Tyrosine Kinase-Like Inhibitors

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SML0788   A 83-01 ≥98% (HPLC) A 83-01 is a TGFβ kinase/activin receptor-like kinase (ALK 5) inhibitor (IC50=12 nM) that prevents phosphorylation of Smad2/3 and inhibits growth induced by TGFβ. A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. Also, A 83-01 inhibits the transcriptional activity induced by TGFβ type I receptor ALK-5, activin type IB receptor ALK-4 and nodal type I receptor ALK-7. A-83-01 induces an expansion of neonatal Nkx2.5-eGFP (+) cells.
DMSO: 5 mg/mL, clear (warmed)
SML1535 DMH2 ≥98% (HPLC) DMH2 is a potent antagonist of the BMP receptor activin receptor-like kinase 3 (ALK3, BMPR-IA) that enhance liver regeneration. DMH2 potently inhibits BMP signaling and induced the greatest reduction of cell growth and expression of Id family members in H1299 non-small cell lung carcinoma cells.
DMSO: 1 mg/mL, clear
SML1403   IN-1130 ≥98% (HPLC) IN-1130 is a potent inhibitor of the activin receptor-like kinase ALK-5 (Type 1 TGF1β recptor). The compound inhibits phosphorylation of Smad-2 with an IC50 of 36 nM. IN-1130 inhibits renal fibrosis, and also reduces tumor volume in prostate tumor xenografts in murine models.
DMSO: 10 mg/mL, clear
I6410 ISCK03 ≥98% (HPLC), solid ISCK03 inhibits in vitro phosphorylation of c-Kit in a dose dependent manner. ISCK03 inhibits SCF (stem cell factor)-induced c-kit phosphorylation in 501mel human melanoma cells. Complete inhibition was observed with 1 and 5 μM ISCK03.
DMSO: ≥20 mg/mL
H2O: insoluble
L6293 LY-364947 ≥98% (HPLC) LY-364947 is a selective, ATP-competitive inhibitor of Transforming Growth Factor-β Type I receptor kinase (TGF-β RI, ALK5) with IC50 = 59 nM. It is much less potent at related kinases, with IC50 = 400 nM for TGF-β RII and IC50 = 1400 nM for mixed lineage kinase-7 (MLK-7), a kinase in the MAP kinase signal pathway and closely related to TGF-β RII. LY-364947 inhibits TGF-β-dependent cellular growth (IC50 = 81 nM) in NIH 3T3 mouse fibroblasts.
DMSO: 2 mg/mL, clear
SML1273 ML347 ≥98% (HPLC) ML347 is a derivative of dorsomorphin that is a highly selective antagonist of BMP receptor isotypes ALK1 and ALK2 (IC50 values = 46 and 32 nM, respectively). ML347 has little effect on other ALK isoforms, including ALK3 (IC50 = 10 μM).
DMSO: 1 mg/mL, clear (warmed)
N6037 Neridronate ≥97% (NMR), solid Neridronate is a bone resorption inhibitor. It is used to treat Osteogenesis Imperfecta, an "orphan disease" characterized by a fragility of the bone enough to be named the "illness of bones of crystal".
H2O: >5 mg/mL
S4317 SB 431542 hydrate ≥98% (HPLC), powder Potent and selective inhibitor of transforming growth factor-β superfamily type I activin receptor-like kinase (ALK) receptors.
SB-431542 inhibits the TGF-β-mediated activation of SMAD proteins, expression of collagen and fibronectin, cell proliferation and cell motility. It does not inhibit kinases that are activated in response to serum or stress such as ERK, p38 or JNK.
DMSO: soluble 10 mg/mL
H2O: insoluble
S4696 SB-505124 hydrochloride hydrate ≥98% (HPLC) SB-505124 is an inhibitor of activin receptor-like kinase (ALK) 5, also known as transforming growth factor-α type I receptor kinase, with an IC50 of 47 ± 5 nM.
SB-505124 selectively inhibits TGF-β type I receptors, activin receptor-like kinases (ALK) 4, 5 and 7. It inhibits ALK4-, 5- and 7-mediated activation of Smad2, Smad3 and MAPK pathway induced by TGF-β.1 SB-505124 inhibits the human fibroblast trans-differentiation induced by the co-culture with Esophageal squamous cell carcinoma.2
DMSO: >10 mg/mL
H2O: insoluble
S8822 SB-525334 ≥98% (HPLC) SB-525334 blocks the activation of Smad2/3 induced by TGFβ1 in renal proximal tubule cells.4 The sensitivity of TGFβ1 is decreased by SB-525334 that benefits the pulmonary arterial hypertension condition by reversing the pulmonary arterial pressure.5 SB-525334 is reduces the tumor incidence and size of mesenchymal tumors such as uterine leiomyoma.6
SB-525334 is a potent activin receptor-like kinase (ALK5)/ type I TGFβ-receptor kinase inhibitor with IC50 = 14.3 nM.
DMSO: ≥20 mg/mL
S0447 SIS3 ≥98% (HPLC), powder SIS3 is a novel specific inhibitor of TGF-β1/ALK-5 phosphorylation of Smad3
Sugar insensitive 3 (SIS3) promotes drug-induced apoptosis and hinders the function of adenosine triphosphate (ATP)-binding cassette (ABC) transporter (ABCB1) and ABCG2. It resensitizes ABCB1 and ABCG2 overexpressed in cancerous cells, which contributes to chemotherapeutics.
DMSO: >20 mg/mL
H2O: <2 mg/mL