博文
- 一种双重ATP竞争性 PI3K 和 mTOR 抑制剂-BEZ235
- BEZ235 (NVP-BEZ235, Dactolisib) 是一种双重ATP竞争性 PI3K 和 mTOR 抑制剂，在无细胞试验中，抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR，IC50 为 21 nM，而对 Akt 和 PDK1 的抑制作用很弱。Phase 2。 BEZ235 ...
- 一种23元大环内酯物-Tacrolimus (FK506)
- Tacrolimus (FK506) 是一种23元大环内酯物，通过结合到抑免蛋白 FKBP12 (FK506 结合蛋白) 产生新的复合物，从而降低T细胞中肽酰脯氨酰异构酶活性。 FK-506和环孢霉素A阻断细胞质成分的移位，而不影响T淋巴细胞中核亚基的合成。 FK-506通过抑制需要白细胞介素-2转录诱导的Ca(2+)-依 ...
- Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ
- Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Phase 2. GDC-0941 is equipotent against PI3Kα and PI3Kδ as well as PI3Kα mutants E545-K and H1047-R, displayi ...
- BEZ235 (NVP-BEZ235, Dactolisib) is a dual ATP-competitive PI
- BEZ235 (NVP-BEZ235, Dactolisib) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. &nbs ...
- CL-387785 (EKI-785) is an irreversible, and selective EGFR i
- CL-387785 (EKI-785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM. CL-387785 blocks EGF-stimulated autoposphorylation of the receptor in cells (IC50, 5 nM), In cell lines that overexpress EGF-R or c-erbB-2, CL-387785 inhibits cel ...
- Osimertinib (AZD9291) is an oral, irreversible, and mutant-s
- Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3. AZD9291 shows significantly more potent inhibition of proliferat ...
- Cimetidine, a histamine congener, competitively inhibits
- Cimetidine (Tagamet) , a histamine congener, it competitively inhibits histamine binding to histamine H2 receptors. Cimetidine has a range of pharmacological actions. It inhibits gastric acid secretion, as well as pepsin and gastrins output. It also blocks the activity of cytochrome P-450 which ...
- Nizatidine is a histamine H2 receptor antagonist
- Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM. Nizatidine, a selective histamine H2-receptor antagonist, is a potent inhibitor of gastric acid secretion, with IC50 of 0.9 nM. Nizatidine also reve ...
- RO4929097 is a γ secretase inhibitor
- RO4929097 is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2. RO4929097 decreases the amount of Aβ peptides secreted into the culture medium in HEK293 c ...
- EUK 134, a synthetic superoxide dismutase (SOD)/catalase mim
- EUK 134, a synthetic superoxide dismutase (SOD)/catalase mimetic, exhibits potent antioxidant activities, and inhibits the formation of β-amyloid and related amyloid fibril. EUK 134 shows potent catalase and SOD activities, and protects human fibroblasts against cytotoxicity by gl ...
