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 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 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 ...
SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM in a cell-free assay, 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6. SB 525334 shows no inhibition in the enzymes ALK2, 3, and 6, with IC50 values 1 ...
Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3. LY2157299 potently inhibits the TGFβ receptor signaling. LY2157299 abolishes the TGFβ induced Smad2 phosphorylation in HUVEC cells. LY2157299 also shows ...
TWS119 is a GSK-3β inhibitor with IC50 of 30 nM in a cell-free assay; capable of inducing neuronal differentiation and may be useful to stem cell biology. Treatment of a monolayer of P19 cells with 1 μM TWS119 causes 30–40% cells to differentiate specifically into neuron ...
HO-3867 , an analog of curcumin, is a selective STAT3 inhibitor. HO3867 produces significant cytotoxicity in A2780 and other tested ovarian cancer cell lines, with less toxic to noncancerous ovarian surface epithelial cells. HO-3867 induces G(2)-M cell cycle arrest in A2780 cells and p ...
GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1. GSK690693 is very selective for the Akt isoforms versus the majority of kinases in other ...
MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2. MK-2206 is an allosteric inhibitor and is activated by the pleckstr ...
Trifluoperazine is a dopamine D2 receptor inhibitor with IC50 of 1.1 nM. Trifluoperazine binds to α1A- and α1B-adrenoceptor with Ki value of 27.6 nM and 19.2 nM, respectively, with α1B/α1A ratio of 0.7. Trifluoperazine inhibits Mycobacterium tuberculosis (Mtb) wi ...
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