TH 257
- CAS No.
- 2244678-29-1
- Chemical Name:
- TH 257
- Synonyms
- TH 257;TH-257 ，S6836;TH-257, 10 mM in DMSO;N-Benzyl-N-butyl-4-(N-phenylsulfamoyl)benzamide;LIM Kinase (LIMK),LIMKs,Inhibitor,TH-257,inhibit,TH257;Benzamide, N-butyl-4-[(phenylamino)sulfonyl]-N-(phenylmethyl)-
- CBNumber:
- CB95476799
- Molecular Formula:
- C24H26N2O3S
- Molecular Weight:
- 422.54
- MDL Number:
- MOL File:
- 2244678-29-1.mol
| Product description | Number | Pack Size | Price |
| TH-257 98.91% | CS-0087663 | 10mg | $113 |
| TH257 99% | Axon2973 | 50mg | $368.5 |
| TH-257 98.91% | CS-0087663 | 5mg | $73 |
| N-Benzyl-N-butyl-4-(N-phenylsulfamoyl)benzamide 98+% | A1193405 | 5mg | $93 |
| TH257 | CSN24750 | 1mg | $27 |
| storage temp. | 2-8°C |
|---|---|
| solubility |
DMSO:42.25(Max Conc. mg/mL);100.0(Max Conc. mM) Ethanol:42.25(Max Conc. mg/mL);100.0(Max Conc. mM) |
| form | powder |
| color | white to beige |
| InChI | 1S/C24H26N2O3S/c1-2-3-18-26(19-20-10-6-4-7-11-20)24(27)21-14-16-23(17-15-21)30(28,29)25-22-12-8-5-9-13-22/h4-17,25H,2-3,18-19H2,1H3 |
| InChIKey | VNCIWNGCMAKKEO-UHFFFAOYSA-N |
| SMILES | O=C(C1=CC=C(C=C1)S(NC2=CC=CC=C2)(=O)=O)N(CC3=CC=CC=C3)CCCC |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| WGK Germany | WGK 3 | |||||||||
| Storage Class | 11 - Combustible Solids | |||||||||
| NFPA 704 |
|
TH 257 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0087663 | TH-257 98.91% | 2244678-29-1 | 10mg | $113 | 2021-12-16 | Buy |
| Axon Medchem | Axon2973 | TH257 99% | 2244678-29-1 | 50mg | $368.5 | 2021-12-16 | Buy |
| ChemScene | CS-0087663 | TH-257 98.91% | 2244678-29-1 | 5mg | $73 | 2021-12-16 | Buy |
| Ambeed | A1193405 | N-Benzyl-N-butyl-4-(N-phenylsulfamoyl)benzamide 98+% | 2244678-29-1 | 5mg | $93 | 2021-12-16 | Buy |
| CSNpharm | CSN24750 | TH257 | 2244678-29-1 | 1mg | $27 | 2021-12-16 | Buy |
TH 257 Chemical Properties,Uses,Production
Uses
TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM[1].
Biological Activity
TH-257 is a potent, type III allosteric LIM-kinase (LIMK1 & LIMK2) inhibitor (LIMK1/2 IC50 in nM = 48/29 by cell-free kinase assay and 250/150 by live cell NanoBRET assay using respective transfectants) th at targets LIMK1/2 DFG-out conformation in a non-ATP-competitive manner and exhibits no significant off-target activity by KINOMEscan assay at 1 μM. TH-263 is a structure analog and the recommended negative control for TH-257. For characterization details of TH-257, please visit the TH-257 probe summary on the Structural Genomics Consortium (SGC) website.
TH-263 is the negative control for the active probe, TH-257. TH-263 is available from Sigma. To learn more about and purchase TH-263, click here.
To learn about other SGC chemical probes, visit sigma.com/sgc
IC 50
LIMK1: 84 nM (IC50); LIMK2: 39 nM (IC50)
storage
Store at +4°C
References
[1] Manetti F. Recent advances in the rational design and development of LIM kinase inhibitors are not enough to enter clinical trials. Eur J Med Chem. 2018 Jul 15;155:445-458. DOI:10.1016/j.ejmech.2018.06.016
[2] Collins R, et, al. Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. J Med Chem. 2022 Oct 27;65(20):13705-13713. DOI:10.1021/acs.jmedchem.2c00751
TH 257 Preparation Products And Raw materials
Raw materials
Preparation Products
TH 257 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32470 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| HANGZHOU LEAP CHEM CO., LTD. | +86-571-87711850 | market18@leapchem.com | China | 24597 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39042 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 | |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 18149758185; | sales-cpd@caerulumpharma.com | China | 3505 | 58 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4795 | 55 | |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9803 | 58 |
