ChemicalBook > CAS DataBase List > TH 257

TH 257

Product Name: 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
Formula Weight: 422.54
MOL File: 2244678-29-1.mol

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TH 257 Property

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

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Safety

WGK Germany: WGK 3
Storage Class: 11 - Combustible Solids

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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

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0087663
Product name: TH-257
Purity: 98.91%
Packaging: 10mg
Price: $113
Updated: 2021/12/16

Axon Medchem

Product number: Axon2973
Product name: TH257
Purity: 99%
Packaging: 50mg
Price: $368.5
Updated: 2021/12/16

ChemScene

Product number: CS-0087663
Product name: TH-257
Purity: 98.91%
Packaging: 5mg
Price: $73
Updated: 2021/12/16

Ambeed

Product number: A1193405
Product name: N-Benzyl-N-butyl-4-(N-phenylsulfamoyl)benzamide
Purity: 98+%
Packaging: 5mg
Price: $93
Updated: 2021/12/16

CSNpharm

Product number: CSN24750
Product name: TH257
Packaging: 1mg
Price: $27
Updated: 2021/12/16

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TH 257 Chemical Properties,Usage,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

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2244678-29-1, TH 257Related Search:

TH 257

Benzamide, N-butyl-4-[(phenylamino)sulfonyl]-N-(phenylmethyl)-

LIM Kinase (LIMK),LIMKs,Inhibitor,TH-257,inhibit,TH257

N-Benzyl-N-butyl-4-(N-phenylsulfamoyl)benzamide

TH-257, 10 mM in DMSO

TH-257 ，S6836

2244678-29-1