TGF-β / Smad Signaling

Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that can bind to the ligands of the transforming growth factor β superfamily. Luspatercept increases red blood cell count and promotes maturation of red blood cell precursors. Luspatercept binds with GDF11, inhibiting the Smad2/3 signaling pathway. Luspatercept can be used for research on anemia.

Lyn-IN-1 (Bafetinib analog) is a highly active dual inhibitor of Bcr-Abl and Lyn.

PT-262 is an effective ROCK inhibitor with an IC50 value of approximately 5 μM. PT-262 induces loss of mitochondrial membrane potential and increases activation of caspase-3 and cell apoptosis. PT-262 inhibits phosphorylation of ERK and CDC2 through a p53-independent pathway. PT-262 blocks cellular cytoskeleton function and cell migration. PT-262 has anti-cancer activity.

R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 μM). R 59-022 hydrochloride inhibits OAG phosphorylation to OAPA. It is also a 5-HT receptor antagonist that can activate protein kinase C (PKC). R 59-022 enhances the production of thromboxane in platelets induced by thrombin and inhibits phosphatidic acid production in neutrophils.

SJ000063181 is an effective BMP signal activator with an EC50 ≤1 µM. It can be used as a chemical probe to explore BMP signaling because it can penetrate zebrafish embryos.

SY-LB-35 is an effective bone morphogenetic protein (BMP) receptor agonist. It can stimulate C2C12 cells to significantly increase cell number and cell vitality, causing the cell cycle to transition into S phase and G2/M phase. SY-LB-35 stimulates typical Smad and atypical PI3K/Akt, ERK, p38, and JNK intracellular signaling pathways.

TGFβ1-IN-1 is a highly effective, orally active transforming growth factor β1 (TGF-β1) specific inhibitor that can significantly block the TGF-β1 signaling pathway and inhibit the upregulation of fibrosis-related proteins (such as α-smooth muscle actin and fibronectin) mediated by it. It is suitable for the mechanism research and treatment development of fibroproliferative diseases such as liver fibrosis.

Trabedersen (AP 12009) is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen can be used to study malignant brain tumors and other solid tumors that overexpress TGF-β2, such as skin, pancreatic, and colon tumors.

Vamotinib (PF-114) is an effective, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the self-phosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib exhibits anti-proliferative and anti-tumor activity. Vamotinib has potential in the study of resistant Philadelphia chromosome-positive (Ph+) leukemia.

Z-Arg-SBzl is a substrate for activating protein C in both cows and humans.

(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor.

Rho-Kinase-IN-3 (compound 12) is a potent and selective Rho kinase (ROCK1) inhibitor with an IC50 value of 8 nM.

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.

LIMK-IN-1 (Compound 14) is an inhibitor of LIM-Kinase (LIMK), with IC50s of 0.5 nM and 0.9 nM for LIMK1 and LIMK2, respectively.

Chromenone 1 is a potent osteogenic bone morphogenetic protein (BMP) potentiator.

Zelasudil is a Rho-associated (ROCK) kinase inhibitor.

Chroman 1 dihydrochloride is a highly potent and selective ROCK inhibitor.

ROCK2-IN-6 hydrochloride (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research.

HG-7-86-01 (Compound 26) is type II tyrosine kinase inhibitor.

Kartogenin (KGN) sodium is an inducer of chondrogenic tissue formation (EC50: 100 nM).

Vanicoside A is a protein kinase C(PKC) inhibitor from Polygonum pensylvanicum.

SAMβA TFA is conjugated to the cell permeable peptide TAT47-57.

KRFK TFA, a peptide derived from TSP-1, can activate TGF-β.

Vicatertide is a TGF beta-1 inhibitor.