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Tyrosine Kinase (TK)

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BM0019 BMS-777607 ≥98% (HPLC) BMS-777607 is an ATP-competitive inhibitor of the Met kinase superfamily with IC50 values of 1.8, 3.9, 4.3, and 1.1 nM, respectively, for Ron, Met, Tyro-3, and AxI kinases. BMS-777607 has been studied in a variety of cancer models and has shown anti-cancer activity, causing increased apoptosis, and decreased proliferation and migration, although it has also been shown to induce polyploidy, which may lead to chemoresistance.
C7869 CEP-701 hydrate ≥98% (HPLC) CEP-701 is a Flt-3 receptor tyrosine kinase inhibitor.
SML1769 Cyclotraxin-B trifluoroacetate salt ≥95% (HPLC) Cyclotraxin-B is a potent and selective Trk B (BDNF/NT-3) receptor inhibitor. Cyclotraxin-B prevents receptor activation by BDNF without interfering with BDNF binding. Cyclotraxin-B has an IC50 value < 1 nM. In rodent studies Cyclotraxin-B, sometimes fused with tat-protein for increased brain permeability, has been shown to have anxiolytic properties, prevent cold hypersensitivity induced by BDNF, and to reduce cocaine self-administration.
D8696 DMH4 >99.0% (HPLC) DMH4 is a potent VEGF inhibitor and an angiogenesis inhbitor. It is a selective VEGF inhibitor with an IC50 of 161 nM for VEGFR inhibition compared to 8000 nM for AMPK. Unlike the structurally similar DMH1, which is a selective BMP inhibitor, DMH4 shows little affinitiy for BMP with an IC50 of 3500 nM for BMPR-I.
G3381 Geldanamycin from Streptomyces hygroscopicus ≥98% (HPLC), powder Geldanamycin is a potent antitumor antibiotic active at nanomolar concentration against 60 cell lines.
Geldanamycin binds specifically to the heat shock protein Hsp90 and to its endoplasmic reticulum homologue GP96, and thus interferes with conformational maturation of proteins and the cellular stress response. In addition, Geldanamycin is a potent inhibitor of the nuclear hormone receptor family.
G6649 Genistein synthetic, ≥98% (HPLC), powder Inhibitor of tyrosine protein kinase; competitive inhibitor of ATP in other protein kinase reactions. Antiangiogenic agent, down-regulates the transcription of genes involved in controlling angiogenesis.
G6776 Genistein from Glycine max (soybean), ~98% (HPLC) Inhibitor of tyrosine protein kinase; competitive inhibitor of ATP in other protein kinase reactions. Antiangiogenic agent, down-regulates the transcription of genes involved in controlling angiogenesis.
G0897 Genistin from Glycine max (soybean), ≥95% (HPLC) Inactive analog of genistein; useful as a negative control for genistein and other tyrosine kinase inhibitors.
Selective inhibitor of mammalian terminal deoxynucleotidyl transferase (TdT), with no measurable effect on mammalian or microbial DNA polymerases.
SML1047 GW2580 ≥98% (HPLC) GW2580 is a cell-permeable, potent and selective ATP-competitive inhibitor of cFMS kinase, receptor for macrophage-colony stimulating factor, M-CSF or CSF-1, and a key regulator of macrophage and osteoclast activation and differentiation. FMS is a type III receptor tyrosine kinase that binds to the macrophage or monocyte colony-stimulating factor (M-CSF or CSF-1). Overexpression of CSF-1 and/or FMS has been implicated in a number of disease states including the growth of metastasis of some types of cancer, in promoting osteoclast proliferation in bone osteolysis, and in several inflammatory disorders. GW2580 selectively inhibits cFMS-mediated cellular functions in vitro at 0.06 μM as well as CSF-1-dependent tumor growth in vivo. GW2580 was inactive against 26 other kinases.
H6649 Herbimycin A from Streptomyces hygroscopicus ≥95% (HPLC), powder An antibiotic that inhibits protein tyrosine kinase. Herbimycin A is a potent inhibitor of angiogenesis.
L1289 Lavendustin C ≥97%, solid Potent inhibitor of protein tyrosine kinases.
