Y-33075 dihydrochloride

SKU: orb1308924

Description

Y-33075 dihydrochloride is a potent and selective ROCK inhibitor with an IC50 of 3.6 nM. This compound is a valuable research tool for investigating Rho-kinase signaling in cellular studies and has been utilized in preclinical models to explore cardiovascular and neurological pathways.

Research Area

Cell Biology, Epigenetics & Chromatin, Neuroscience, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 173897-44-4
• MW: 353.25
• Purity: 99.89% (May vary between batches)
• Formula: C₁₆H₁₈Cl₂N₄O
• SMILES: Cl.Cl.C[C@@H](N)c1ccc(cc1)C(=O)Nc1ccnc2[nH]ccc12
• Target: ROCK,CaMK,PKC
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (11.32 mM);H2O:50 mg/mL (141.54 mM);DMSO:100 mg/mL (283.09 mM)

Bioactivity

• Target IC50:
  CaMK II:810 nM|PKC:420 nM|ROCK:3.6 nM
• In Vivo:
  Y-33075 (≥0.01%) significantly lowers intraocular pressure (IOP) at 2 hours after topical administration in rabbits. Y-33075 (0.05%)-treated eyes show significant reduction of IOP between 2 and 7 hours after topical administration in monkeys. Y-33075 (100 μM) increases the regenerating axons of retinal ganglion cells (RGCs) in the eyes of the rats.
• In Vitro:
  Y-33075 (Y-39983) is a potent inhibitor of ROCK with an IC50 of 3.6 nM and exhibits greater inhibitory effects on PKC and CaMKII compared to Y-27632. The IC50 values for PKC are 9.0 μM for Y-27632 and 0.42 μM for Y-33075, while for CaMKII, the IC50s are 26 μM and 0.81 μM, respectively. The IC50s for Y-27632 and Y-33075 for PKC are 82 and 117 times higher than for ROCK, respectively, and for CaMKII, they are 236 and 225 times higher than for ROCK, respectively . Y-33075 (Y-39983, 10 μM) promotes neurite extension in retinal ganglion cells (RGCs) compared to untreated cells , and at 1 μM, it inhibits the histamine-evoked contraction of rabbit ciliary artery segments in Ca2+-free solutions .

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CaMKII, inhibit, Inhibitor, Y 33075, Y 33075 Dihydrochloride, Y 33075 dihydrochloride, Rho-associated protein kinase, Rho-associated kinase, Rho-kinase, ROK, ROCK, PKC, Y33075 dihydrochloride, Y33075 Dihydrochloride, Y-33075, Y-33075 Dihydrochloride, Y33075

Compound Identifiers

PubChem CID

20601328