ROCK2-IN-13 

ROCK2-IN-13 is a selective ROCK2 inhibitor. ROCK2-IN-13 reduces nuclear expression by disrupting the interaction of ROCK2 with transcriptional co activators p300> and PGC 1α, repressing oncogenic transcription. ROCK2-IN-13 activates FOXO1 driven PTEN expression, leading to suppression of the PI3K/Akt pathway, induction of G₂/M cell cycle arrest, and promotion of apoptosis. ROCK2-IN-13 ablates the nuclear transcriptional function of ROCK2 that sustains oncogenic signaling and restores the tumor suppressive PTEN/FOXO1 axis. ROCK2-IN-13 can be used for prostate cancer reseach^[1].

ROCK2-IN-13 (compound 25) (30 μM, 24 h) exhibits strong antiproliferative activity (84.5% inhibition) in human prostate cancer cells (PC-3), demonstrates potent and consistent efficacy with GI₅₀ values of 3.7 μM in PC-3 cells and 3.9 μM in LNCaP cells, and shows substantially lower cytotoxicity toward normal cells (CC_50s: 55.0 μM for CCD841 and 41.8 μM for HEK-293)^[1].
ROCK2-IN-13 reduces the expression of the highly expressed oncoprotein FOXA2 (HNF-3β) along with the less abundant FOXO1 in PC-3 cells^[1].
ROCK2-IN-13 (1-10 μM) induces a concentration-dependent decrease in FOXA2 mRNA and an increase in FOXO1 mRNA, leading to reduced nuclear FOXA2 protein, enhanced FOXO1 nuclear accumulation, decreased cytoplasmic FOXO1 phosphorylation, and ultimately suppressing the PI3K/Akt axis via PTEN upregulation, which subsequently elevates p27 expression and the Bax/Bcl-2 ratio while reducing cyclin D1 levels, in PC-3 and LNCaP cells^[1].
ROCK2-IN-13 (1-10 μM, 24 h) reduces the proportions of cells in the G1 and S phases and induces a marked accumulation of cells in the G₂/M phase in PC-3 cells^[1].
ROCK2-IN-13 (1-10 μM) induces a concentration-dependent induction of apoptosis with the proportion of early and late apoptotic cells reaching 15.7% and 8.7%, respectively, at 10 μM in PC-3 cells^[1].
ROCK2-IN-13 (1-10 μM, 48 h) suppresses the PI3K/Akt signaling pathway predominantly via PTEN activation, rather than through direct EGFR inhibition in PC-3 cells^[1].
ROCK2-IN-13 (1-10 μM, 48 h) induces a concentration-dependent increase in PGC-1α mRNA, significantly reduces the mRNA expression of both ROCK1 and ROCK2 with a greater effect on ROCK2, decreases nuclear ROCK2 protein while leaving cytoplasmic ROCK1 unchanged, enhances the transcription of FOXO1 by recruiting RNA polymerase II and PGC-1α to its promoter, and facilitates PTEN transcription by promoting the binding of RNA polymerase II and key co-regulators (ROCK1/2, PGC-1α, and p300) to the PTEN promoter in PC-3 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ROCK2-IN-13 (compound 25) (30 and 50 mg/kg, i.p., daily for 26 days) significantly suppresses tumor growth in a prostate cancer xenograft model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

372.37

C₁₈H₁₁F₃N₄S

N#CC1=CC=C(C=C1C(F)(F)F)NC(NC2=CC=C3C=NC=CC3=C2)=S

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• [1]. Lee J, et al. Inhibition of nuclear ROCK2 by a novel thiourea derivative induces potent antitumor effects through PTEN/FOXO1 pathway restoration in prostate cancer. Bioorg Chem. 2025 Dec;167:109211.  [Content Brief]