Inhibitor/Activator
| Cat.No. | Name | Information |
|---|---|---|
| M9243 | ITD-1 | ITD-1 is a selective TGFβ receptor inhibitor with an IC50 of about 0.4-0.8 μM. |
| M5037 | A 83-01 | A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively).*The compound is unstable in solutions, freshly prepared is recommended |
| M2108 | SB-525334 | SB-525334 is a potent activin receptor-like kinase (ALK5)/ type I TGFβ-receptor kinase inhibitor with IC50 of 14.3 nM. |
| M2081 | LY2109761 | LY2109761 is a novel TGF-β receptor type I and type II dual inhibitor, with Ki values of 38 nM and 300 nM, respectively. |
| M2016 | LY364947 | LY364947 is a selective small molecule inhibitor of the TGFβ type I receptor kinase with IC50 of 59 nM. |
| M1980 | LY2157299 | LY2157299 (Galunisertib) is a novel clinically relevant TBRI (ALK5 kinase) inhibitor with IC50 of 56 nM. |
| M59322 | TGF-beta RI Kinase Inhibitor VII | TGF-beta RI Kinase Inhibitor VII is a selective TGF-β inhibitor. TGF-beta RI Kinase Inhibitor VII can effectively inhibit the TGF-β signaling pathway. TGF-beta RI Kinase Inhibitor VII has IC50 values of 13 μM and 0.63 μM for c-Src kinase and ALK5 kinase, respectively. |
| M59149 | TGFβ1-IN-1 | TGFβ1-IN-1 is a potent, orally active TGF-β1 inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin). |
| M57237 | AZ12601011 | AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth. |
| M54015 | LSKL TFA | LSKL TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. |
| M53984 | LSKL | LSKL is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. |
| M50385 | KRFK TFA | KRFK TFA is a peptide derived from TSP-1, which can activate TGF-β. |
| M24896 | Murlentamab | Murlentamab (3C23K; GM102) is a humanized anti-AMHRII antibody. AMHRII is the anti-Müllerian hormone receptor. Murlentama significantly promotes macrophage-mediated antibody-dependent cell-mediated cytotoxicity (ADCC). Murlentama stimulates pro-inflammatory and anti-tumor internal environment, recruits and activates T cells. Murlentama suppresses tumors growth by inducing naïve macrophage orientation and promoting tumor-associated macrophage (TAM) reprogramming. |
| M10596 | BIBF0775 | BIBF0775 is a potent and selective inhibitor of the transforming growth factor β receptor I (TGFβRI, Alk5) with an IC50 of 34 nM. |
| M9683 | SM16 | SM16 inhibits TGFβ-induced plasminogen activator inhibitor-luciferase activity (IC50=64 nM). |
| M9222 | LY3200882 | LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 is also used as an immune modulatory agent. |
| M5246 | EW-7197 | Vactosertib (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. |
| M5038 | SD-208 | SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII. |
| M5036 | A 77-01 | A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM. |
| M2550 | SB-505124 | Sb-505124 is a selective inhibitor of TGF-βI receptor (ALK4, ALK5, ALK7) with IC50 values of 129 nM and 47 nM for ALK4 and ALK5, respectively. Sb-505124 also inhibits ALK7, but not ALK1, 2, 3 and 6. |
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