ROCK/HDAC-IN-1

ROCK/HDAC-IN-1

• UNSPSC Description: ROCK/HDAC-IN-1 (Compound 10h) is an orally active ROCK/HDAC inhibitor. ROCK/HDAC-IN-1 inhibits ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). ROCK/HDAC-IN-1 stimulates the activation of DAMPs, specifically Calreticulin (CRT) exposure and HMGB1 release, indicating that it is a potential ICD inducer.. ROCK/HDAC-IN-1 has antiproliferative activity against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cell), and inhibits tumor growth and activates T cells without apparent toxicity[1].
• Target Antigen: HDAC; ROCK
• Type: Reference compound
• Related Pathways: Cell Cycle/DNA Damage;Cytoskeleton;Epigenetics;Stem Cell/Wnt;TGF-beta/Smad
• Applications: COVID-19-anti-virus
• Field of Research: Cancer; Inflammation/Immunology
• Assay Protocol: https://www.medchemexpress.com/rock-hdac-in-1.html
• Smiles: O=C(NCCCCCCC(NO)=O)C1=CC2=CC(C3=CNN=C3)=CC=C2S1
• Molecular Weight: 386.47
• References & Citations: [1]Mao C, et al. Discovery of the First-in-Class Dual-Target ROCK/HDAC Inhibitor with Potent Antitumor Efficacy in Vivo That Trigger Antitumor Immunity. J Med Chem. 2024 Nov 10.
• Shipping Conditions: Room temperature
• Clinical Information: No Development Reported