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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC78593 BJH-86
BJH-86 is a soluble mitochondrial complex 1 inhibitor (oxygen consumption rate inhibition IC50 = 5 μM). BJH-86 exhibits weak inhibitory activity against phosphodiesterase 10A (PDE10A) (IC50 >10 μM). BJH-86 can reduce cellular oxygen consumption and inhibit cancer cell proliferation. BJH-86 can be used for the research of cancer, such as lung cancer.
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DC78592 ZINC13000658
ZINC13000658 is a METTL inhibitor. ZINC13000658 exhibits significant anti proliferative activity in various cells and can induce G1 phase cell cycle arrest and apoptosis such as HepG2 (IC50 = 5.632 µM) and SNU-449 (IC50 = 6.184 µM) cells. ZINC13000658 may be related to the inhibition of the activity of multiple methyltransferases such as METTL1, 3, 6, 16, 18, etc. ZINC13000658 can be used for research on various types of cancer.
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DC78591 TPAPyN
TPAPyN is a nitroreductase(NTR)-responsive type I photosensitizer. TPAPyN facilitates the imaging of hypoxic cancer cells and image-guided photodynamic therapy (PDT). TPAPyN does not emit fluorescence in the aqueous environment, but restores when NTR cleaves the nitrofuran quencher with aggregation-induced emission. TPAPyN can be used as a fluorescent probe for specific imaging of hypoxic cancer.
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DC78590 CIMBA hydrochloride
CIMBA hydrochloride is a selective G protein-coupled estrogen receptor (GPER) antagonist. CIMBA hydrochloride is used in the research of cholesterol gallstones in women.
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DC78589 SKF-96365
SKF-96365 is a blocker of calcium store-operated calcium influx (SOCE) and transient receptor potential channels (TRPC). SKF-96365 reduces the increase in intracellular calcium concentration by blocking TRPC channels and SOCE. SKF-96365 enhances the reverse operation of Na⁺/Ca²⁺ exchanger (NCX) (Ca²⁺ influx) in glioblastoma, leading to intracellular calcium overload and cytotoxicity. SKF-96365 inhibits the CaMKIIγ/AKT pathway and simultaneously induces apoptosis and cell protective autophagy in colorectal cancer cells. SKF-96365 can be used in calcium signaling and cancer research.
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DC78588 UK-78282
UK-78282 is a selective Kv1.3 voltage-gated potassium channel inhibitor with an IC50 of 200 nM. UK-78282 also inhibit Kv1.4 potassium channel. UK-78282 can inhibit human T cell activation.
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DC78587 FHND5071 (1H)
FHND5071 (1H) is a selective inhibitor targeting the RET (rearrangement during transfection) tyrosine kinase. FHND5071 (1H) is promising for research of RET-driven cancers (such as thyroid cancer, lung cancer, etc.).
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DC78586 DDR1 ligand 1-piperidine
DDR1 ligand 1-piperidine is a target protein ligand and linker conjugate, which can be used for the synthesis of PROTAC DDR1 degrader-1.
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DC78584 GRL-07524
GRL-07524 (Compound 4e) is a potent inhibitor of HIV-1 protease (Ki = 0.22 nM). GRL-07524 contains oxaspirocyclic carbamates as the P2 ligands. GRL-07524 exhibits good antiviral activity with an EC50 = 210 nM. GRL-07524 binds to the HIV-1 PR active site in one of the four symmetry independent molecules along with key catalytic residues.
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DC78583 CD-10
CD-10 is an orally active and BBB-penatrable Keap1-Nrf2 protein-protein interaction (PPI) inhibitor. CD-10 binds to Keap1 with a KD value of 193 nM. CD-10 exhibits potent anti-oxidative and anti-inflammatory effects through Keap1-Nrf2 pathway activation, evidenced by reduced levels of MDA, IL-4, IL-10 and increased expression of HO-1. CD-10 effectively alleviated anxiety and depressive behaviors and restored serum neurotransmitter levels by promoting Nrf2 nuclear translocation in the chronic unpredictable mild stress (CUMS) mouse model. CD-10 can be used for the study of depression.
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DC78582 Z55660043
Z55660043 is a Regulator of G protein signaling-14 (RGS14) inhibitor with an IC50 of 2.3  μM. Z55660043 selectively and non-covalently inhibits RGS14 GTPase-accelerating protein (GAP) activity without measurable cytotoxicity. Z55660043 can be used for central nervous system and metabolic disorders research.
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DC78581 KI-DX-014
KI-DX-014 is a DDX21 inhibitor with an IC50 of 3.31  μM. KI-DX-014 significantly inhibits the DDX21-RNA interaction and modulates ATPase activity and biomolecular condensate formation. KI-DX-014 reduces the DDX21-dependent release of P-TEFb from the 7SK snRNP complex, inhibits P-TEFb-dependent phosphorylation of the RNA polymerase II CTD, and induces developmental defects in zebrafish embryos. KI-DX-014 can be used for cancers and neurodegenerative disorders research.
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DC78580 VU6080824 hydrochloride
VU6080824 (hydrochloride), a derivative of ML-133), is an inward-rectifier potassium channel (Kir2.1) inhibitor with an IC50 of 0.35  μM. VU6080824 (hydrochloride) has superior thallium flux and manual patch clamp (MPC) functional potency.
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DC78579 VU6080824
VU6080824 (Compound 5s), a derivative of ML-133), is an inward-rectifier potassium channel (Kir2.1) inhibitor with an IC50 of 0.35  μM. VU6080824 has superior thallium flux and manual patch clamp (MPC) functional potency.
