RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC50 of 4 nM.
3,7-DMF is an orally active inhibitor of TGF-β1-induced activation of HSCs. 3,7-DMF induces antioxidant genes and quenches ROS away, which can be used to study liver fibrosis[1].
Protein Kinase C (beta) Peptide is a peptide fragment of Protein Kinase Cβ. Protein Kinase Cβ is related with hyperglycemia decreases endothelium-derived nitric oxide. Inhibition of Protein kinase Cβ prevents the reduction in endothelium-dependent vasodilation induced by acute hyperglycemia[1].
LDN193189 is a BMP signaling inhibitor, inhibiting ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8, 0.8, 5.3, 16.7 nM, respectively.
Hydrochlorothiazide-13C6 is the 13C labeled Hydrochlorothiazide[1]. Hydrochlorothiazide (HCTZ), an orally active diuretic drug of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect[2][3][4].
Hypocrellin A, a naturally occurring PKC inhibitor, has many biological and pharmacological properties, such as antitumour, antiviral, antibacterial, and antileishmanial activities. Hypocrellin A is a promising photosensitizer for anticancer photodynamic therapy (PDT)[1][2][3][4].
Protein Kinase C (gamma) Peptide is a peptide fragment of Protein Kinase Cγ. Protein Kinase Cγ is a protein causative for dominant ataxia, that can negatively regulate nuclear import of recessive-ataxia-related aprataxin[1].
Exoenzyme C3, clostridium botulinum is a promising agent to inactivate RhoA in neurons due to preventing the detrimental effect of active Rho in the recovery of injured neuronal systems. Exoenzyme C3, clostridium botulinum is used for the study of post-traumatic neuro-regeneration[1].
SB-505124 hydrochloride is a selective inhibitor of TGFβR with IC50 of 129 nM and 47 nM for ALK4, ALK5, respectively, and it does not inhibits ALK1, 2, 3, or 6 but ALK7.
Cotosudil is a ROCK kinase inhibitor, which can be used for glaucoma or ocular hypertension research[1].
ROCK2-IN-6 hydrochloride (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research[1].
Ac-MBP (4-14) Peptide is an acetylated MBP (4-14) peptide. MBP (4-14) Peptide is a very selective (protein kinase C) PKC substrate. Ac-MBP (4-14) Peptide can be used for PKC assay in extracts without prior purification to eliminate interfering protein kinases or phosphatases[1].
CCT 365623 (CCT365623) hydrochloride is a potent, orally active small molecule inhibitor of lysyl oxidase (LOX) with IC50 of 0.89 uM; inhibits LOX actvity in living cell system (MDCK cysts) at 5 uM, reduces EGFR retention at the cell surface, suppresses EGFR and AKT phosphorylation driven by EGF, also activates SMAD2 and downregulates MATN2; delays the growth of primary and metastatic tumour cells in vivo.
Daphnoretin (Dephnoretin), isolated from Wikstroemia indica, possesses antiviral activity[1]. Daphnoretin likes PMA, may direct activation of protein kinase C which in turn activated NADPH oxidase and elicited respiratory burst[2].
Fasudil Hydrochloride is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Kis of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.
Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β
Sovesudil, formally known as PHP-201, is a well-tolerated and low toxicity Rho-associated protein kinase (ROCK) inhibitor. Sovesudil can be used for the research of normal-tension glaucoma (NTG)[1].
Protein Kinase C (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC50 of 0.18 μM. Protein Kinase C (19-36) markedly attenuated vascular hyperproliferation and hypertrophy as well as glucose-induced suppression of natriuretic peptide receptor response[1].
Psychosine-d7 is deuterium labeled Psychosine. Psychosine, a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell
Y-27632 is an ATP-competitive inhibitor of ROCK-I and ROCK-II, with Ki of 220 nM and 300 nM for ROCK-I and ROCK-II, respectively.
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[1][2].
Disitertide is an inhibitor of TGF-β1. Sequence: Thr-Ser-Leu-Asp-Ala-Ser-Ile-Ile-Trp-Ala-Met-Met-Gln-Asn.
Bisindolylmaleimide III is a potent and selective inhibitor of protein kinase C (PKC). Bisindolylmaleimide III selectively interacts with either PKCα or ribosomal S6 protein kinase 1 after activation of these kinases[1].
Bisindolylmaleimide II is a general inhibitor of all PKC subtypes[1].
GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.
Midostaurin (CGP41231; PKC412) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50 ranging from 16-500 nM.
FIM-1 is a fluorescent PKC (protein kinase C) probe that can be used for mitochondrial staining. FIM-1 inhibits PKC and acts as ATP-competitive catalytic site inhibitor[1].
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[1].
Sphingosine (d14:1) (Tetradecasphing-4-enine), a sphingolipid, is a potent Protein kinase C (PKC) inhibitor. Sphingosine (d14:1) prevents its interaction with sn-1,2-diacylglycerol (DAG)/Phorbol esters[1].