TH-263
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MedKoo CAT#: 555717

CAS#: 313520-94-4

Description: 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

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TH-263
CAS# 313520-94-4
Instruction

Theoretical Analysis

MedKoo Cat#: 555717
Name: TH-263
CAS#: 313520-94-4
Chemical Formula: C21H20N2O3S
Exact Mass: 380.12
Molecular Weight: 380.462
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 2 weeks
100mg USD 750 2 weeks
200mg USD 1250 2 Weeks
500mg USD 2650 2 Weeks
1g USD 3850 2 Weeks
2g USD 6450 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.

Biological target:
In vitro activity:
In vivo activity:

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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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https://www.thesgc.org/chemical-probes/TH-257