3,6-DICHLORO-BENZO[B]THIOPHENE-2-CARBOXYLIC ACID
- Product Name
- 3,6-DICHLORO-BENZO[B]THIOPHENE-2-CARBOXYLIC ACID
- CAS No.
- 34576-94-8
- Chemical Name
- 3,6-DICHLORO-BENZO[B]THIOPHENE-2-CARBOXYLIC ACID
- Synonyms
- BT2;BT2 ，E2663;BT2, 10 mM in DMSO;3,6-DICHLORO-BENZO[B]THIOPHENE-2-CARBOXY;Bcl-2 Family,BT2,Inhibitor,BT-2,inhibit,BT 2;3,6-dichlorobenzothiophene-2-carboxylic acid;3,6-dichloro-2-benzothiophenecarboxylic acid;3,6-Dichloro-1-benzothiophene-2-carboxylicaci;3,6-Dichlorobenzo[β]thiophene-2-carboxylic acid;Benzo[b]thiophene-2-carboxylic acid, 3,6-dichloro-
- CBNumber
- CB01492789
- Molecular Formula
- C9H4Cl2O2S
- Formula Weight
- 247.1
- MOL File
- 34576-94-8.mol
3,6-DICHLORO-BENZO[B]THIOPHENE-2-CARBOXYLIC ACID Property
- Boiling point:
- 426.4±40.0 °C(Predicted)
- Density
- 1.653±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- Soluble in DMSO (up to at least 20 mg/ml)
- pka
- 2.09±0.30(Predicted)
- form
- solid
- color
- Off-white
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 22948
- Product name
- 3,6-dichloro-benzo[b]thiophene-2-Carboxylic Acid
- Purity
- ≥95%
- Packaging
- 100mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 22948
- Product name
- 3,6-dichloro-benzo[b]thiophene-2-Carboxylic Acid
- Purity
- ≥95%
- Packaging
- 250mg
- Price
- $63
- Updated
- 2024/03/01
- Product number
- 22948
- Product name
- 3,6-dichloro-benzo[b]thiophene-2-Carboxylic Acid
- Purity
- ≥95%
- Packaging
- 500mg
- Price
- $109
- Updated
- 2024/03/01
- Product number
- COR0002384
- Product name
- 3,6-DICHLOROBENZO[B]THIOPHENE-2-CARBOXYLIC ACID
- Purity
- 95.00%
- Packaging
- 1G
- Price
- $721.57
- Updated
- 2021/12/16
- Product number
- FD57151
- Product name
- 3,6-Dichlorobenzo[b]thiophene-2-carboxylic acid
- Packaging
- 2g
- Price
- $450
- Updated
- 2021/12/16
3,6-DICHLORO-BENZO[B]THIOPHENE-2-CARBOXYLIC ACID Chemical Properties,Usage,Production
Description
3,6-dichloro-benzo[b]thiophene-2-Carboxylic acid is an inhibitor of myeloid cell leukemia 1 (Mcl-1) with a Ki value of 59 μM for binding of FITC-Mcl-1-BH2 peptide binding to Mcl-1. It has been used as a building block in the synthesis of inhibitors of Mcl-1, the toll-like receptor 3/double-stranded RNA (TLR3/dsRNA) complex, and D-amino acid oxidase (DAO).
Uses
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].
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. |
IC 50
BDK: 3.19 μM (IC50); Mcl-1: 59 μM (Ki)
References
[1] SHIH-CHIA TSO. Benzothiophene carboxylate derivatives as novel allosteric inhibitors of branched-chain α-ketoacid dehydrogenase kinase.[J]. The Journal of Biological Chemistry, 2014, 289 30: 20583-20593. DOI:10.1074/jbc.m114.569251
[2] ANDERS FRIBERG. Discovery of Potent Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods and Structure-Based Design[J]. Journal of Medicinal Chemistry, 2012, 56 1: 15-30. DOI:10.1021/jm301448p
3,6-DICHLORO-BENZO[B]THIOPHENE-2-CARBOXYLIC ACID Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from 3,6-DICHLORO-BENZO[B]THIOPHENE-2-CARBOXYLIC ACID manufacturers
- Product
- 3,6-DICHLORO-BENZO[B]THIOPHENE-2-CARBOXYLIC ACID 34576-94-8
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 96%
- Supply Ability
- 500kg
- Release date
- 2018-08-20