H-1152

SKU: orb1685480

Description

H-1152 is a potent and cell-permeable ROCK inhibitor with a Ki of 1.6 nM. It promotes neurite outgrowth in cultured neurons and blocks LPA-induced MARCKS phosphorylation at Ser159. This compound is widely used in neuroscience research to investigate Rho/ROCK signaling pathways in neuronal development, axon guidance, and regeneration models both in vitro and in vivo.

Research Area

Cell Biology, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 451462-58-1
• MW: 319.42
• Purity: 98.01% (May vary between batches)
• Formula: C₁₆H₂₁N₃O₂S
• SMILES: S(=O)(=O)(C=1C2=C(C=CC1)C=NC=C2C)N3[C@@H](C)CNCCC3
• Target: ROCK
• Solubility: DMSO:80 mg/mL (250.45 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (10.33 mM)

Bioactivity

• Target IC50:
  PKC:5.68 μM|GSK3α:60.7 μM|MLCK:28.3 μM|AMPK:100 μM|Src:3.06 μM|ROCK2:12 nM|MKK4:16.9 μM|Abl:7.77 μM|PKA:3.03 μM|EGFR:50 μM|Aurora A:0.745 μM|PKG:0.36 μM|CaMK II:0.18 μM|P38α:100 μM
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• In Vitro:
  H-1152 potently inhibits Rho kinase (Ki = 1.6 nM) while exhibiting only mild inhibitory effects on PKA, PKC, and MLCK with Ki values of 0.63 μM, 9.27 μM, and 10.1 μM, respectively. In LPA-treated cells, H-1152 (0.1-10 μM) significantly suppresses MARCKS protein phosphorylation with an IC₅₀ of 2.5 μM, whereas no such pronounced effect was observed in PDBu-treated cells . H-1152 (0.5-10 μM) does not reduce neuronal viability. Neither does H-1152 (1, 5, or 10 μM) alter the proportion of different neuronal morphologies. Furthermore, in both BMP4 and LIF culture systems, H-1152 (10 μM) enhances neurite outgrowth length .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, H 1152, H1152, H-1152, ROK, ROCK, Rho-associated kinase, Rho-associated protein kinase, Rho-kinase

Compound Identifiers

PubChem CID

448043