TH-257 is a potent and selective allosteric LIMK 1/2 inhibitor with IC50 values of 84 nM and 39 nM, respectively.
| Molecular Weight | 422.54 |
| Formula | C24H26N2O3S |
| CAS Number | 2244678-29-1 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related LIM Kinase Products |
|---|
| 8beta,9alpha-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide
8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide (compound 3), a sesquiterpene, has anti-LIMK1 activity. 8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide has inhibitory property on cell motility. |
| LIMK-IN-1
LIMK-IN-1 is an inhibitor of LIM-Kinase (LIMK), with IC50s of 0.5 nM and 0.9 nM for LIMK1 and LIMK2, respectively. |
| Curcolonol
Curcolonol is a furan type sesquiterpene. Curcolonol can be isolated from several medical herbs. Curcolonol has inhibitory activity for LIM kinase 1. Curcolonol can be used for the research of breast cancer. |
| CRT 0105446
CRT 0105446 (compound 22d) is a LIMK1 inhibitor, with an IC50 of 8 nM. |
| CRT0105950
CRT0105950 is a potent LIMK inhibitor, with IC50s of 0.3 nM and 1 nM for LIMK1 and LIMK2 respectively. CRT0105950 can be used for the research of cancer. |
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