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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC81712 USP1-IN-14
USP1-IN-14 (compound 27) is a ubiquitin-specific protease 1 (USP1) inhibitor with an IC50 of 0.001 µM. USP1-IN-14 can be used for USP1-related cancers, autoimmune and inflammatory disorders research.
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DC81711 Usistapide
Usistapide (JNJ-16269110) is a microsomal triglyceride transfer protein (MTP) inhibitor. Usistapide is promising for research of obesity.
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DC81708 UDP-α-sulfoquinovose
UDP-α-sulfoquinovose is a nucleoside metabolite.
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DC81707 UDP-N-acetylmuramoyl-L-alanyl-D-glutamyl-6-carboxy-L-lysyl-D-alanyl-D-alanine
UDP-N-acetylmuramoyl-L-alanyl-D-glutamyl-6-carboxy-L-lysyl-D-alanyl-D-alanine is a nucleoside metabolite.
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DC81706 UDP-Mannose
UDP-Mannose exists in mouse brain, especially hypothalamus and neocortex at a higher concentration compared to other organs. UDP-Mannose regulates glycosylation, in particular mannosylation in specific organs or conditions. UDP-Mannose can be used as a substrate for structural study of glycosyltransferase.
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DC81705 UDP-2-alkyne-GlcNAc
UDP-2-alkyne-GlcNAc (Compound 3) is a UDP-GlcNAc derivative. UDP-2-alkyne-GlcNAc can be used for the remodeling of cell surface glycans.
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DC81704 UCM-A86
UCM-A86 is a selective positive allosteric modulator of GluN1/GluN3 NMDA receptors with EC50 values of 21 µM and 19 µM at GluN1/GluN3A and GluN1/GluN3B receptors, respectively. UCM-A86 selectively potentiates responses from GluN1/GluN3A/B over GluN1/GluN2A-D receptors. UCM-A86 can be used in the research of central nervous system diseases.
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DC81703 UAWJ-247
UAWJ-247 is a potent and reversible SARS-CoV-2 main protease (Mpro) inhibitor with an IC50 of 0.042 μM and a Ki of 0.035 μM. UAWJ-247 can be used for the research of covid-19.
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DC81702 UAB116
UAB116 is a Liver X Receptor (LXR)/Retinoid X Receptor (RXR) agonist. UAB116 can decreases metastatic phenotype in hepatoblastoma by inhibiting the Wnt/β-Catenin pathway via upregulation of TRIM29. UAB116 can reduce proliferation, stemness and invasiveness of metastatic hepatoblastoma cells.
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DC81701 UA2239
UA2239 is an antimalarial agent and acyclic nucleoside phosphonate. UA2239 disrupts the essential cGMP-dependent egress pathway by decreasing cGMP levels. UA2239 targets guanylyl cyclase α. UA2239 demonstrates rapid and irreversible inhibitory effects on Plasmodium parasites.
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DC81699 U 88204
U 88204 is a potent HIV-1 reverse transcriptase (RT) inhibitor with an IC50 of 0.25 μM. U 88204 blocks HIV-1 replication in infected cells. U 88204 can be used for the research on HIV-infection and of acquired immunodeficiency syndrome (AIDs).
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DC81698 Tyrosine kinase-IN-11
Tyrosine kinase-IN-11 (Compound 4b) is a tyrosine kinase inhibitor. Tyrosine kinase-IN-11 decreases general tyrosine kinase activity, selectively inhibits PDGFR-β, SRC, and c-MET kinases. Tyrosine kinase-IN-11 induces apoptosis, accompanied by reduced ERK signalings. Tyrosine kinase-IN-11 exhibits selective anticancer activity against pancreatic cancer and renal cancer.
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DC81697 Tyrosinase-IN-50
Tyrosinase-IN-50 (Compound 14) is a Tyrosinase inhibitor (with a Tyrosinase IC50 of 0.06 μM in MNT-1 cells and a Tyrosinase IC50 of 0.16 μM in B16-F10 cells). Tyrosinase-IN-50 inhibits melanogenesis in multiple cell types. Tyrosinase-IN-50 can be used for the research of hyperpigmentation-related diseases.
