2. Search Result
Search Result
Results for "

ROCK1 selectivity

" in MedChemExpress (MCE) Product Catalog:

31

Inhibitors & Agonists

1

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15307
    Belumosudil
    30+ Cited Publications

    KD025; SLx-2119

    		 ROCK Inflammation/Immunology Cancer
    Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties .
    Belumosudil
  • HY-15392
    Chroman 1
    Maximum Cited Publications
    63 Publications Verification

    		 ROCK Cardiovascular Disease
    Chroman 1 is a highly potent and selective ROCK inhibitor. Chroman 1 is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 also has inhibitory activity against MRCK, with an IC50 of 150 nM .
    Chroman 1
  • HY-11000
    GSK429286A
    5+ Cited Publications

    		 ROCK Cancer
    GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.
    GSK429286A
  • HY-15307A
    Belumosudil mesylate
    30+ Cited Publications

    KD025 mesylate; SLx-2119 mesylate

    		 ROCK Inflammation/Immunology
    Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties .
    Belumosudil mesylate
  • HY-119937
    ROCK inhibitor-2
    2 Publications Verification

    		 ROCK Cardiovascular Disease Inflammation/Immunology Cancer
    ROCK inhibitor-2 (compound 6) is a selective dual inhibitor of ROCK1 and ROCK2, with IC50 values of 160 nM and 21 nM, respectively. ROCK inhibitor-2 inhibits pMYPT1 with IC50 of 75 nM. ROCK inhibitor-2 exhibits antitumor activity .
    ROCK inhibitor-2
  • HY-162596
    NRL-1049

    BA-1049 free base

    		 ROCK Neurological Disease
    NRL-1049 (BA-1049 (free base)) is an orally available and selective ROCK2 inhibitor with IC50 values of 0.59 µM for ROCK2 and 26 µM for ROCK1, respectively. NRL-1049 modulates ROCK signaling, preserves blood-brain barrier integrity, reduces edema, seizures and hemorrhage, and alleviates cerebral cavernous malformation lesion burden. NRL-1049 can be used for the study of acute brain injury, ischemic stroke, and cerebral cavernous malformations .
    NRL-1049
  • HY-18990
    GSK180736A
    5+ Cited Publications

    		 ROCK G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
    GSK180736A
  • HY-16758
    Verosudil

    AR-12286

    		 ROCK Neurological Disease
    Verosudil (AR-12286) is a ROCK inhibitor. Verosudil has equal inhibitory activity against ROCK1 and ROCK2 (Ki: 2 nM). Verosudil is less selective for PKA, PKCT, MRCKA, and CAM2A (Ki: 69 nM, 9322 nM, 28 nM, 5855 nM, respectively). Verosudil increases trabecular outflow capacity to reduce intraocular pressure. Verosudil is useful in the study of glaucoma and ocular hypertension .
    Verosudil
  • HY-15392A
    Chroman 1 dihydrochloride
    Maximum Cited Publications
    63 Publications Verification

    		 ROCK Cardiovascular Disease
    Chroman 1 dihydrochloride is a highly potent and selective ROCK inhibitor. Chroman 1 dihydrochloride is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 dihydrochloride also has inhibitory activity against MRCK, with an IC50 of 150 nM .
    Chroman 1 dihydrochloride
  • HY-109562A
    CCG258208 hydrochloride
    1 Publications Verification

    GRK2-IN-1 hydrochloride

    		 G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 hydrochloride can be used in heart failure research .
    CCG258208 hydrochloride
  • HY-139690
    CCG258747
    1 Publications Verification

    		 Opioid Receptor G Protein-coupled Receptor Kinase (GRK) Mas-related G-protein-coupled Receptor (MRGPR) Cardiovascular Disease Inflammation/Immunology
    CCG258747 is a selective GRK2 inhibitor (IC50 = 18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, > 5500, and > 550-fold, respectively). CCG258747 also blocks the internalization of the µ-opioid receptor (MOR). CCG258747 attenuates IgE mediated anaphylaxis by inhibiting GRK2 and FcεRI signaling pathway but activates mast cells via MRGPRX2 and MRGPRB2. CCG258747 can be used to study diseases related to overexpression of GRK2 (such as heart failure, opioid tolerance) .
    CCG258747
  • HY-Q22471
    ROCK1-IN-1
    1 Publications Verification

