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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC80889 JNK3-IN-10
JNK3-IN-10 is a blood-brain barrier-impermeable JNK3 inhibitor (IC50=0.257 nM) with over 400-fold selectivity over JNK1. JNK3-IN-10 blocks the JNK3-mediated signaling pathway downstream of TGF-β1, inhibits TGF-β1-induced phosphorylation of c-Jun, reduces the expression of pro-fibrotic markers, and restores the expression of the epithelial protein E-cadherin. JNK3-IN-10 exhibits low cytotoxicity, anti-fibrotic, cytoprotective and renoprotective effects, and alleviates albuminuria, glomerulosclerosis and podocyte foot process fusion. JNK3-IN-10 can be used for the research of chronic kidney disease, glomerulosclerosis and adriamycin-induced nephropathy.
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DC80888 JNK2/MKK7 PPI-IN-1
JNK2/MKK7 PPI-IN-1 is an orally active JNK2 inhibitor with an IC50 of 0.99 μM and a Kd of 81.6 μM. JNK2/MKK7 PPI-IN-1 inhibits JNK2 kinase activity, disrupts JNK2-MKK7 protein-protein interaction, and reduces c-Jun phosphorylation. JNK2/MKK7 PPI-IN-1 inhibits LPS-induced overexpression of inflammatory cytokines IL-6 and TNF-α. JNK2/MKK7 PPI-IN-1 can be used for the research of acute lung injury.
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DC80886 JNJ-10450232
NTM-006 is a selective and brain-penetrant adenosine A3 receptor (A3AR) agonist. NTM-006 selectively interacts with adenosine A3AR via π-π stacking with Phe168 and π-alkyl interactions receptor residues. NTM-006 inhibits Acetic acid-induced writhing responses in mice. NTM-006 can be used for the research of chronic neuropathic pain, cancer-related pain, osteoarthritis-associated pain.
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DC80885 JI-101 hydrochloride
JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity.JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis.JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes.JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route.JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors.
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DC80884 JHU-58
JHU-58 is a peptidomimetic agonist targeting mouse MRGPRC11 and rat MRGPRC receptors. JHU-58 demonstrates analgesic effects in mouse models of neuropathic pain. JHU-58 is promising for research of neuropathic pain.
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DC80880 JAK2-IN-20
JAK2-IN-20 is an orally active dual inhibitor targeting JAK2 kinase (IC50=49.17 nM) and influenza A virus PB2 protein (IC50=3.337 μM, Kd=2.82 μM). JAK2-IN-20 effectively blocks the JAK/STAT signaling pathway by reducing the phosphorylation levels of STAT1 and STAT3, thereby inhibiting viral replication and downregulating the expression of viral NP and PB2 proteins. In addition, JAK2-IN-20 significantly inhibits the mRNA expression of key inflammatory cytokines such as IL-6, TNF-α and IFN-β in inflammation and influenza infection models. JAK2-IN-20 serves as an important tool molecule for the study of influenza A virus infection and related pathologies.
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DC80879 JAK2-IN-18
JAK2-IN-18 (Compound example1) is a selective JAK2 inhibitor. JAK2-IN-18 can inhibit JAK-STAT signaling and shows an IC50 of <100 nM for pSTAT5 in HEL9217 cells. JAK2-IN-18 can inhibit the proliferation of abnormally proliferating myeloid cells and can be used for the research of myeloproliferative disorders, such as essential thrombocythemia.
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DC80878 JAK2-IN-16
JAK2-IN-16 (Compound Example 4) is a JAK2 V617F inhibitor. JAK2-IN-16 can be used for the research of cancer.
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DC80877 JAK2-IN-15
JAK2-IN-15 is an orally active, potent, selective JAK2 inhibitor (IC50 = 1.17 nM). JAK2-IN-15 can inhibit the AK2-STAT signaling pathway. JAK2-IN-15 significantly improves key pathological indicators such as hematocrit and splenomegaly in an Epoetin beta (rhEPO)-induced mouse model. JAK2-IN-15 can be used for the study of Polycythemia Vera (PV).