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DC81696 Tyk2-IN-23
Tyk2-IN-23 is a potent, orally active, selective TYK2 inhibitor (IC50 = 18 nM), exhibiting more than > 70-fold selectivity over JAK1/2/3 isoforms. Tyk2-IN-23 potently inhibits p-STAT3 in TYK2-dependent signaling activated by IFN-α and IL-10. Tyk2-IN-23 potently inhibits IFN-α-induced STAT1 phosphorylation in H9 cells. Tyk2-IN-23 can be used for the study of alopecia areata and allergic Rhinitis.
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DC81695 Tubulin-IN-66
Tubulin-IN-66 is a tubulin (tubulin) and P-gp inhibitor with antiproliferative activity against cancer cells. Tubulin-IN-66 covalently binds to the Colchicine-binding site at Cys239 of the β-tubulin subunit, inhibits tubulin polymerization and disrupts the microtubule network. Tubulin-IN-66 inhibits P-gp function to overcome multidrug resistance. Tubulin-IN-66 arrests the cell cycle at the G2/M phase and induces apoptosis (apoptosis). Tubulin-IN-66 inhibits colony formation and migration of cancer cells. Tubulin-IN-66 can be used in the research of tumors such as breast cancer.
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DC81694 Tubulin-IN-65
Tubulin-IN-65 (Compound Imp-18) is a Tubulin inhibitor. Tubulin-IN-65 exhibits tubulin-disrupting activity. Tubulin-IN-65 disrupts microtubule integrity. Tubulin-IN-65 induces Apoptosis and increases the expression of CDK1 and Cyclin B1. Tubulin-IN-65 possesses anticancer activity against breast cancer and colorectal cancer. Tubulin-IN-65 can be used in research related to triple-negative breast cancer and colorectal adenocarcinoma.
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DC81693 Tubulin/VEGFR-2-IN-2
Tubulin/VEGFR-2-IN-2 is an orally active tubulin and VEGFR-2 inhibitor with IC50s of 3.27 and 0.09 μM, respectively. Tubulin/VEGFR-2-IN-2 exerts the antitumor effects through multifaceted pathways, including enhancing reactive oxygen species (ROS) generation, disrupting mitochondrial membrane potential, inducing apoptosis, and arresting the cell cycle. Tubulin/VEGFR-2-IN-2 demonstrates anti-angiogenic properties by significantly impairing endothelial cell migration, invasion, and tube formation in vitro. Tubulin/VEGFR-2-IN-2 suppresses angiogenesis, tumor growth, and metastasis in vivo. Tubulin/VEGFR-2-IN-2 can be used for non-small lung cancer, breast cancer, gastric cancer and lymphoma.
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DC81692 Tubulin polymerization-IN-90
Tubulin polymerization-IN-90 is a tubulin polymerization inhibitor. Tubulin polymerization-IN-90 disrupts tubulin polymerization by binding to the nocodazole-binding site on β-tubulin. Tubulin polymerization-IN-90 induces the release of extracellular vesicles marked by the tetraspanin CD63. Tubulin polymerization-IN-90 induces the release of IL-8 from cells. Tubulin polymerization-IN-90 reduces the viability of cancer cells. Tubulin polymerization-IN-90 can be used in the research of cancers such as acute T-lymphoblastic leukemia.
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DC81688 TTP-6171
TTP-6171 is a non-covalent inhibitor of Monkeypox virus I7L protease, and it can be used for research on poxvirus infections.
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DC81687 TTBK1-IN-5
TTBK1-IN-5 (Compound 32) is a potent TTBK1 inhibitor with an IC₅₀ of 239 nM. TTBK1-IN-5 can be used for research on Alzheimer's disease.
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DC81686 TTBK1-IN-3
TTBK1-IN-3 (Compound 18) is a potent inhibitor of TTBK1, with a biochemical IC₅₀ of 18 nM and a cellular IC₅₀ of 259 nM. TTBK1-IN-3 can be used for research on Alzheimer's disease.
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DC81684 TSI-13-57
TSI-13-57 is a pan-TLR inhibitor (IC50: 2.7 μM, 6.03 μM, 7.37 μM, 6.38 μM for TLR9, TLR7, TLR2, TLR4, respectively). TSI-13-57 inhibits homodimerization of the TIR domains of MyD88. TSI-13-57 reduces systemic inflammatory responses in LPS-induced mice.
