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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC33579 RO2959 Hydrochloride Featured
RO2959 is a novel, potent and selective CRAC current inhibitor. RO2959 completely inhibited cytokine production as well as T cell proliferation mediated by TCR stimulation or MLR (mixed lymphocyte reaction). RO2959 potently blocked TCR triggered gene expression and T cell functional pathways similar to CsA and another calcineurin inhibitor FK506.
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DC32533 TCPOBOP Featured
TCPOBOP is an agonist of the constitutive androstane receptor (CAR) (EC50 = 20 nM). TCPOBOP enhances the nuclear receptor CAR transactivation of cytochrome P450 (CYP), as dose-dependent direct agonist of CAR. The most potent known member of the phenobarbital-like class of CYP-inducing agents. TCPOBOP has been used for enhancing Mcl-1-Italics promoter functions in mouse hepatoma cells. TCPOBOP has also been used to study constitutive androstane receptor(CAR)-induced gene expression in mouse hepatocytes.
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DC11706 R-10015 Featured
A potent, selective inhibitor of human LIMK1 with IC50 of 38 nM .
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DC21486 PF-05150122 Featured
PF-05150122 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5..
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DC22137 LGD2226 Featured
LGD-2226 (LGD2226) is an orally active, selective androgen receptor modulator (SARM) with binding Ki of 1 nM, >1000-fold selectivity over GR,PR, MR and ER.
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DC40718 Pyrrolnitrin Featured
Pyrrolnitrin is an antibiotic isolated from Pseudomonas pyrrocinia. Pyrrolnitrin shows a broad spectrum of antibiotic activity against fungi, yeast and gram-positive bacteria.
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DC11802 AX-024 free base Featured
AX-024 is an cytokine release inhibitor which can strongly inhibit the production of interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10 and IL-17A.
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DC7085 BIBR-1532 Featured
BIBR 1532 is a potent, selective, non-competitive telomerase inhibitor with IC50 of 100 nM.
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DC22587 FT011 Featured
FT011 is an anti-fibrotic agent, reduces mRNA expression of collagens I and III and inhibits collagen synthesis.
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DC22552 IC-87201 Featured
A small molecule inhibitor of PSD-95/nNOS interaction with IC50 of 31 uM, without inhibiting nNOS catalytic activity.
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DC7843 JNJ 42153605 Featured
JNJ 42153605 is a positive allosteric modulator of the metabotropic glutamate 2 receptor.
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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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