Search results for: 'signaling pathways membrane transporter ion channel cftr AND select 5033'
Items 1-10 of 43
- LY2090314Catalog No. :A3570Potent GSK-3 inhibitorLY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) which plays an important role in many pathways, including initiation of protein synthesis, cell proliferation, cell differentiation, and apoptosis.
- LY2109761Catalog No. :A8464TβRI/II kinase inhibitorLY2109761 is a small-molecule inhibitor selectively targeting both TGF-β receptor type I and II ((TβRI/II)) with Ki of 38 nM and 300 nM, respectively . It gave IC50 value of 69 nM in TβRI enzymatic assay . Crystal structure showed the binding of LY2109761 to the ATP binding site of the TGF-β R1 kinase domain . Weak inhibitory activities were reported for other kinases, including Lck, Sapk2α, MKK6, Fyn, and JNK3 (18–89% inhibition at 20 µM) .
- Trametinib (GSK1120212)Catalog No. :A3018MEK1 and MEK2 inhibitor, potent and selective
Trametinib (also known as GSK1120212 or JTP 74057), originally identified as a p15 inductive compound, is a novel and potent allosteric inhibitor of MEK kinase, which exhibits ATP non-competitive inhibition against MEK1 and MEK2 kinase.
- BYL-719Catalog No. :A8346Selective PI3Kα inhibitor
BYL719 is a selective PI3Kα inhibitor with IC50 of 5 nM.
- Everolimus (RAD001)Catalog No. :A8169MTOR inhibitor
Everolimus, also known as RAD001, is a potent and orally bio-available inhibitor of mammalian target of rapamycin (mTOR), a key component of active PI3K/Akt pathway in human cancers.
- Gefitinib (ZD1839)Catalog No. :A8219Selective EGFR inhibitor
Gefitinib, also known as ZD1839 or Iressa, is a potent and orally-bioavailable small-molecule inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with 50% inhibition concentration IC50 values of 0.033 μM and 0.027 μM in A431 membrane prep and baculovirus lysate respectively.
- CyclopamineCatalog No. :A8340Hedgehog (Hh) signaling Inhibitor
Cyclopamine is a naturally occurring Hedgehog (Hh)‑specific small‑molecule signaling steroidal alkaloid inhibitor, causes a profound inhibition of tumor growth, has significant anti‑invasive, anti‑proliferative and anti‑estrogenic potency in human breast cancer cells  .
- LDE225 (NVP-LDE225,Erismodegib)Catalog No. :B2266Smoothened inhibitor,potent and selective
LDE225 is a potent and selective inhibitor of smoothened with IC50 values of 1.3nM in mouse and 2.5nM in human, respectively .
- Masitinib (AB1010)Catalog No. :A2942Tyrosine kinase inhibitor, potent and selectiveThe stem cell factor receptor (KIT) is a therapeutic target for the cancer, mastocytosis, and inflammatory diseases treatment. Masitinib (AB1010) is a novel phenylaminothiazole-type tyrosine kinase inhibitor that targets KIT.
- PF-00562271Catalog No. :A8320FAK/Pyk2 inhibitor,potent and ATP-competitive
PF-562271 is a potent, ATP-competitive and reversible inhibitor of both focal adhesion kinase (FAK), a non-receptor tyrosine kinase involved in a variety of cellular events, and proline-rich tyrosine kinase 2 (Pyk2), an FAK homolog containing 48% amino acid identity, with half maximal inhibitory concentration (IC50) of 1.5 nmol/L and 14 nmol/L respectively. As a potential therapeutic agent either alone or in combination with other agents for the treatment of cancer, PF-562271 has been reported to effectively inhibit the proliferation of tumors in both xenograft and transgenic mouse models, in which it dose-dependently inhibits FAK phosphorylation in tumor-bearing mice with half maximal effective concentration (EC50) of 93 ng/mL.