ROCK Inhibitor

Fasudil (HA-1077; AT877) mesylate is a nonspecific and orally active RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i of 0.33 μM for ROCK1, IC₅₀s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil mesylate is also a potent Ca²⁺ channel antagonist and vasodilator.

GSK317354A is a ROCK and GRK inhibitor. GSK317354A can be used for heart failure and Parkinson’s disease research.

HA-100 hydrochloride is a potent protein kinase inhibitor, with IC₅₀s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 hydrochloride also used as a ROCK inhibitor.

Rock2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Rock2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

ROCK-IN-5 (compound I-B-37) is a potent inhibitor of ROCK, ERK, GSK, and AGC protein kinases. ROCK-IN-5 has the potential for proliferative, cardiac and neurodegenerative diseases research.

Rhodblock 1a is an inhibitor of the Rho kinase signaling pathway. It inhibits the normal formation of the cleavage furrow during cell division by interfering with the localization and function of Rho pathway proteins, causing some cells to fail to form a cleavage furrow or the formed cleavage furrow to break, resulting in binucleated cells. Rhodblock 1a can be used to study the mechanism of cell division and is expected to be used in the research of diseases such as cardiovascular diseases and cancer.

BIPM is a potent ROCK2 inhibitor. BIPM leads to significant changes in neurite length, cell migration and actin stress fibers. BIPM plays an important role in anti-cancer metastasis.

Khasianine (Standard) is the analytical standard of Khasianine (HY-N2322). This product is intended for research and analytical applications. Khasianine is a steroidal glycoalkaloid. Khasianine alleviates psoriasis-like skin inflammation by inhibiting the TNF-α/NF-κB axis. Khasianine can downregulate the RhoA pathway and exhibits potential antimetastatic activity. Khasianine upregulates the expression of TNFR I and TNFR II without inducing apoptotic effects. Khasianine can be used in studies related to psoriasis, pancreatic ductal adenocarcinoma, and liver cancer.

Fimosudil (ROCK2-IN-6) (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research.

Y-33075 hydrochloride (Y-39983) is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC₅₀ of 3.6 nM.

ROCK-IN-32 is a ROCK inhibitor, with an IC₅₀ value of 11 nM for ROCK2. ROCK-IN-32 can be used in research of cardiovascular disease, cancer and inflammation.

ROCK-IN-7 (compound 9) is a ROCK kinase inhibitor. ROCK-IN-7 can be used for research in ocular diseases (such as glaucoma and retinal diseases).

4-(Indolin-1-yl) pyrimidin-2-amine (13a, non-salt form) is a ROCK inhibitor.

ROCK-IN-8 (Example 4) is a ROCK inhibitor, with an IC₅₀ value less than 100 nM. ROCK-IN-8 has anti-inflammatory activity. ROCK-IN-8 can be used for research of respiratory and gastro-intestinal diseases.

Chloroxoquinoline is an anticancer agent. Chloroxoquinoline damages the DNA templates of cancer cells, inducing DNA breaks and cell death, and inhibits cell invasion via down-regulating Rho/Rho kinase signaling pathway. Chloroxoquinoline enhances the radiation sensitivity of Lewis lung cancer cells and xenograft tumors in tumor-bearing mouse models but decreases efficacy after long term exposure in rat models by auto-induction effects on CYP1A and CYP3A. Chloroxoquinoline has a broad-spectrum anticancer activity, such as non-small-cell lung carcinoma (NSCLC), breast cancer and gastric cancer.

ROCK-IN-9 (Compound T345) is a ROCK inhibitor. ROCK-IN-9 shows cytotoxicity in HepG2 cell, with an IC₅₀ of 40.8 μM. ROCK-IN-9 has good pharmacokinetic properties in mice, and shows high in vivo exposure and oral bioavailability at lower doses.

Rock1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Rock1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

ROCK-IN-10 (compound 50) is a potent ROCK inhibitor with IC₅₀ values of 6 nM and 4 nM for ROCK1 and ROCK2, respectively. ROCK-IN-10 shows >100-fold selectivity against other kinases.

Fluanisone (Standard) is the analytical standard of Fluanisone. This product is intended for research and analytical applications. Fluanisone has potent sedative effect in vivo. Fluanisone can be used to study schizophrenia.

ROCK-IN-D1 serves as a highly effective and selective inhibitor of ROCK.