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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC28782 MMP-9-IN-1 Featured
MMP-9-IN-1 is a specific matrix metalloproteinase-9 (MMP-9) inhibitor, which selectively target the hemopexin (PEX) domain of MMP-9, but not other MMPs.
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DC28149 SR59230A hydrochloride Featured
SR59230A hydrochloride is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.
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DC28441 BTSA1 Featured
BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediat
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DC29234 GSK621 (GSK 621;GSK-621) Featured
GSK621 (GSK-621) is a potent, specific AMPK agonist (activator), induces cytotoxicity in AML (IC50=13-30 uM) but not in normal hematopoietic cells; GSK621 is more potent than A-769662 at inducing AMPK activation, as measured by the level of ACC phosphoryl
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DC28576 DS-1001b Featured
DS-1001b is a mutant IDH-1 (Isocitrate Dehydrogenase-1) inhibitor extracted from patent WO2016052697A1, Example 168, and has antitumor activity.
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DC30025 TCS JNK 6o(JNK Inhibitor VIII) Featured
JNK Inhibitor VIII is an aminopyridine compound that inhibits JNK1, JNK2, and JNK3 with Ki values of 2, 4, and 52 nM, respectively.
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DC26034 NUC3373(Fosifloxuridine nafalbenamide) Featured
NUC-3373 is a phosphoramidate-based prodrug of the monophosphate form of 5-fluoro-2'-deoxyuridine, the active metabolite of fluorouracil,an antimetabolite fluoropyrimidine analog of the pyrimidine nucleoside, with potential antineoplastic activity.
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DC8531 TASP0415914 Featured
PI3Kγ is required for for T-cell and B-cell as well as mast cell migration and degranulation. As such, these kinases are attractive targets for potential anti-infmamatory drugs. TASP0415914 has shown excellent results in cell based assays. It is orally av
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DC8529 S6K-18 Featured
S6K-18 is a highly selective inhibitor of S6K1, with an IC50 of 52nM.
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DC8520 GSK-25 Featured
GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).
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DC8517 BS194 Featured
BS-194 is a selective and potent CDK inhibitor, which inhibits CDK2, CDK1, CDK5, CDK7, and CDK9 with IC50 values of 3, 30, 30, 250, and 90 nM respectively.
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DC21317 ML 086 (CID-1674999) Featured
ML 086 is a potent, specific inhibitor of phosphatase PHOSPHO1 with IC50 of 139 nM, with no activity against TNAP (IC50>100 uM).
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DC9243 LP533401 HCl Featured
LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.
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DC21072 Voxilaprevir Featured
Voxilaprevir (GS-9857) is a potent HCV NS3/4A protease inhibitor that is used in combination with sofosbuvir and velpatasvir for treatment of HCV infection.
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DC23302 Disarib Featured
Disarib is a novel BCL2-specific inhibitor that binds predominantly to the BH1 domain, demonstrates strong affinity to BCL2, but not to other antiapoptotic BCL2 family members(BCL-xL, BCL2A1 etc.).
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DC10134 Obicetrapib (AMG-899,TA-8995) Featured
Obicetrapib is a CETP inhibitor, on the elevation of high-density lipoprotein cholesterol (HDL-C) and reduction of low-density lipoprotein cholesterol (LDL-C), alone and in combination with statin therapy.
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DC46355 γ-Terpinene
γ-Terpinene, a monoterpene, is an orally active antioxidant compound which can scavenge radicals directly. γ-Terpinene has potent antinociception activity.
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DC12202 Pradefovir mesylate (Remofovir mesylate) Featured
Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.
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DC33076 NRC-2694 Featured
NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist potentially for the treatment of solid tumors.
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DC9365 MLN8054 Featured
MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM; exhibits more than 40-fold selective for Aurora A than Aurora B.
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DC11017 ZLDI-8 Featured
ZLDI-8 (IAC-8) is a novel Notch signaling pathway inhibitor for Notch activating/cleaving enzyme ADAM-17, significantly decreases the level of NICD and accumulation of NICD in the nucleus; exhibits cytotoxic acitviity against MHCC97-H cells with IC50 of 5.32 uM, reduces the expression of pro-survival/anti-apoptosis regulators, Survivin and cIAP1/2, also increases the expression of epithelial marker E-Cadherin and reduces mesenchymal markers N-Cadherin and Vimentin in HCC cells; significantly disrupted the activity of Notch pathway in HCC cells and inhibits the epithelial-mesenchymal transition (EMT) process of HCC cells; ZLDI-8 treatment enhances the susceptibility of HCC cells to Sorafenib, Etoposide, and Paclitaxel both in vitro and in vivo.
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DC11125 TCH-165 Featured
TCH-165 is a specific small molecule modulator of proteasome assembly, regulates the dynamic equilibrium between the 20S and 26S proteasome complexes, favoring 20S-mediated protein degradation.
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DC23376 KDM5-C70 Featured
KDM5-C70 is the cell-permeable derivative of KDM5-C49, potent, selective and cell permeable KDM5 inhibitor with IC50 of 0.3, 0.3 and 0.58 uM for KDM5A, B and C, respectively.
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DC10285 KDM5-IN-1 Featured
KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
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DC20650 AKI603 Featured
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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DC45109 β-Gentiobiose
β-Gentiobiose (Gentiobiose) is a naturally occurring oligosaccharin with a rapid turnover rate in ripening tomato fruit.
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DC8909 Maribavir Featured
Maribavir(GW257406X; BW1263W94; 1263W94) inhibits HCMV replication is by inhibition of an HCMV encoded protein kinase enzyme called UL97 or pUL97.
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DC7473 NVP-BHG712 Featured
NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
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DC12075 U18666A Featured
U18666A, a cell permeable drug, is a cholesterol synthesis and transport inhibitor.
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DC8650 Vps34-IN-1 Featured
VPS34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks.
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