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DC80876 JAK1-IN-20
JAK1-IN-20 (Compound 38) is a gut-restricted, orally active, selective JAK1 inhibitor with an IC50 of <0.5 nM. JAK1-IN-20 inhibits the enzymatic activity of JAK1, reduces the production of proinflammatory cytokines (TNF-α, IL-6), and suppresses the phosphorylation of STAT3. JAK1-IN-20 ameliorates ulcerative colitis. JAK1-IN-20 can be used for the research of inflammatory bowel disease.
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DC80875 JAK1/2-IN-2
JAK1/2-IN-2 (Compound 37) is a potent and selective JAK1/2 inhibitor with Ki values of 2 and 0.6 nM .
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DC80873 J-104118
J-104118 is a potent and orally active squalene synthase (SQS) inhibitor with an IC50 of 0.52 nM. J-104118 inhibits cholesterol synthesis in mice. J-104118 can be used for cholesterol-lowering research.
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DC80872 IVL 745
IVL 745 (XRP 1745A) is a very late antigen 4 (VLA-4, integrin α4β1) antagonist. IVL 745 reduces the airway inflammatory response of sensitized rats and sheep. IVL 745 can be used for airway inflammation and asthma research.
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DC80870 ITRI-90
ITRI-90 is an orally active androgen receptor (AR) PROTAC degrader. ITRI-90 effectively degrades both full-length AR (AR-FL) and the splice variant AR-V7 protein via the ubiquitin-proteasome system, thereby inhibiting AR transcriptional activity and the target gene expression. ITRI-90 significantly inhibits the proliferation of prostate cancer cells and induces apoptosis, include Enzalutamide-resistant growth cell. ITRI-90 exhibits favorable pharmacokinetic properties and demonstrates potent antitumor efficacy in vivo. ITRI-90 can be used for prostate cancer research.
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DC80868 ISR activator 3
ISR activator 3 (Compound cc81) is the active metabolite of A8. ISR activator 3 activates the integrated stress response (ISR) by binding to RIG-I (KD ≈ 0.55 μM), without inducing lipid droplet clearance. ISR activator 3 enhances the interferon response under viral mimicry signals. ISR activator 3 can be used for research on neurodegenerative diseases and immune stress.
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DC80867 Isofusidienol A
Isofusidienol A (Compound 26) is a chromone compound. Isofusidienol A can be isolated from Artemisia vulgaris. Isofusidienol A has significant antibacterial activity against Bacillus subtilis. Isofusidienol A also has potent antifungal activity against Candida albicans. Isofusidienol A can be used for bacterial and fungal infections research.
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DC80865 IRBM-Z-2
IRBM-Z-2 is a non-competitive, orally active Zika virus (ZIKV) NS2B-NS3 protease inhibitor, with IC50 values of 0.04 μM and 3.1 μM against the wild-type and I156T mutant strains, respectively. IRBM-Z-2 exhibits broad-spectrum anti-flavivirus potential, with IC50 values of 2.1 μM and 0.09 μM against the NS2B-NS3 proteases of dengue virus 2 (DENV2) and West Nile virus (WNV), respectively. IRBM-Z-1 inhibits ZIKV replication and alleviates virus-induced cytopathic effects. IRBM-Z-1 can be used in studies related to ZIKV infection.
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DC80863 Iptacopan hydrochloride hydrate
Iptacopan (LNP023) hydrochloride hydrate is an effective and orally-active highly selective factor B inhibitor with an IC50 value of 10 nM and KD of 7.9 nM. Iptacopan hydrochloride hydrate exerts a proximal effect in the complement cascade reaction, preventing the destruction (hemolysis) of red blood cells in PNH and the damage of renal cells in IgAN and C3G. Iptacopan hydrochloride hydrate can be used for the study of complement-mediated diseases, particularly paroxysmal nocturnal hemoglobinuria (PNH), primary immunoglobulin A nephropathy (IgAN), and complement 3 glomerulopathy (C3G).
