Catalog No.
Product Name
Application
Product Information
Citations
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PKC activator
Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator and a potent skin tumor promoter. -
PKC-θ inhibitor
PKC-theta inhibitor is a selective PKC-θinhibitor, with an IC50 of 12 nM. -
ROCK2 inhibitor
ROCK2-IN-2 is a selective ROCK2 inhibitor extracted from patent US20180093978A1, Compound A-30, has an IC50 of <1 μM. -
ROCK inhibitor
SB-772077B dihydrochloride is an aminofurazan-based Rho kinase (ROCK) inhibitor with IC50s of 5.6 nM and 6 nM toward ROCK1 and ROCK2, respevtively. -
PKA activator
Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC50 of 6.5 nM and Kd of 8 nM in Trypanosoma brucei. Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity. -
ROCK inhibitor
Rho-Kinase-IN-1 is a Rho kinase (ROCK) inhibitor (Ki values of 30.5 and 3.9 nM for ROCK1 and ROCK2, respectively) extracted from US20090325960A1, compound 1.008. - EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
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TGFβRI kinase inhibitor
TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively. -
ROCK1/ROCK2 inhibitor
ROCK inhibitor-2 is a selective dual ROCK1 and ROCK2 inhibitor with IC50s of 17 nM and 2 nM, respectively. -
PKCθ inhibitor
PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. -
PKC inhibitor
Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. It can be used for the treatment of uveal melanoma.
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BMP activator
SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules. - Alantolactone, an allergenic sesquiterpene lactone, has recently been found to have significant antitumor effects on malignant tumor cells.
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PKA inhibitor
PKA inhibitor fragment (6-22) amide is a synthetic peptide that acts as a protein kinase inhibitor. -
PKC inhibitor
PKC (19-36), pseudosubstrate peptide inhibitor of protein kinase C (IC50 = 0.18 uM). - Protein Kinase C (19-31), this peptide derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, it was used as protein kinase C substrate peptide for testing the protein kinase C activity.
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Akt inhibitor
AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively, little activity outside the AGC kinase family. -
ROCK inhibitor
H-1152 dihydrochloride, an isoquinolinesulfonamide derivative, is a more specific, stronger and membrane-permeable inhibitor of Rho-kinase with a Ki value of 1.6 nM, but poor inhibitor of other serine/threonine kinases. -
ROCK inhibitor
Hydroxyfasudil, metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. -
ROCK inhibitor
Hydroxyfasudil hydrochloride, metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. -
ROCK activator
Narciclasine is a Rho/Rho kinase/LIM kinase/cofilin signaling pathway activator. -
ROCK2 Inhibitor
SLx-2119 is a small molecule and selective inhibitor of ROCK2 with IC50 of 105 nM; > 200 fold selecivity over ROCK1(IC50 =24 uM). -
antiviral agent
Daphnoretin (Dephnoretin), isolated from Wikstroemia indica, possesses antiviral activity. Daphnoretin likes PMA, may direct activation of protein kinase C which in turn activated NADPH oxidase and elicited respiratory burst. -
ROCK/ERK/GSK/AGC Inhibitor
ROCK-IN-5 (compound I-B-37) is a potent inhibitor of Rho-associated protein kinase (ROCK), as well as ERK, GSK-3, and AGC protein kinases. This compound exhibits significant biological activity in regulating cellular proliferation and has applications in researching cardiac conditions and neurodegenerative diseases. Its broad inhibitory profile makes it a valuable tool for studies aimed at understanding signaling pathways involved in various disease mechanisms. -
PKA Inhibitor
HA-1004 hydrochloride is a selective inhibitor of protein kinase A (PKA), known for its ability to inhibit lipolysis and promote vascular relaxation. In addition to its PKA inhibition, HA-1004 also functions as a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein synthesis, impacting smooth muscle and second messenger pathways. This compound serves as a vasodilator, effective in inhibiting the contraction of rabbit aortic strips, and can also antagonize ERK and tyrosine hydroxylase phosphorylation in morphine abstinence models. -
PKA Inhibitor
