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TH-257

CAT: 0804-HY-122630-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-122630-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
2244678-29-1
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
LIM Kinase (LIMK)
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage
Applications
Neuroscience-Neuromodulation
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 Formula
C24H26N2O3S
Molecular Weight
422.54
Precautions
H302, H315, H319, H335
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)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
LIMK1; LIMK2

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