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 ...
Methazolastone causes formation of DNA alkali-labile sites which are present in similar amounts and repaired at a similar rate in L-1210 and L-1210/BCNU cell lines. In L-1210 but not in L-1210/BCNU methazolastone induces an arrest of cells in SL-G2-M phases. Methazolastone sensitivity o ...
Trametinib (GSK1120212) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. GSK1120212 inhibits the phosphorylation of MBP regardless of the isotype of Raf and MEK, wit ...
TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc. Phase 1. TAK-733 is highly potent and selective MEK allosteric site inhibitor with IC50 of 3.2 nM. TAK-733 shows pot ...
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