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DC78578 SVC112
SVC112 is a translation elongation inhibitor that prevents the cyclic dissociation of EF2 from the ribosome, thereby inhibiting the elongation step of translation. SVC112 shows activity in growth inhibition among cancer cell lines of various origins (acute myeloid leukemia (AML), multiple myeloma (Myeloma), colorectal cancer (CRC), and head and neck squamous cell carcinoma (HNSCC)). SVC112 preferentially impedes ribosomal processing of mRNAs, and decreaseds CSC-related proteins including Myc and Sox2. SVC112 induces apoptosis in hematologic cancer cell lines, while phosphorylation of c-Myc correlates with sensitivity to SVC112 in colorectal cancer cell lines. SVC112 inactivates HNSCC stem cells in vitro and prevents the regrowth of HNSCC tumor xenografts in mice. SVC112 can be used for the study of HNSCC.
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DC78577 MG-Lin3
Lin28 degrader MG-Lin3 is a molecular glucose degrading agent that targets the Lin28 protein. Lin28 degrader MG-Lin3 significantly reduces the Renilla luciferase signal at 100 µM. Lin28 degrader MG-Lin3 inhibits the maturation of tumor microRNA let-7. Lin28 degrader MG-Lin3 can be used for cancer research.
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DC78576 5-HT2AR ligand 1
5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT2AR ligand with nanomolar affinity for 5-HT2AR (Ki: 32 nM). 5-HT2AR ligand 1 is capable of inducing β-arrestin 2 recruitment. 5-HT2AR ligand 1 can be used in the research of neurological diseases.
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DC78575 DJ-89
DJ-89 (Compound 77) is a potent soluble epoxide hydrolase (sEH) inhibitor with an IC50 value of 0.51 nM . DJ-89 inhibits sEH from hydrolyzing epoxyeicosatrienoic acids (EETs), reducing the production of pro-inflammatory substances. DJ-89 is promising for research of acute and chronic inflammatory diseases (such as rheumatoid arthritis).
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DC78568 β-Blocker B-24/76
β-Blocker B-24/76 is a beta adrenoceptor blocker. β-Blocker B-24/76 exhibits beta 1-adrenoceptor blocking and beta 2-adrenoceptor stimulating properties. β-Blocker B-24/76 can suppress the increased ornithine decarboxylase activity in hypertrophied hearts. β-Blocker B-24/76 can be used for the research of cardiovascular disease.
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DC78567 Metralindole
Metralindole is an inhibitor of human cyclin-dependent kinase CDK2 and human protein kinase CK2 holoenzyme. Metralindole shows good potential as a non-small cell lung cancer inhibitor.
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DC78566 (Z)-1,2-Dimethoxy-4-(3-fluoro-2-propenyl)benzene
(Z)-1,2-Dimethoxy-4-(3-fluoro-2-propenyl)benzene is a fluorine analog of Methyl eugenol (ME) and is attractive to oriental fruit fly B. dorsalis.
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DC78565 SCH-1518291
SCH-1518291 (Compound 27) is an orally active PDE10A inhibitor. SCH-1518291 exhibits antipsychotic activity in an ADHD rat model. SCH-1518291 can be used in research on neurological disorders such as psychosis.
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DC78564 BRP-821
BRP-821 is a soluble epoxide hydrolase (sEH) inhibitor with an IC50 of 0.4 nM. BRP-821 can be used for the researches of inflammation, cardiovascular, metabolic and neurological disease .
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DC78563 PGE 9262932
PGE 9262932 is a quinolone antibacterial agent. PGE 9262932 can be used for the research of infection.
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DC78562 WCK-1152
WCK-1152 is a fluoroquinolone antibacterial agent. WCK-1152 is active against resistant pathogens bearing mutations of DNA gyrase and/or topoisomerase IV which also express efflux pumps. WCK-1152 can be used for the research of infection, such as respiratory infections caused by resistant pneumococci and staphylococci.
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DC78561 DC-756
DC-756 is a fluoroquinolone antibiotic. DC-756 possesses potent activity against Gram-positive and Gram-negative pathogens comparable to Trovafloxacin, with MIC, against Ofloxacin-resistant strains 16-fold better than Trovafloxacin. DC-756 is well absorbed orally in rats and found to have good photostability. DC-756 can be used to study bacterial resistance.
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DC78560 Dopamine D3 receptor ligand-6
Dopamine D3 receptor ligand-6 (Compound 196476) is a selective dopamine D3 receptor (D3) antagonist. Dopamine D3 receptor ligand-6 is promising for research of substance use disorders (such as opioid and psychostimulant addiction).
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DC78558 4'-Acetyl-chrysomycin A
4'-Acetyl-chrysomycin A is an analog of chrysomycin A. 4'-Acetyl-chrysomycin A has antibacterial activity.
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DC78557 L-759656
L-759656 is a selective cannabinoid CB2 receptor agonist, with the Ki of 11.8 nM for the human CB2 receptor. L-759656 potently inhibits Forskolin-stimulated cyclic AMP production in Chinese Hamster Ovary (CHO) cells, with an EC50 of 3.1 nM. L-759656 can be used for the study of immune-related diseases and inflammatory diseases.
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DC78556 (±)-WB 4101
(±)-WB 4101 is a highly selective α1-adrenergic receptor antagonist. (±)-WB 4101 blocks norepinephrine-induced vascular smooth muscle contraction to exert antihypertensive and benign prostatic hyperplasia (BPH)-relieving effects. (±)-WB 4101 is promising for research of hypertension and BPH.
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