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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC24100 LY2365109 hydrochloride Featured
A potent and selective GlyT1 inhibitor with IC50 of 15.8 nM, displays no activity for GlyT2 (IC50>30 uM).
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DC8859 SKF38393 HCl Featured
SKF38393 HCl is a selective dopamine D1/D5 receptor agonist.
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DC4130 Tirapazamine Featured
Tirapazamine is an experimental anticancer drug that is activated to a toxic radical only at very low levels of oxygen (hypoxia). Such levels are common in human solid tumors, a phenomenon known as tumor hypoxia.
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DC23216 TCS 401 Featured
TCS 401 is a potent, selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B) with Ki of 0.29 uM, weakly inhibits the protein phosphatases CD45 D1D2, PTPβ, PTPε D1, SHP-1, PTPα D1, and LAR D1D2 with Ki of 59, 560, 1,100, >2,000, >2,000, and >2,000 u
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DC32283 Azeliragon HCl Featured
Azeliragon 2HCl (also known as TTP488 2HCl and PF-04494700 2HCl) is a potent and orally bioactive RAGE (Receptor for Advanced Glycation End products) inhibitor that has the potential for the treatment of mild-to-moderate Alzheimer's disease and cerebral amyloid angiopathy. RAGE is a pattern recognition receptor that affects the movement of amyloid (a biomarker for Alzheimer's disease) into the brain. In preclinical studies, azeliragon decreased brain amyloid in mice and improved their performance on behavior tests. Azeliragon has been shown to be involved in adaptive immune responses. It is currently in Phase 3 clinical trial.
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DC22521 SAR405 Featured
SAR405 is a highly potent and selective PI3K class III isoform Vps34 inhibitor with IC50 of 1.2 nM, inhibits the formation of autophagosomes in GFP-LC3 cells with IC50 of 4 nM.
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DC11565 E3 Ligase Ligand 2 Featured
E3 ligase Ligand 2 is a Ligand for E3 Ligase used in PROTAC technology.
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DC28934 VAF347 Featured
VAF347 is a cell permeable and highly affinity aryl hydrocarbon receptor (AhR) agonist and induces AhR signaling. VAF347 inhibits the development of CD14+CD11b+ monocytes from granulo-monocytic (GM stage) precursors. VAF347 has anti-inflammatory effects.
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DC48426 Rafutrombopag
Rafutrombopag is a thrombopoietin (TPO) agonist extracted from patent CN113929668 A.
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DC48425 TGFβR-IN-1
TGFβR-IN-1 is a long-acting tumor-activated prodrug of a TGFβR inhibitor.
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DC48423 Boc-NH-PEG11-OH
Boc-NH-PEG11-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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DC48422 6-Bnz-cAMP sodium salt
6-Bnz-cAMP sodium salt is a cell-permeable cAMP analog. 6-Bnz-cAMP selectively activates cAMP-dependent PKA but not Epac signaling pathways.
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DC48421 SHP2 protein degrader-1
SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for the treatment of SHP2 related diseases.
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DC48420 Orexin B, rat, mouse TFA
Orexin B, rat, mouse (Rat orexin B) TFA is an endogenous orexin receptor agonist. Orexin B, rat, mouse TFA binds and activates two closely related orphan G protein-coupled receptors OX1-R and OX2-R. Orexin B, rat, mouse TFA stimulates food intake and energy expenditure and plays a significant role in sleep-wakefulness regulation.
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DC48419 MA242 free base
MA242 free base is a specific dual inhibitor of MDM2 and NFAT1. MA242 free base directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 free base induces apoptosis in pancreatic cancer cell lines regardless of p53 status.
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DC48417 IL-17A inhibitor 2
IL-17A inhibitor 2 is an IL-17A inhibitor for treating psoriasis, rheumatoid arthritis, and multiple sclerosis.
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DC48416 Brecanavir
Brecanavir (GW640385) is a novel, potent HIV protease inhibitor.
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DC48415 Pirmitegravir
Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties.
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DC48414 EZH2-IN-6
EZH2-IN-6 is an EZH2 inhibitor with enhanced antitumor activity.
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DC48413 PRMT5-IN-15
PRMT5-IN-15 is a PRMT5 inhibitor with an IC50 value of 0.84 nM.
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DC48412 CPI-1328
CPI-1328 is an EZH2 inhibitor with a Ki value of 63 fM.
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DC48410 CPTH2 hydrochloride
CPTH2 hydrochloride is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 hydrochloride induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B).
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DC48408 GSK2818713
GSK2818713 is a novel Hepatitis C NS5A replication complex inhibitor.
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DC48407 NS5A-IN-1
NS5A-IN-1 is a prodrug of the HCV NS5A inhibitor Pibrentasvir (ABT-530).
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DC48406 KL-11743
KL-11743 is a potent, orally active, and glucose-competitive inhibitor of the class I glucose transporters, with IC50s of 115, 137, 90, and 68 nM for GLUT1, GLUT2, GLUT3, and GLUT4, respectively. KL-11743 specifically blocks glucose metabolism. KL-11743 can synergize with electron transport inhibitors to induce cell death.
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DC48405 BAY 1003803
BAY 1003803 is a glucocorticoid receptor agonist for the topical treatment of psoriasis or severe atopic dermatitis.
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DC48404 Ghrelin receptor full agonist-2
Ghrelin receptor full agonist-2 is a highly potent Ghrelin receptor full agonist.
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DC48403 Ftase inhibitor III
Ftase inhibitor III is an anion-dependent Farnesyltransferase inhibitor from a phenotypic screen.
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DC48402 EAAT2 activator 1
EAAT2 activator 1 is the potent activator of excitatory amino acid transporter 2 (EAAT2). EAAT2 is the major glutamate transporter and functions to remove glutamate from synapses. EAAT2 activator 1 increases EAAT2 protein levels dose-dependently.
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DC48400 Mal-PEG8-amide-Val-Ala-(4-NH2)-Exatecan
Mal-PEG8-amide-Val-Ala-(4-NH2)-Exatecan is a conjugate used to synthesis ADC. Mal-PEG8-amide-Val-Ala-(4-NH2)-Exatecan comprises topoisomerase inhibitor derivative with a linker for connecting to a ligand unit (extracted from patent US20200306243A1).
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