    		 ROCK Cardiovascular Disease
    ROCK1-IN-1 is a potent selective ROCK1 inhibitor with a Ki of 540 nM. ROCK1-IN-1 can be used for the research of hypertension .
    ROCK1-IN-1
  • HY-14362
    GSK-25

    		ROCK Ribosomal S6 Kinase (RSK) Cardiovascular Disease
    GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) .
    GSK-25
  • HY-126432
    NRL-1049 dihydrochloride

    BA-1049

    		 ROCK Neurological Disease
    NRL-1049 dihydrochloride (BA-1049) is a selective and orally active rho-associated protein kinase 2 (ROCK2) inhibitor with an IC50 of 0.59 μM. NRL-1049 dihydrochloride shows selectivity for ROCK2 is 44 times that of ROCK1 (IC50 = 26 μM). NRL-1049 dihydrochloride can preserve the blood-brain barrier after acute injury .
    NRL-1049 dihydrochloride
  • HY-178821
    ROCK2-IN-12

    		ROCK TGF-beta/Smad STAT Inflammation/Immunology
    ROCK2-IN-12 (Compound A25) is a selective ROCK2 inhibitor with an IC50 of 7.0  nM for ROCK2 over ROCK1. ROCK2-IN-12 has potent antifibrotic effects via the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-12 significantly reduces collagen deposition and reverses fibrotic progression in Bleomycin (HY-108345)-induced pulmonary fibrosis (PF) mouse models. ROCK2-IN-12 can be used for lung diseases like pulmonary fibrosis research .
    ROCK2-IN-12
  • HY-110339
    RKI-1447 dihydrochloride
    4 Publications Verification

    		 ROCK Apoptosis Cancer
    RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively . RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis .
    RKI-1447 dihydrochloride
  • HY-109562
    CCG258208

    GRKs-IN-1

    		 G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    CCG258208 (GRK2-IN-1) is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 can be used in heart failure research .
    CCG258208
  • HY-178013
    ROCK2-IN-11

    		ROCK Inflammation/Immunology
    ROCK2-IN-11 (Compound A20) is a selective ROCK2 inhibitor with an IC50 of 0.18 μM for ROCK2 over ROCK1. ROCK2-IN-11 can be used for idiopathic pulmonary fibrosis and cGVHD research .
    ROCK2-IN-11
  • HY-118151
    Rho-Kinase-IN-3

    		ROCK Cardiovascular Disease Neurological Disease
    Rho-Kinase-IN-3 (compound 12) is a potent and selective Rho kinase (ROCK1) inhibitor with an IC50 value of 8 nM. Rho-Kinase-IN-3 can be used in research of hypertension .
    Rho-Kinase-IN-3
  • HY-10833
    ROCK-IN-10

    		ROCK Cardiovascular Disease
    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 .
    ROCK-IN-10
  • HY-122011
    PF-4950834

    		ROCK SGK PKA PKC Inflammation/Immunology
    PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration .
    PF-4950834
  • HY-15307AR
    Belumosudil mesylate (Standard)

    KD025 mesylate (Standard); SLx-2119 mesylate (Standard)

    		 ROCK Reference Standards Inflammation/Immunology Cancer
    Belumosudil (mesylate) (Standard) is the analytical standard of Belumosudil (mesylate). This product is intended for research and analytical applications. Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties .
    Belumosudil mesylate (Standard)
  • HY-15307R
    Belumosudil (Standard)

    KD025 (Standard); SLx-2119 (Standard)

    		 ROCK Reference Standards Inflammation/Immunology Cancer
    Belumosudil (Standard) is the analytical standard of Belumosudil. This product is intended for research and analytical applications. Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties .
    Belumosudil (Standard)
  • HY-175843
    ROCK2-IN-10

    		ROCK STAT Cancer
    ROCK2-IN-10 is a potent and selective ROCK2 inhibitor (IC50 = 0.020 μM) with 41-fold selectivity over isoform ROCK1. ROCK2-IN-10 inhibits metastasis by disrupting the cytoskeleton, independent of proliferative suppression. ROCK2-IN-10 shows superior inhibitory potency against cancer cell metastasis, which closely related to the suppression of STAT3 phosphorylation. ROCK2-IN-10 can be used for breast cancer metastasis research .
    ROCK2-IN-10
  • HY-123254
    CCG-224406

