TGF-β / Smad Signaling

CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM.

BIO-013077-01 is a pyrazole TGF-β inhibitor.

Ruboxistaurin is an orally available inhibitor of protein kinase C (PKC), with IC 50 values of 0.36μM, 0.0047μM, and 0.0059μM for PKCα, βI, and βII, respectively.

Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers.

Myelin Basic Protein (MHP4-14) TFA, a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM).

Kobophenol A, an oligomeric stilbene, blocks the interaction between the ACE2 receptor and S1-RBD with an IC50 of 1.81 μM and inhibits SARS-CoV-2 viral infection in cells with an EC50 of 71.6 μM.

Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.

Aurothiomalate sodium is a potent and selective oncogenic PKCι signaling inhibitor.

PKC-iota inhibitor 1 (compound 19) is a protein kinase C-iota (PKC-ι ?) inhibitor with an IC50 value of 0.34 μM.

ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3.

EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung.

Fresolimumab is a high-affinity humanized monoclonal antibody that binds to and inhibits all isoforms of the protein transforming growth factor β (TGFβ). The K d values of Fresolimumab for TGFβ1, TGFβ2, and TGFβ3 are 1.7±0.6nM, 3.0±1.2nM, and 2.0±1.2nM, respectively.

Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide.

SNIPER(ABL)-020, conjugating Dasatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein.

Protein kinase inhibitor H-7 is a potent inhibitor of protein kinase C (PKC) and cyclic nucleotide dependent protein kinase, with a Ki of 6 μM for PKC.

Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington's research.

ROCK1-IN-1 is a ROCK1 inhibitor with a Ki value of 540 nM. ROCK1-IN-1 can be used for the research of hypertension, glaucoma and erectile dysfunction.

Disitertide diammonium is a specific inhibitor of transforming growth factor β1 (TGF-β1) receptor type I.

Ponsegromab (PF 06946860) is a potent and selective humanized anti- GDF15 antibody inhibitor with anti-cachexia activity.

Aprinocarsen (ISIS 3521) sodium is a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-alpha). Aprinocarsen sodium is a 20-mer oligonucleotide that can regulate cell differentiation and proliferation. It can inhibit the growth of human tumor cell lines in nude mice. Aprinocarsen sodium has value as a chemotherapy compound for human cancer.

Carotuximab (TRC105) is an IgG1 monoclonal antibody that can block endoglin (CD105) and its downstream Smad signaling pathway. Carotuximab has immunomodulatory and anti-tumor effects.

Elezanumab (ABT-555; AE12-1Y-QL) is a human monoclonal antibody that selectively targets repulsive guidance molecule A (RGMa). Elezanumab effectively inhibits RGMa-mediated BMP signaling through the SMAD1/5/8 pathway, with an IC50 of approximately 97 pM. Elezanumab promotes neuronal regeneration and neuroprotection in models of nerve injury and demyelination by binding to the N-terminal of RGMa, blocking BMP signaling, and lacking cross-reactivity with RGMc. Elezanumab has activity in promoting neuronal regeneration and neuroprotection without affecting iron metabolism.