TGFβRI/ALK5 Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S7223 RepSox

RepSox is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively.

Selective TGFβR1(ALK5), IC50: 4 nM
S1476 SB525334

SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.

Selective TGFβR1(ALK5), IC50: 14.3 nM
S2750 GW788388

GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor.

Selective ALK5, IC50: 18 nM
S7624 SD-208

SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.

Selective TGF-βRI (ALK5), IC50: 48 nM
S2230 Galunisertib (LY2157299)

Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2/3.

Selective TβRI, IC50: 56 nM
S7530 EW-7197

EW-7197 is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.

Pan ALK5, IC50: 11 nM
S2704 LY2109761

LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2.

Pan TβRI, Ki: 38 nM
S2186 SB505124

SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6.

Pan ALK5, IC50: 47 nM
S2805 LY364947

LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, shows 7-fold selectivity over TGFβR-II.

Pan TGFβRI, IC50: 59 nM
S1067 SB431542

SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases.

Pan ALK5, IC50: 94 nM
S7359 K02288

K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.

Pan ALK5, IC50: 321 nM; ALK5, IC50: 321 nM
S7147 LDN-212854

LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively.

Pan ALK5, IC50: 9276 nM