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DC80862 Iprazochrome
Iprazochrome is a serotonin antagonist. Iprazochrome can be used in prophylaxis of migraine.
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DC80859 Inolitazone hydrochloride hydrate
Inolitazone hydrochloride hydrate (Efatutazone hydrochloride hydrate) is a novel PPARγ high-affinity agonist, with an EC50 value one-fiftieth that of Rosiglitazone, and shows no inhibitory effect on RIE cells that do not express PPARγ. Inolitazone hydrochloride hydrate can be used in the research of cancer.
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DC80858 Influenza virus-IN-10
Influenza virus-IN-10 is a dual-target antiviral agents for influenza that targets both PAC (KD = 8.9 μM) and NP (KD = 52.5 μM) simultaneously. Influenza virus-IN-10 exhibits an EC50 values of 1.64 μM) against influenza A virus (H1N1, A/WSN/33) and broad-spectrum activity against other influenza strains, including influenza B virus and multiple subtypes of influenza A.
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DC80857 Influenza A virus-IN-19
Influenza A virus-IN-19 (Compound (S)-63) is an orally active, selective Influenza A virus inhibitor with an EC50 of 0.44 μM. Influenza A virus-IN-19 exhibits moderate binding affinity to Hemagglutinin, with a Kd of 5.66 μM. Influenza A virus-IN-19 inhibits trypsin-mediated cleavage of HA0, blocks the early viral entry process, and suppresses the replication of Influenza A virus. Influenza A virus-IN-19 improves the survival rate of mice in lethal influenza models. Influenza A virus-IN-19 can be used in studies related to Influenza A virus infection.
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DC80856 Influenza A virus-IN-17
Influenza A virus-IN-17 (Compound 6a) is a potent influenza A inhibitor with EC90s of 3.5 μM and 2.6 μM for H3N2 and H1N1, respectively. Influenza A virus-IN-17 inhibits U2-PB2 chimeric mRNA (EC90 = 2.1 μM from cap snatching polymerase).
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DC80855 IND8
IND8 is a α7 nAChR activator and cognitive enhancer. IND8 mediates cognitive enhancement by activating α7 nAChR . IND8 improves spatial working memory, episodic short-term memory and spatial long-term memory in amnesic mice induced by Scopolamine. IND8 improves memory function in mice with delayed natural memory decline. IND8 can be used in research related to Alzheimer's disease.
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DC80854 INCB059872 TFA
INCB059872 TFA is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 TFA can be used for the research of myeloid leukemia.
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DC80852 Immunosuppressant-2
Immunosuppressant-2 (Example 21) is an orally active immunosuppressant. Immunosuppressant-2 significantly reduces the number of circulating lymphocytes. Immunosuppressant-2 can be used for research on various autoimmune diseases and organ transplant rejection.
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DC80850 Imidazole-4-pyruvic acid
Imidazole-4-pyruvic acid is derived from histidine catalyzed by histidine transaminase. Imidazole-4-pyruvic acid can be used as a precursor for selective His-labeling in E.coli overexpressed proteins.
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DC80849 IL-17-IN-7
IL-17-IN-7 (Compound 23) is a IL-17 inhibitor with a pIC50 of 7.1 against IL-17A.
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DC80848 IL-17-IN-6
IL-17-IN-6 is a IL-17 inhibitor with a pIC50 of 7.6 against human targets. IL-17-IN-6 binds to IL-17A and blocks downstream pro-inflammatory signaling pathways. IL-17-IN-6 inhibits the release of IL-6 from normal human skin fibroblasts stimulated by IL-17A and TNF. IL-17-IN-6 can be used for research on inflammatory and autoimmune diseases.
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DC80845 IKZF2-degrader 3
IKZF2-degrader 3 (compound 6) is a molecular glue IKZF2 degrader with a DC50 of 2.0 nM.
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