M1323 Midostaurin hydrate ≥98% (HPLC), solid Midostaurin is an inhibitor of tyrosine kinase, protein kinase C, and VEGF. Midostaurin inhibits cell growth and phosphorylation of FLT3, STAT5, and ERK. Midostaurin is a potent inhibitor of a spectrum of FLT3 activation loop mutations.
SML0333 NVP-BHG712 ≥98% (HPLC) NVP-BHG712 is a very potent, selective inhbitor of the receptor tyrosine kinase EphB4 (ED50 = 25 nM). NVP-BHG712 blocks Ephrin receptor autophosphorylation and VEGF-induced angiogenesis.
B7063 PD158780 ≥98% (HPLC) PD158780 is a potent, cell-permeable, reversible ATP-competitive inhibitor of EGFR tyrosine kinase activity with IC50 values of 0.008, 49 and 52 nM for EGFR, ErbB2 (HER2) and Erb4 (HER4).
PZ0114 PD-166866 ≥98% (HPLC) PD-166866 is a selective inhibitor of the FGF-1 receptor tyrosine kinase (FGFR1) with IC50 = 55 nM, and no effect on c-Src, PDGFR-b, EGFR or insulin receptor tyrosine kinases or MEK, PKC, and CDK4.
PZ0254 PF-06273340 ≥98% (HPLC) PF-06273340 is a brain penetrant, orally available and potent tropomyosin-related kinase (Trk) inhibitor. PF-06273340 is under development as a remedy acute and chronic pain.
P0042 PP2 ≥98% (HPLC) PP2 is a selective inhibitor of Src-family tyrosine kinases with >10,000-fold selectivity over ZAP-70 and JAK2.
R8907 RPI-1 ≥98% (HPLC) RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor. Recently it was discover that the compound also inhibits c-Met. Increased tumorigenicity, motility, and invasiveness have been described as biological consequences of HGF/Met deregulation in tumor cells, thus not surprisingly RPI-1 treatment of H460 cells resulted in a strong reduction of both colony number and size (IC50 = 24.5 + 0.5 microM). Compound is also active at mouse NSCLC H460 xenograft tumor and metastasis model. Mechanistically RPI-1 inhibits Met phosphorylation at Tyr1234/Tyr1235, known to activate the intrinsic kinase activity. It appears that " Ret/ptc1 cross talks with Met at transcriptional and signaling levels and promotes ?-catenin transcriptional activity to drive thyrocyte neoplastic transformation". It appears that we do not have anything specific in Ret area. Handbook lists RPI-1 as Ret inhibitor.
S9820 SU 11274 ≥98% (HPLC), powder SU 11274 is a Met tyrosine kinase inhibitor.
SU 11274 is a class I c-Met inhibitor that competes with ATP to bind to the activation loop of c-Met.1 Inhibition of c-Met by SU 11274 is effective in improving the clinical outcome in non-small cell lung cancer cell lines.2
PZ0150 SU5614 ≥98% (HPLC) SU5614 is a FMS-like tyrosine kinase 3 (FLT3) inhibitor; selective inhibitor of VEGF and PDGF receptor tyrosine kinases.
SML0465 Symadex ≥98% (HPLC) Symadex is an FMS-like tyrosine kinase 3 (FLT3) and topoisomerase-II inhibitor; ABCG2 substrate; cell cycle modulator.
T6318 Tyrphostin AG 34 ≥98%, solid Inhibitor of tyrosine protein kinase in human colon cancer cell lines.
T5818 Tyrphostin AG 974 ≥98%, solid Tyrphostin AG 974 is an EGFR protein tyrosine kinase inhibitor. Studies have reported that AG-974 can induce cell death in fibrosarcoma cell lines1.
T5943 Tyrphostin AG 1007 ≥98%, solid Tyrphostin AG 1007 is known to function as a receptor tyrosine kinase inhibitor. It has been reported that replacement of oxygen in the carbonyl group of AG-1007 significantly increased the inhibition of tyrosine autophosphorylation of IGF-1R1.
SML1163 UNC2881 ≥98% (HPLC) UNC2881 is a selective inhbitor of Mer kinase, a member of the TAM (Tyro3, Axl, Mer) receptor tyrosine kinase family. The IC50 values for inhibition of Mer, Axl and Tyro 3 are 4.3, 360 and 250 nM, respectively.