| DC20650 |
AKI603
Featured
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AKI-603 is a novel small molecule Aurora A kinase inhibitor with IC50 of 12.3 nM, also inhibits Aurora B kinase activity to a less extent; disrupts normal spindle structure, and induces cell-cycle arrest; t; suppresses stem cell properties in breast cancer cells, and also suppresses the expression of self-renewal genes (β-catenin, c-Myc, Sox2, and Oct4); reduces xenograft tumor growth after intragastric administration. |
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| DC23772 |
CMLD-2 |
A novel small molecule disruptor of HuR-mRNA interaction with Ki of 350 nM. |
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| DC11632 |
Cardioprotectant |
A novel small molecule inducer of heme oxygenase-1 that protect human iPSC-derived cardiomyocytes from oxidative stress. |
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| DC25072 |
Deltasonamide 1 |
A novel small molecule inhibitor of PDE6δ/KRas interaction with Kd of 203 pM. |
|
| DC11817 |
Compound L |
A novel small molecule inhibitor of the DNA repair protein Ku70/80, disrupts of Ku70/80-DNA interaction with IC50 of 3.5 uM in EMSA assay. |
|
| DC21679 |
Spindlactone A |
A novel small molecule inhibitor of transforming acidic coiled-coil-containing protein 3 (TACC3) that selectively inhibits the nucleation of centrosome microtubules in ovarian cancer cells. |
|
| DC21680 |
Spindlactone B |
A novel small molecule inhibitor of transforming acidic coiled-coil-containing protein 3 (TACC3) that selectively inhibits the nucleation of centrosome microtubules in ovarian cancer cells. |
|
| DC22764 |
CS-11 |
A novel small molecule inhibitor that inhibits PP2A and β-catenin interaction by selectively engaging PR55α binding site (Kd=45 pM). |
|
| DC11822 |
YD-277 |
A novel small molecule KLF5 inhibitor derived from ML264, demonstrates >10-fold enhanced efficacy in multiple cancer cell lines with IC50 of 1.5-10 uM. |
|
| DC22879 |
YK-3-237 |
A novel small molecule sirtuin-1 (SIRT1) activator that reduces acetylation of mutant 53 and exhibits anti-proliferative effects against TNBC cells carrying mutant p53. |
|
| DC21330 |
MM-206 |
A novel small molecule STAT3 inhibitor that inhibits STAT3 DNA binding activity with IC50 of 1.16 uM, binds to the STAT3 coiled-coil domain (CCD). |
|
| DC11954 |
JP-153
Featured
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JP-153 (JP153) is a novel small molecule targets the Src-FAK-Paxillin signaling, inhibits Src-dependent phosphorylation of paxillin (Y118) and downstream activation of Akt (S473) in RECs; potently inhibits VEGF-induced proliferation and migration, inhibits retinal neovascularization in the murine oxygen-induced retinopathy model.
|
|
| DC20389 |
GATA4 activator 7 |
A novel small molecule that activates GATA4/NKX2-5 transcriptional synergy with EC50 of 7 uM in cell reporter assay. . |
|
| DC21039 |
GATA4-IN-3
Featured
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A novel small molecule that inhibits GATA4/NKX2-5 transcriptional synergy with IC50 of 3 uM, with no activity on the protein kinases involved in the regulation of GATA4 phosphorylation. |
|
| DC11852 |
CTX-1 |
A novel small molecule that overcomes HdmX-mediated p53 repression, binds directly to HdmX (Kd=450 nM) to prevent p53-HdmX complex formation. |
|
| DC11669 |
CB-002
Featured
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CB-002 is a novel small molecule that restores p53 function in mutant p53-expressing colorectal cancer cells without toxicity to normal human fibroblasts; increases expression of endogenous p53 target genes NOXA, DR5, and p21 and cell death; decreases the stability of mutant p53 in RXF393 cancer cells and an exogenously expressed R175H p53 mutant in HCT116 p53-null cells. |
|
| DC21426 |
NSC654259 |
A novel small molecule Wnt signaling inhibitor that targets the cysteine-rich domain of Frizzled, specifically binds to the Wnt binding site on the Frizzled8 cysteine-rich domain with Kd of 2.9 uM, IC50 of 5.7 uM.. |
|
| DC11877 |
F3406 |
A novel small-molecule arenaviruse inhibitor that exhibits strong anti-LCMV activity (IC50<1 uM) without cell toxicity. |
|
| DC11908 |
Ralaniten |
A novel small-molecule inhibitor of androgen receptor (AR) N-terminal domain inhibitor for the treatment of advanced prostate cancer. |
|
| DC11909 |
Ralaniten acetate |
A novel small-molecule inhibitor of androgen receptor (AR) N-terminal domain inhibitor for the treatment of advanced prostate cancer. |
|
| DC20873 |
CCT-031374 hydrobromide |
A novel small-molecule Wnt signaling inhibitor that inhibits TCF-dependent transcription with IC50 of 6.1 uM in 7dF3 reporter assay. |
|
| DC21232 |
Licogliflozin |
A novel sodium glucose transporter type 1 and type 2 (SGLT1/2) inhibitor for the oral treatment of type 2 diabetes.. |
|
| DC23587 |
AMG1 |
A novel specific CRAC channel inhibitor that blocks function of effector but not regulatory T cells in vitro and attenuates the pogression and severity of EAE in vivo. |
|
| DC21056 |
GMI-1271
Featured
|
A novel specific glycomimetic E-Selectin antagonist with Kd of 0.46 uM, IC50 of 1.75 uM. |
|
| DC11795 |
BL-140 |
A novel specific p110β inhibitor with IC50 of 5.74 nM. |
|
| DC22863 |
FPND |
A novel specific ROCK1 kinase inhibitor with IC50 of 11.2 uM, without inhibitory activity against ROCK2. |
|
| DC20372 |
Elismetrep |
A novel specific TRPM8 channel antagonist for treatment or prevention vasomotor symptoms.. |
|
| DC12000 |
AUT2 |
A novel specific, cell permeant modulator of Kv3 channels with EC50 of 0.9 and 1.9 uM for Kv3.1b and Kv3.2a, respectively. |
|
| DC22931 |
1Z105 |
A novel synthetic, orally bioavailable TLR4/MD2 ligand, significantly reduces the IL-6 secretion by subsequent challenge with LPS at 0.63 uM. |
|
| DC23945 |
Pyr10
Featured
|
Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels[1]. |
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