CAS NO. |
Products Name |
675576-97-3 |
Nutlin-3b |
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Nutlin-3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a |
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890090-75-2 |
Nutlin-3 |
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Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM; stabilizes p73 in p53-deficient cells |
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209984-57-6 |
LY411575 |
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LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch clevage with withIC50 of 0.39 nM |
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698387-09-6 |
Neratinib (HKI-272) |
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Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3 |
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1005342-46-0 |
LCL161 |
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LCL161 is an oral small molecule antagonist of Inhibitor of Apoptosis Proteins (IAPs) that sensitizes a subset of tumors from diverse lineages to treatment with cytotoxic therapies |
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1268524-70-4 |
(+)-JQ1 |
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(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2), binding to all bromodomains of the BET family, but not to bromodomains outside the BET family |
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1229236-86-5 |
LY2874544 |
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LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2 |
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1374828-69-9 |
GNE-0877 |
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GNE0877 is a highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitor with an IC50 of 3 nM. |
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1276105-89-5 |
CNX-1351 |
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CNX-1351 is a selective covalent Inhibitor of PI3Kα. CNX-1351 was tested against all four of the class I PI3K enzymes α, β, γ, and δ. In an end point assay, CNX-1351 potently inhibited PI3Kα and was 20−400 times less potent against β, γ, and δ. CNX-1351 inhibit PI3Kα signaling in cells and shows prolonged inhibition consistent with a covalent mechanism of Action. CNX-1351 inhibits growth of cells dependent on PI3Kα. CNX-1351 also inhibits PI3Kα signaling in vivo and bonds to p110α |
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471905-41-6 |
MK-0752 |
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MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2. |
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