TH-257

• UNSPSC Description:

  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].

• Target Antigen:

  LIM Kinase (LIMK)

• Type:

  Reference compound

• Related Pathways:

  Cell Cycle/DNA Damage

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/th-257.html

• Purity:

  98.36

• Solubility:

  DMSO : 250 mg/mL (ultrasonic)

• Smiles:

  O=C(N(CCCC)CC1=CC=CC=C1)C2=CC=C(S(=O)(NC3=CC=CC=C3)=O)C=C2

• Molecular Weight:

  422.54

• References & Citations:

  [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.|[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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  No Development Reported

• CAS Number:

  2244678-29-1