    		G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    CCG-224406 is a selective G protein-coupled receptor kinase 2 (GRK2) inhibitor with the IC50 values of 13 nM, greater than 700-fold selectivity over other GRK subfamilies, and no inhibition of ROCK1. CCG-224406 can be used for study of heart failure .
    CCG-224406
  • HY-15307S
    Belumosudil-d7

    KD025-d7; SLx-2119-d7

    		 Isotope-Labeled Compounds ROCK Inflammation/Immunology Cancer
    Belumosudil-d7 (KD025-d7) is deuterium labeled Belumosudil. Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties .
    Belumosudil-d7
  • HY-16758A
    Verosudil hydrochloride

    AR-12286 hydrochloride

    		 ROCK Neurological Disease
    Verosudil (AR-12286) hydrochloride is the hydrochloride form of Verosudil (HY-16758). Verosudil hydrochloride is a ROCK inhibitor. Verosudil hydrochloride has equal inhibitory activity against ROCK1 and ROCK2 (Ki: 2 nM). Verosudil hydrochloride is less selective for PKA, PKCT, MRCKA, and CAM2A (Ki: 69 nM, 9322 nM, 28 nM, 5855 nM, respectively). Verosudil hydrochloride increases trabecular outflow capacity to reduce intraocular pressure. Verosudil hydrochloride is useful in the study of glaucoma and ocular hypertension .
    Verosudil hydrochloride
  • HY-181583
    LASSBio-2389

    		ROCK Cancer
    LASSBio-2389 is a selective ROCK2 inhibitor with an IC50 of 0.051 μM and an IC50 of 1.143 μM against ROCK1. LASSBio-2389 reduces the viability of MDA-MB-231 cells and inhibits cell migration. LASSBio-2389 is applicable to the research of triple-negative breast cancer .
    LASSBio-2389
  • HY-162596A
    (Rac)-NRL-1049 dihydrochloride

    (Rac)-BA-1049

    		 ROCK Neurological Disease
    (Rac)-NRL-1049 is the racemic mixture of NRL-1049 (BA-1049 (free base)) (HY-162596). NRL-1049 is an orally available and selective ROCK2 inhibitor with IC50 values of 0.59 µM for ROCK2 and 26 µM for ROCK1, respectively. NRL-1049 modulates ROCK signaling, preserves blood-brain barrier integrity, reduces edema, seizures and hemorrhage, and alleviates cerebral cavernous malformation lesion burden. NRL-1049 can be used for the study of acute brain injury, ischemic stroke, and cerebral cavernous malformations .
    (Rac)-NRL-1049 dihydrochloride
  • HY-181576
    ROCK2-IN-14

    		ROCK Inflammation/Immunology
    ROCK2-IN-14 is an orally active, selective ROCK2 inhibitor (IC50=4.8 nM) with 212-fold selectivity over ROCK1 (IC50=1.01 μM). By inhibiting the ROCK2/S100A9 signaling pathway, ROCK2-IN-14 downregulates S100A9 expression, inhibits NM2 phosphorylation and restores cytoskeletal abnormalities. Furthermore, ROCK2-IN-14 reduces inflammatory cytokine levels, alleviates skin inflammation and exerts anti-inflammatory activity. ROCK2-IN-14 also significantly inhibits ear thickening in a mouse model of atopic dermatitis (AD), and decreases the levels of IgE, TNF-α, IL-6 and TSLP. ROCK2-IN-14 can be used for research on atopic dermatitis .
    ROCK2-IN-14
  • HY-184149
    ROCK2-IN-17

    		ROCK TGF-beta/Smad STAT Inflammation/Immunology
    ROCK2-IN-17 is an orally active and selective ROCK2 inhibitor with an IC50 of 8.1 nM. ROCK2-IN-17 achieves its antifibrotic effect by inhibiting the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-17 can be used for pulmonary fibrosis research .
    ROCK2-IN-17

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: