[CAS NO. 2244678-29-1] TH-257
PRODUCTS SPECIFICATIONS [2244678-29-1]
DESCRIPTION [2244678-29-1]
Overview
| MDL | MFCD31697753 |
|---|---|
| Molecular Weight | 422.54 |
| Molecular Formula | C24H26N2O3S |
| SMILES | O=C(N(CCCC)CC1=CC=CC=C1)C2=CC=C(S(=O)(NC3=CC=CC=C3)=O)C=C2 |
Summary
TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC 50 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] .
IC50 & Target
|
LIMK1 84 nM (IC 50 ) |
LIMK2 39 nM (IC 50 ) |
In Vitro
TH-257 exhibits good biochemical and cellular potencies. But its extremely rapid in vitro clearance renders it unsuitable as a potential in vivo tool [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 591.66 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3666 mL | 11.8332 mL | 23.6664 mL |
| 5 mM | 0.4733 mL | 2.3666 mL | 4.7333 mL |
| 10 mM | 0.2367 mL | 1.1833 mL | 2.3666 mL |
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.
- [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.