Brigatinib | pan-ALK inhibitor
NMR (Conforms)
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Nintedanib (656247-17-5) is a potent inhibitor of VEGFR, PDGFR, FGFR (IC50 = 13-34 nM for VEGFR, 59-65 nM for PDGFR and 37-108 nM for FGFR subtypes).1 Also
Pazopanib (444731-52-6) inhibits multiple receptor tyrosine kinases including VEGFR1,2 and 3 (IC50s=10, 30, 47 nM respectively) and PDGFRα, β and c-Kit (IC50s=71, 84, 74 nM respectively)
ABT-869 (796967-16-3) ia a structurally novel, potent inhibitor of receptor tyrosine kinases inhibiting VEGFR and PDGFR and related kinases with IC50s= 3, 4, 4, 66, 3
JNK-IN-8 (1410880-22-6) is a potent and selective irreversible JNK inhibitor (IC50s=4.67, 18.7 and 0.98 nM for JNK1, 2 and 3 respectively).1 JNK blockade with JNK-IN-8 overcomes
GSK2636771 (1372540-25-4) is a potent, selective (>1000-fold over α, 10-fold over δ, and >2000-fold over γ), and orally bioavailable inhibitor of PI3Kß (IC50 = 5.2 nM).1
LDC1267 (1361030-48-9) is a potent and selective inhibitor of the TAM kinases Tyro3, Axl, and Mer (IC50s respectively: 8 nM, <5 nM, 29 nM).1 It was
LDC1267 (1361030-48-9) is a potent and selective inhibitor of the TAM kinases Tyro3, Axl, and Mer (IC50s respectively: 8 nM, <5 nM, 29 nM).1 It was
JH-X-119-01 (2227368-54-7) is a highly selective (only significantly inhibited YSK4 and MEK3 in a panel of over 300 kinases) and potent (IC50 = 9 nM) covalent
UCB9608 (1616413-96-7) is a potent (IC50 = 5 nM), highly selective, and orally bioavailable inhibitor of the phosphatidylinositol kinase PI4KIIIß.1 It acts as a potent immunosuppressive
JNK-IN-8 (1410880-22-6) is a potent and selective irreversible JNK inhibitor (IC50s=4.67, 18.7 and 0.98 nM for JNK1, 2 and 3 respectively).1 JNK blockade with JNK-IN-8 overcomes
UNC7467 (2922283-43-8) is a potent inhibitor of inositol hexakisphosphate kinase (IP6K) – the isoform IP3K1 regulates metabolism, promotes insulin secretion from ß cells, attenuates certain aspects
PF-543 (1706522-79-3) is a potent (IC50 = 2.0 nM) and selective (>100-fold over SphK2) reversible inhibitor of sphingosine kinase-1 (SphK1).1 It induced autophagy in head and neck squamous
CBR-470-1 (2416095-06-0) is an activator of NRF2 signaling (EC50 ~ 1 µM cellular ARE-LUC assay).1 It inhibits phosphoglycerate kinase 1 leading to a build-up of methylglyoxal which inactivates
3-[4-(4-Morpholinyl)pyrido[3’,2’:4,5]furo[3,2-d]pyrimidin-2-yl]-phenol
NMR (Conforms)
Nintedanib (656247-17-5) is a potent inhibitor of VEGFR, PDGFR, FGFR (IC50 = 13-34 nM for VEGFR, 59-65 nM for PDGFR and 37-108 nM for FGFR subtypes).1 Also
GSK2636771 (1372540-25-4) is a potent, selective (>1000-fold over α, 10-fold over δ, and >2000-fold over γ), and orally bioavailable inhibitor of PI3Kß (IC50 = 5.2 nM).1
3-[4-(4-Morpholinyl)pyrido[3’,2’:4,5]furo[3,2-d]pyrimidin-2-yl]-phenol
NMR (Conforms)
XMU-MP-1 (2061980-01-4) is a potent, reversible, and selective inhibitor of the HIPPO pathway kinases MST1 and MST2 (IC50s = 71 nM and 38 nM respectively).1 It
Selpercatinib (2152628-33-4) is a potent (IC50 = 0.45 nM)1 and selective inhibitor of RET kinase.2 Clinically relevant for the treatment of RET-altered non-small cell lung cancer3
WS6 (1421227-53-3) stimulates human β-cell proliferation both in a dispersed islet proliferation assay and in intact human cultures.1 It has been shown to induce both α-
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