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BT2 

Cat. No.: HY-114855
Handling Instructions

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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BT2 Chemical Structure

BT2 Chemical Structure

CAS No. : 34576-94-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 50 In-stock
Estimated Time of Arrival: December 31
50 mg USD 90 In-stock
Estimated Time of Arrival: December 31
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Description

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)[1]. BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM[2].

IC50 & Target[1][2]

BDK

3.19 μM (IC50)

Mcl-1

59 μM (Ki)

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[1].

Animal Model: C57BL/6J male mice (8-10-week-old)[1]
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.
Molecular Weight

247.10

Formula

C₉H₄Cl₂O₂S

CAS No.

34576-94-8

SMILES

O=C(O)C1=C(C2=CC=C(C=C2S1)Cl)Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (337.23 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0469 mL 20.2347 mL 40.4694 mL
5 mM 0.8094 mL 4.0469 mL 8.0939 mL
10 mM 0.4047 mL 2.0235 mL 4.0469 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.42 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.42 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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KeyWords:

BT2 | BT 2 | BT-2 | Bcl-2 Family | Inhibitor | inhibitor | inhibit

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Product name:
BT2
Cat. No.:
HY-114855
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