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Cat. No. Product Name CAS No. Information
PC-63129

LY 3200882

1898283-02-7

LY 3200882 (LY3200882) is a novel potent, highly selective, ATP competitive TGF-β receptor type 1 (TGFβRI, ALK5) inhibitor; potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors; LY 3200882 shows potent anti-tumor activity in the orthotopic 4T1-LP model of triple negative breast cancer and this activity correlated with enhanced tumor infiltrating lymphocytes in the tumor microenvironment.

Solid Tumors

Phase 1 Clinical

PC-60916

San78-130

66018-45-9

San78-130 is a potent, selective activin receptor-like Kinase 1 (ALK1) inhibitor with IC50 of 62 nM, with greater selectivity compared with L-783277; inhibits (>80%) only 6 kinases including ALK1, FLT3, FLT4, KDR, MEK2 and MKK6 in a panel of 342 kinases, shows weak inhibition for other ALK isotypes; suppresses the BMP9-induced Smad1/5 pathway by mainly inhibiting ALK1 in C2C12 cells, promotes angiogenesis in both endothelial tube formation and microfluidic chip based 3D angiogenesis assays

PC-60770

VU 0469381

1062368-49-3

A potent, sellective BMP receptor ALK2 antaognist with Ki of 32 nM, with no affinity for ALK3/4/5/6.

PC-60769

VU 0465350

1414843-61-0

A potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 92.3 nM; shows no activity for ALK2/4/5, also shows affinity for TGFBR2, VEGFR2 and AMPK; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver regeneration after partial hepatectomy.

PC-60768

VU 0364849

1206711-14-9

A potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 5.4 nM; also inhibits ALK6 (Ki<1 nM) and ALK2 (Ki=42.77 nM), little to no affinity for ALK4/5, BMPR2, AMPK etc.; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver regeneration after partial hepatectomy.

PC-42581

SB-431542

301836-41-9

SB-431542 is a potent, specific TGF-β type I receptor (ALK5) inhibitor with IC50 of 94 nM; also substantially inhibits ALK4 and 7, but not other ALKs; efficiently inhibits the ability of activated ALK4, ALK5, and ALK7 to phosphorylate Smad2; a selective inhibitor of endogenous activin and TGF-beta signaling but has no effect on BMP signaling, and has no effect on components of the ERK, JNK, or p38 MAP kinase pathways.

PC-45058

LDN-214117

1627503-67-6

A potent and selective ALK2 inhibitor with a biochemical IC50 of 24 nM, a cell-based IC50 for BMP6 of 100 nM; displays 164-fold selectivity for BMP6 versus TGF-β1; a highly selective probes of BMP-mediated cellular physiology.

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