80 μM To investigate the effect of BCAA on neuronal ferroptosis. Cell Death Dis. 2023 Sep 26;14(9):634
human microvascular endothelial cells (HMEC-1) 30 μM 4 h BT2 blocked serum-inducible expression of FosB/ΔFosB and c-Fos Sci Adv. 2020 Jul 29;6(31):eaaz7815
Primary mouse hepatocytes 200 μM 8 h BT2 inhibited cAMP-stimulated hepatic glucose production and gluconeogenic gene expressions Cell Death Dis. 2024 Oct 10;15(10):736

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Brown Norway pigmented rats Choroidal laser injury model Intravitreal injection 192 μg Two injections (days 0 and 7) BT2 reduced retinal vascular leakage by ~50%, an effect similar to aflibercept/Eylea Sci Adv. 2020 Jul 29;6(31):eaaz7815
Mice High-fat diet-induced obese mouse model Oral 30 or 100 mpk Once daily for 8 weeks To evaluate the effects of BT2 on metabolism and liver steatosis in high-fat diet-induced obese mice. Results showed that BT2 treatment significantly improved insulin sensitivity and reduced liver steatosis and inflammation. Mol Metab. 2022 Dec;66:101611
C57BL/6 mice Cerebral ischemia-reperfusion injury model Intraperitoneal injection 40 mg/kg Once daily for 24 hours To investigate the effect of BT2 on cerebral ischemia-reperfusion injury. Results showed that BT2 significantly reduced neuronal ferroptosis and improved neurological functional recovery. Cell Death Dis. 2023 Sep 26;14(9):634

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.05mL

0.81mL

0.40mL

20.23mL

4.05mL

2.02mL

40.47mL

8.09mL

4.05mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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