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Cat. No. Product Name CAS No. Information
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.

PC-45749

EW-7197

1352608-82-2

EW-7197 (Vactosertib, TEW-7197) is a highly potent, selective inhibitor of TGF-β type I receptor kinase (ALK5) with IC50 of 11 nM; also inhibits ALK4 (IC50=13 nM) and shows less potency for p38α (IC50=280 nM); exhibits no inhibition on ALK1/2/3/6 (>10 uM); inhibits Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in MMTV/c-Neu mice and 4T1 orthotopic-grafted mice; oral bioavailability (Hcl salt).

Blood Cancer

Phase 1 Clinical

PC-35964

BMP signaling agonist sb4

100874-08-6 BMP signaling agonist sb4 is a small molecule BMP signaling agonist with EC50 of 73.6 nM, enhances the efficacy of BMPs and activates endogenous BMP4 target genes; increases the phosphorylation of key second messengers (SMADs-1/5/9) and also increased expression of direct target genes (inhibitors of DNA binding, ID1 and ID3) in canonical BMP signaling.
PC-35812

AZ12799734

1117684-36-2 AZ12799734 (AZ-12799734) is a pan BMP/TGFβ inhibitor that potently inhibits ligand activated SMAD3/4 transcription with IC50 of 47 nM, inhibits receptor-mediated phosphorylation of SMAD1 by ALK1, BMPR1A and BMPR1B and phosphorylation of SMAD2 by ALK4, TGFBR1 and ALK7; inhibits TGFβ-induced migration in HaCaT cells.
PC-35811

AZ12601011

AZ12601011 (AZ-12601011) is a potent, selective inhibitor of ALK4, ALK7 and TGFBR1 (Kd=2.9 nM), inhibits TGFβ-induced reporter activity with IC50 of 18 nM; inhibits TGFBR1 kinase activity (competition binding) with Kd of 2.9 nM, shows some inhibitory activity against the related receptors ALK4 and BMPR1B, but shows only weakly activity against ALK1, ALK2 and BMPR1A in in vitro kinase assays; AZ12601011 is a more effective inhibitor of TGFβ-induced reporter activity than SB-431542 (IC50=84nM) and LY2157299 (galunisertib) (IC50=380nM), inhibits phosphorylation of SMAD2 via the type 1 receptors ALK4, TGFBR1 and ALK7; AZ12601011 is highly effective at inhibiting basal and TGFβ-induced migration of HaCaT keratinocytes, inhibits tumour growth and metastasis to the lungs in a 4T1 syngeneic orthotopic mammary tumour model.
PC-43408

SD-208

627536-09-8 SD-208 is a potent, selective TGF-β receptor I kinase (TGF-βRI) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII kinase and >20-fold over a panel of related protein kinases; inhibits the growth inhibition of TGF-beta-sensitive CCL64 cells mediated by recombinant TGF-β1 or TGF-β2 or of TGF-β-containing glioma cell supernatant with EC50 of 0.1 uM; inhibits constitutive and TGF-β–induced invasion of glioma cells, inhibits TGF-β signaling in immune effector cells; blocks TGF-β signaling in the brain and inhibits the growth of syngeneic SMA-560 experimental gliomas in vivo.

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