TGFβRI/ALK5 Selective Inhibitors
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
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|
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|
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|
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|
Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2/3.
|Selective||TβRI, IC50: 56 nM|
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|
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|
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|
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|
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|
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|
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|