You are here:Home-Inhibitors & Agonists-TGF-beta/Smad-TGF beta Receptor (TGFBR)

Request The Product List ofTGF beta Receptor (TGFBR) TGF beta Receptor (TGFBR)

Cat. No. Product Name CAS No. Information
PC-63322

JL5

2244238-50-2

JL5 is a novel potent, selective BMP receptor inhibitor with IC50 of 1, <5 and 2 nM for ALK2/ACVR1, ALK3/BMPR1A and ALK6/BMPR1B, respectively; shows much weaker acitivity against BMPR2, ALK5/TGFβR1 and TGFβR2 with IC50 of 8,510, 440 and 40 nM; shows a greater volume of distribution and suppresses the expression of Id1 and pTak1 in tumor xenografts, induces tumor cell death and tumor regression in xenograft mouse models without immune cells and humanized with adoptively transferred human immune cells.

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-61454

TP-0427736

864374-00-5

TP-0427736 (TP0427736) is a novel potent and selective ALK5 inhibitor with IC50 of 2.72 nM, displays 300-fold selecitvity over ALK3; inhibits Smad2/3 phosphorylation in A549 cells (IC50=8.7 nM) and decreases the growth inhibition of human outer root sheath cells; significantly decreases Smad2 phosphorylation in mouse skin after topical application, may serves as a potential new therapy for AGA.

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.

Request The Product List

* Indicates a Required FieldYour information is safe with us.

  • *Product List:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Country:
  • Additional Information:
Contact Us sales@probechem.com