MedKoo Cat#: 555717 | Name: TH-263
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

TH-263 is an inactive analog control for the type III allosteric LIM-kinase (LIMK) inhibitors TH-257, TH-255 and TH-251. LIM kinases belong to the family of cytoplasmic tyrosine-like kinases with dual specificity (serine/threonine and tyrosine). However, known LIMK substrate are usually phosphorylated at serine and threonine residues LIM kinases comprises LIM kinase 1 (LIMK1) and LIM kinase 2 (LIMK2) which show 50% sequence identity in human. Both LIMK1 and LIMK2 present with a unique domain organization containing two N-terminal LIM domains, a PDZ domain, a proline/serine-rich domain and a C-terminal kinase domain.

Chemical Structure

TH-263
TH-263
CAS#313520-94-4

Theoretical Analysis

MedKoo Cat#: 555717

Name: TH-263

CAS#: 313520-94-4

Chemical Formula: C21H20N2O3S

Exact Mass: 380.1195

Molecular Weight: 380.46

Elemental Analysis: C, 66.30; H, 5.30; N, 7.36; O, 12.62; S, 8.43

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 weeks
100mg USD 750.00 2 weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,650.00 2 Weeks
1g USD 3,850.00 2 Weeks
2g USD 6,450.00 2 Weeks
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Related CAS #
313520-94-4 1004044-80-7 (wrong structure)
Synonym
TH-263; TH 263; TH263;
IUPAC/Chemical Name
N-benzyl-4-(N-benzylsulfamoyl)benzamide
InChi Key
QDGVJMITKNOVTP-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H20N2O3S/c24-21(22-15-17-7-3-1-4-8-17)19-11-13-20(14-12-19)27(25,26)23-16-18-9-5-2-6-10-18/h1-14,23H,15-16H2,(H,22,24)
SMILES Code
O=C(NCC1=CC=CC=C1)C2=CC=C(S(=O)(NCC3=CC=CC=C3)=O)C=C2
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Note: Sigma's TH-263 (cas3SML2276) has CAS#1004044-80-7, which is a wrong structure. TH-257 is 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. It potently inhibits cofilin phosphorylation with an IC50 of 84 nM for LIMK1 and 39 nM for LIMK2 in a RapidFire MS assay. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay (Dx) at 1 μM (IC50 >> 50 % inhibition). In a life cell NanoBRET assay (Promega) TH257 has an IC50 of 250 nM against ectopically expressed full-length LIMK1 and 150 nM LIMK2, respectively.

Preparing Stock Solutions

The following data is based on the product molecular weight 380.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
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. Epub 2018 Jun 8. PMID: 29908439.