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.
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- 화학식: C18H11F3N4S
- 분자량:372.37
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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ROCKII |
FOXO1 |
PI3K |
Akt |
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 (CC50s: 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.
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Cell Line:PC-3 cells
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Concentration:30 μM
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Incubation Time:24 h
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Result:Exhibited the strongt antiproliferative activity achieving inhibition rates exceeding 80%.
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Cell Line:PC-3 cells
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Concentration:1, 3, and 10 μM
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Incubation Time:24 h
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Result:Reduced the proportions of cells in the G1 and S phases and induced a marked accumulation of cells in the G2/M phase.
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Cell Line:PC-3 cells
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Concentration:1, 3, and 10 μM
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Incubation Time:48 h
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Result:Exhibited greater cytotoxicity than Gefitinib (HY-50895) (a selective EGFR inhibitor) and their combined treatment synergistically reduced PC-3 cell viability.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:PC-3 cells (1 × 106, s.c.) induce- BALB/c nude mice (Seven-week-old)[1]
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Dosage:30 and 50 mg/kg
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Administration:i.p., daily for 26 days
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Result:Significantly and dose-dependently reduced tumor growth in the xenograft model.
Had anti-tumor effect after 26 days of daily administration at 3 mg/kg.
Produced a significantly lower tumor weight than docetaxel.
Chemical Information
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분자량 372.37
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화학식 C18H11F3N4S
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SMILES
N#CC1=CC=C(C=C1C(F)(F)F)NC(NC2=CC=C3C=NC=CC3=C2)=S
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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