TGF-β / Smad Signaling

ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).

p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1.

Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca2+ influx from an internal store in RBL-213 cells.

Protein Kinase C 19-31, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity.

Protein Kinase C 19-36 is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC50 of 0.18 μM.

Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.

ROCK inhibitor-2 is a selective Rho kinase (ROCK) inhibitor with IC 50 values of 17nM and 2nM for ROCK1 and ROCK2, respectively, and has anti-tumor activity.

Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect.

Y-33075 is a potent ROCK (Rho-associated protein kinase) inhibitor with an IC 50 value of 3.6nM.

A coumarin with diverse biological activities

DCPLA-ME, the methyl ester form of DCPLA, is a potent PKCε activator for use in the treatment of neurodegenerative diseases.

Desmethylglycitein, a metabolite of daidzein, is a potent tyrosinase inhibitor with an IC 50 value of 9.2μM for mushroom tyrosinase.

GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM).

CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.

N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.

LSKL, Inhibitor of Thrombospondin TSP-1, is a tetrapeptide derived from Latency-Associated Protein (LAP)-TGFβ. LSKL competitively binds to and inhibits TGF-β1.

Bosutinib-d8 is intended for use as an internal standard for the quantification of bosutinib by GC- or LC-MS.

Pirfenidone-d5 is intended for use as an internal standard for the quantification of pirfenidone by GC- or LC-MS.

L-erythro Sphingosine is a synthetic stereoisomer of sphingosine (d18:1).

Trimethylamine N-oxide (TMAO) is a product of the oxidation of TMA by flavin-containing mono-oxygenase 3 in the liver.

A natural mycotoxin

Afuresertib is a selective, orally bioavailable inhibitor of Akt1, 2, and 3 with Ki values of 0.08, 2, and 2.6 nM, respectively.

C8 Ceramide (d18:1.8:0) (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides.

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability.