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YO-01027 interacts directly with the¦Ã-secretase complex and targets the N-terminal Presenilin fragment. Increasing concentrations of YO-01027 administered to APPL- or Notch-expressing cells leads to the progressive accumulation of APPL CTF fragments and a decrease in NICD production in a strictly dose-dependent manner. 10 ¦ÌM of YO-01027 reduces breast cancer stem cells (BCSC) number and activity. A recent research indicates YO-01027 impairs mucin protein MUC16 biosynthesis in a concentration-dependent manner in undifferentiated cells at both preconfluent and confluent stages through Notch inhibition, but not in postmitotic stratified cells.

June 21, 2017

prudect name : YO-01027 interacts directly with the¦Ã-secretase complex and targets the N-terminal Presenilin fragment. Increasing concentrations of YO-01027 administered to APPL- or Notch-expressing cells leads to the progressive accumulation…

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Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

prudect name : Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.Y…

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XMD17-109 is a novel, specific ERK-5 inhibitor with an EC50 4.2 uM in HEK293 cells.

prudect name : XMD17-109 is a novel, specific ERK-5 inhibitor with an EC50 4.2 uM in HEK293 cells.XMD17-109 Synonyms: CAS NO: 1435488-37-1Molecular Formula: C36H46N8O3Molecular Weight: 638.8Purity: 98% minSolubility: in DMSOStorage:…

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XL147 is a selective inhibitor of Class I PI3K isoforms. XL147 reversibly binds to class 1 PI3Ks in an ATP-competitive manner, inhibiting the production of PIP3 and activation of the PI3K signaling pathway.XL147 exhibits dose-dependent and sustained inhibition of PI3K signaling in multiple human tumor xenograft models when administered as a single agent. Administration of XL147 in combination with various targeted and chemotherapeutic agents results in enhanced anti-tumor activity in multiple xenograft models over that observed with the corresponding single agents.

prudect name : XL147 is a selective inhibitor of Class I PI3K isoforms. XL147 reversibly binds to class 1 PI3Ks in an ATP-competitive manner, inhibiting the production of PIP3 and…

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XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.

prudect name : XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in…

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XL-019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1; shows good biochemical and cellular potency against JAK2 with good selectivity against the Janus Kinase family as well as a broad kinase panel.

prudect name : XL-019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, 100 fold selectivity over JAK1; shows good biochemical and cellular potency against JAK2 with…

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PI3K-IN-1 is a potent inhibitor of PI3K, more information can be found in patent WO2012103524 A2 and WO2013147649 A2.

prudect name : PI3K-IN-1 is a potent inhibitor of PI3K, more information can be found in patent WO2012103524 A2 and WO2013147649 A2.XL-765, SAR245409 Synonyms: PI3K-IN-1CAS NO: 1349796-36-6Molecular Formula: C31H29N5O6SMolecular Weight:…

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XL388 is a Novel Class of Highly Potent, Selective, ATP-Competitive, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin (mTOR). XL388 inhibited cellular phosphorylation of mTOR complex 1 (p-p70S6K, pS6, and p-4E-BP1) and mTOR complex 2 (pAKT (S473)) substrates. XL388 displayed good pharmacokinetics and oral exposure in multiple species with moderate bioavailability. Oral administration of XL388 to athymic nude mice implanted with human tumor xenografts afforded significant and dose-dependent antitumor activity.

prudect name : XL388 is a Novel Class of Highly Potent, Selective, ATP-Competitive, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin (mTOR). XL388 inhibited cellular phosphorylation of mTOR…

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XL647 is an orally bioavailable small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. XL647 binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including epidermal growth factor receptor (EGFR; ERBB1), epidermal growth factor receptor 2 (HER2; ERBB2), vascular endothelial growth factor receptor (VEGFR), and ephrin B4 (EphB4). This may result in the inhibition of tumor growth and angiogenesis, and tumor regression.

prudect name : XL647 is an orally bioavailable small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. XL647 binds to and inhibits several tyrosine receptor kinases that play major…

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XMD8-92 is highly selective ERK5/BMK1 inhibitor (KD values are 80, 190, 600 and 890 nM for BMK1, DCAMKL2, PLK4 and TNK1 respectively). XMD8-92 displays selectivity over 402 diverse kinases. XMD8-92 blocks growth factor-induced activation of cellular BMK1 and reduces BMK1 activity in in vitro kinase assays. XMD8-92 also reduces BMK1-dependent transactivating activity of MEF2C. XMD8-92 inhibits proliferation in a variety of cancer cell lines; blocks tumor cell proliferation and tumor-associated angiogenesis.

prudect name : XMD8-92 is highly selective ERK5/BMK1 inhibitor (KD values are 80, 190, 600 and 890 nM for BMK1, DCAMKL2, PLK4 and TNK1 respectively). XMD8-92 displays selectivity over 402…

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