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DC81683 TSHR modulator-1
TSHR modulator-1 is a TSHR modulator.
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DC81681 TrxR-IN-9
TrxR-IN-9 is a thioredoxin reductase (TrxR) inhibitor with an IC50 of 0.26 μM. TrxR-IN-9 disrupts cellular redox balance. TrxR-IN-9 induces S-phase cell cycle arrest, promotes apoptosis and exhibits antiproliferative activity across cancer cells. TrxR-IN-9 exerts effects via synergistic nitric oxide (NO) and reactive oxygen species (ROS) action. TrxR-IN-9 can be used for the research of breast cancer, gastric cancer, colorectal cancer, liver cancer.
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DC81680 TrxR2-IN-1
TrxR2-IN-1 is a thioredoxin reductase 2 (TrxR2) inhibitor with an IC50 value of 0.83 μM. TrxR2-IN-1 accumulates in mitochondria, impairs mitochondrial function and membrane potential, increases reactive oxygen species (ROS) levels, activates ASK1-mediated caspase-dependent apoptosis (apoptosis), induces G2/M cell cycle arrest, and inhibits cancer cell migration. TrxR2-IN-1 can be used in the research of hepatocellular carcinoma.
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DC81679 TRPV4/TRPA1-IN-1
TRPV4/TRPA1-IN-1 is a TRPV4/TRPA1 inhibitor that suppresses TRPV4/TRPA1-mediated calcium influx. TRPV4/TRPA1-IN-1 alleviates pain behaviors in a mouse trigeminal stimulation pain model and inhibits inflammation and pain-related behaviors in a mouse acute pancreatitis model. TRPV4/TRPA1-IN-1 can be used in research on acute pancreatitis.
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DC81677 TRPM5 agonist-1
TRPM5 agonist-1 is an orally active TRPM5 agonist with a pEC50 of 8.1. TRPM5 agonist-1 shows excellent selectivity (> 100-fold) versus related cation channels (TRPM8, TRPV1, TRPV4, TRPA1, TRPM4). TRPM5 agonist-1 exhibits locally acting stimulatory effect on gastrointestinal transit in mice. TRPM5 agonist-1 can be used for research on promoting gastric motility.
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DC81676 TRPA1 agonist-3
TRPA1 agonist-3 is a selective and orally active TRPA1 agonist, with EC50 values of 50.05 μM and 314.04 μM for human and mouse TRPA1, respectively. TRPA1 agonist-3 does not activate hTRPV1, mTRPV2, hTRPV3, hTRPV4, hTRPC6, or hTRPM8 channels. TRPA1 agonist-3 alleviates inflammatory pain in mice through a channel desensitization mechanism.
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DC81675 Triptolide-6-succinate-β-D-glucose
Triptolide-6-succinate-β-D-glucose (Compound 2) is a glucose-conjugated derivative of Triptolide. Triptolide-6-succinate-β-D-glucose is a tumor-selective prodrug targeting glucose transporters ( GLUT). Triptolide-6-succinate-β-D-glucose can induce the degradation of the RPB subunit of RNA polymerase II. Triptolide-6-succinate-β-D-glucose inhibits the proliferation of HEK293T cells with an IC50 value of 268 nM. Triptolide-6-succinate-β-D-glucose can be used for the research of cancer, such as prostatic cancer.
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DC81674 Trioxacarcin B
Trioxacarcin B (TXN-B) is a potent cytotoxic agent and DNA-targeted inhibitor. Trioxacarcin B disrupts DNA function and induces apoptosis in cancer cells. Trioxacarcin B not only effectively inhibits the growth of various Gram-positive and Gram-negative bacteria as well as Plasmodium falciparum, but also blocks the colony formation of cancer stem cells, significantly reduces tumor volume and prolongs survival in preclinical in vivo models. The activity of Trioxacarcin B is highly dependent on its intact spiro-epoxide structure; it loses efficacy once this moiety undergoes hydrolysis, and Trioxacarcin B shows no activity against fungi, microalgae and small RNA viruses. Trioxacarcin B can be used for research on bacterial infections, malaria, and various cancers including colon cancer and melanoma.
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