Search results for: 'research-area pi3k-akt-signaling'
- GDC-0941Catalog No. :A8210PI3K inhibitor,potent and selective
GDC-0941 is a novel selective class I phosphatidylinositol-3-kinase (PI3K) inhibitor. Activation of PI3K/Akt signaling pathway is frequently associated with tumorigenesis. Deregulation of this pathway occurs frequently with a variety of cancers and may contribute to the resistance to many anticancer agents. Developing novel small molecules that specifically block the PI3K/Akt pathway may inhibit tumor growth. GDC-0941 is designed to bind the ATP-binding pocket of PI3K and to prevent formation of phosphatidylinositol-3, 4, 5-triphosphate (PIP3), a second messenger that transmits PI3K downstream signals. [2, 3] It binds to PI3K in an ATP-competitive manner.
- CCT128930Catalog No. :A8617AKT inhibitorCCT128930 is a novel potent ATP-competitive, AKT inhibitor with an IC50 of 6 nM.
- AZD8055Catalog No. :A8214MTOR inhibitor
AZD8055 is a selective inhibitor of mTOR kinase with IC50 of 0.8 nM . It competes with ATP at the ATP-binding cleft of mTOR. AZD8055 showed ~1000 fold selectivity against closely related kinases PI3K isoforms and ATM/DNA-PK . Furthermore, it had no significant activity against a panel of 260 kinases at 10 μM .
- Cucurbitacin ICatalog No. :A4512STAT3/JAK2 signaling inhibitorSelective inhibitor of STAT3/JAK2 signaling. Inhibits the activation of STAT3 and JAK2 and displays no activity on Src, Akt, ERK and JNK. Suppresses phosphotyrosine levels of STAT3, inhibits STAT3 DNA binding and STAT3-mediated gene expression. Induces apoptosis in cell lines expressing constitutively active tyrosine-phosphorylated STAT3.
- 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) .
- LY2157299Catalog No. :A8348TGF-βR1 inhibitor,potent and selective
LY2157299 is a potent small-molecule antagonist that specifically inhibits Transforming Growth Factor-β receptor I (TβRI).
- LY2228820Catalog No. :A5566P38 MAP kinase inhibitorLY2228820 is a potent, selective, ATP-competitive small-molecule inhibitor inhibiting α- and β-isoforms of p38 MAPK with IC(50) values of 5.3nM and 3.2 nM, respectively .
- Enzastaurin (LY317615)Catalog No. :A1670PKC beta inhibitor,potent and selective
Enzastaurin is an ATP-competitive, selective oral inhibitor of protein kinase Cβ with IC50 value of 6 nM .
- ICG 001Catalog No. :A8217Wnt/β-catenin pathway inhibitor
ICG001 is a small molecule inhibitor that targets Wnt/β-catenin pathway. It inhibits TCF/β-catenin mediated transcription by competing with β-catenin for CBP (CREB binding protein) but not p300 binding with an IC50 of 3 µM . It can be used to specifically evaluate the role of CBP/beta-catenin association on WNT signaling and cell physiology.
- Gefitinib hydrochlorideCatalog No. :A3433Potent EGFR inhibitor
Gefitinib is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR.