Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: BT-2
  • Price: ￥650.0/100mg ￥1100.0/250mg ￥2200.0/1g
  • Purity: 98.0%
  • Stocking Period: 1 Day
  • Contact: Tony Cao
Related CAS#:
34576-94-8 34576-95-9
329219-49-0 34576-85-7
374099-98-6 21211-18-7
585560-39-0 585550-85-2
585560-50-5 587838-69-5

34576-94-8

34576-94-8 structure
34576-94-8 structure
  • Name: 3,6-Dichloro-1-benzothiophene-2-carboxylic acid
  • Chemical Name: 3,6-Dichloro-1-benzothiophene-2-carboxylic acid
  • CAS Number: 34576-94-8
  • Molecular Formula: C9H4Cl2O2S
  • Molecular Weight: 247.098
  • Create Date: 2018-12-26 21:04:42
  • Modify Date: 2024-01-12 11:03:19
  • 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].
Name 3,6-Dichloro-1-benzothiophene-2-carboxylic acid
Synonyms 3,6-Dichloro-benzo[b]thiophene-2-carboxylic acid
2-Chlorcarbonyl-3,6-dichlorbenzo<b>thiophen
3,6-Dichlorbenzo<b>thiophen-2-carbonsaeure
3,6-Dichloro-1-benzothiophene-2-carboxylic acid
Benzo[b]thiophene-2-carboxylic acid, 3,6-dichloro-
3,6-Dichlor-benzo-<b>-thiophen-2-carbonsaeurechlorid
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].
Target

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.
References

[1]. Tso SC, et al. Benzothiophene carboxylate derivatives as novel allosteric inhibitors of branched-chain α-ketoacid dehydrogenase kinase. J Biol Chem. 2014 Jul 25;289(30):20583-93.

[2]. Friberg A, et al. Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design. J Med Chem. 2013 Jan 10;56(1):15-30.
Density 1.7±0.1 g/cm3
Boiling Point 426.4±40.0 °C at 760 mmHg
Molecular Formula C9H4Cl2O2S
Molecular Weight 247.098
Flash Point 211.7±27.3 °C
Exact Mass 245.930908
PSA 65.54000
LogP 4.65
Vapour Pressure 0.0±1.1 mmHg at 25°C
Index of Refraction 1.723
Storage condition 2-8℃
HS Code 2934999090
HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Chemsrc provides CAS#:34576-94-8 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 34576-94-8 | Chemsrc address: https://m.chemsrc.com/en/baike/3183.html

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2024 ChemSrc All Rights Reserved