HA-1004 dihydrochloride is a selective inhibitor of protein kinase A (PKA), demonstrating significant inhibition of lipolysis and induction of vascular relaxation. Additionally, it acts as a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein kinase, playing a crucial role in regulating smooth muscle activity and second messenger pathways. This compound serves as a vasodilator, effectively inhibiting contraction in rabbit aortic strips, and also antagonizes ERK and tyrosine hydroxylase phosphorylation in models of morphine abstinence. -
ROCK2 Inhibitor
NRL-1049 dihydrochloride is a selective inhibitor of rho-associated protein kinase 2 (ROCK2), exhibiting an IC50 value of 0.59 μM. This compound demonstrates a remarkable selectivity for ROCK2 over ROCK1, with an IC50 of 26 μM, effectively inhibiting ROCK2 activity. NRL-1049 dihydrochloride has significant potential in research applications focused on the preservation of the blood-brain barrier following acute injury. -
ROCK Inhibitor
Zelasudil is a selective inhibitor of Rho-associated coiled-coil containing protein kinase 2 (ROCK2), demonstrating significant anti-fibrotic activity. This small molecule enhances immunomodulatory responses in metastatic pancreatic tumors, promoting increased infiltration of CD8+ and CD4+ T cells while reducing FOXP3+ regulatory T cells at the tumor periphery. Zelasudil shows potential for advancing research in pancreatic ductal adenocarcinoma and related therapeutic strategies. -
ROCK/NET Inhibitor
Netarsudil functions as a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). This compound effectively reduces intraocular pressure through ROCK inhibition, promoting relaxation of trabecular meshwork cells and dilation of episcleral veins, facilitating aqueous humor outflow while simultaneously decreasing aqueous humor production via NET inhibition. Netarsudil is primarily utilized in research related to ocular hypertension and primary open-angle glaucoma. -
ROCK2 Inhibitor
Belumosudil mesylate is a selective inhibitor of the Rho-associated kinase 2 (ROCK2), demonstrating an IC50 of 105 nM for ROCK2 and 24 µM for ROCK1. This compound exhibits significant anti-fibrotic properties, making it valuable for research in fibrosis-related pathways and diseases. Belumosudil mesylate is applicable in studies aimed at understanding the role of ROCK signaling in various physiological and pathological processes. -
ROCK Inhibitor
SAR407899 is a selective and potent ROCK inhibitor that acts competitively with ATP, exhibiting an IC50 of 135 nM for ROCK-2 and Kis of 36 nM in human and 41 nM in rat ROCK-2. This compound demonstrates stable inhibition of migrasome formation and is valuable for research into cellular migration and related processes. Its application in studies of ROCK signaling pathways may enhance the understanding of various physiological and pathological conditions. -
ROCK/NET Inhibitor
Netarsudil dimesylate is a potent inhibitor of Rho-associated kinases (ROCK I and ROCK II) and also serves as a reversible inhibitor of the norepinephrine transporter (NET). It effectively reduces intraocular pressure through ROCK inhibition, leading to the relaxation of trabecular meshwork cells and dilation of episcleral veins, which facilitates aqueous humor outflow, while simultaneously inhibiting NET to diminish aqueous humor production. This compound is primarily utilized in research related to ocular hypertension and primary open-angle glaucoma. -
ROCK Inhibitor
Sovesudil is a potent Rho kinase (ROCK) inhibitor that functions through ATP-competitive mechanisms, exhibiting IC50 values of 3.7 nM for ROCK-I and 2.3 nM for ROCK-II. It effectively lowers intraocular pressure (IOP) while minimizing the risk of hyperemia, making it a valuable compound for ocular research and potential therapeutic applications in glaucoma treatment and other related conditions. -
ROCK Inhibitor
Verosudil is a potent Rho-associated protein kinase (ROCK) inhibitor, demonstrating robust inhibitory activity against both ROCK1 and ROCK2 with a Ki value of 2 nM. Its relatively lower selectivity for other kinases such as PKA, PKCT, MRCKA, and CAMK2A provides additional research avenues. Verosudil enhances trabecular outflow capacity, making it a valuable reagent in studies targeting intraocular pressure reduction. This compound is particularly relevant for research focused on glaucoma and ocular hypertension. -
ROCK Inhibitor
3-(4-Pyridyl)indole is a selective Rho-kinase (ROCK) inhibitor, exhibiting an IC50 value of 25 μM. This compound is known to effectively inhibit cellular blebbing and promote the dissolution of actin stress fibers, making it a valuable reagent for studying wound healing mechanisms and cytoskeletal dynamics in various biological research applications.
