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ZAK-IN-1 is an orally active and selective inhibitor of the leucine zipper and sterile-alpha motif kinase ZAK, with an IC50 of 4 nM and a KD of 8 nM. It demonstrates exceptional selectivity against 403 types of wild-type kinases. ZAK-IN-1 effectively blocks the p38/GATA-4 and JNK/c-Jun signaling pathways, significantly suppressing cardiac hypertrophy. This compound is applicable in the study of hypertrophic cardiomyopathy (HCM).


| Description | ZAK-IN-1 is an orally active and selective inhibitor of the leucine zipper and sterile-alpha motif kinase ZAK, with an IC50 of 4 nM and a KD of 8 nM. It demonstrates exceptional selectivity against 403 types of wild-type kinases. ZAK-IN-1 effectively blocks the p38/GATA-4 and JNK/c-Jun signaling pathways, significantly suppressing cardiac hypertrophy. This compound is applicable in the study of hypertrophic cardiomyopathy (HCM). |
| In vitro | ZAK-IN-1 (Compound 6p) (0-10 μg/mL, 24 h) effectively inhibits cardiomyocyte hypertrophy induced by ZAKα overexpression in H9c2 cells by blocking the p38/GATA-4 and JNK/c-Jun signaling pathways. |
| In vivo | ZAK-IN-1 (Compound 6p) demonstrated significant anti-cardiac hypertrophy effects in a spontaneous hypertensive rat model when administered orally at doses of 0-10 mg/kg once daily for 8 weeks. |
| Molecular Weight | 559.55 |
| Formula | C27H19F2N7O3S |
| Cas No. | 2362525-64-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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