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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC77540 KAC-50.1
KAC-50.1 is an α-Synuclein (α-syn) PET ligand, with a KD of 35 nM toward site 2 in recombinant α-syn fibrils.
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DC77539 JNJ19567470
JNJ19567470 (R317573) is a selective, non-peptidergic CRF type 1 receptor (CRF1) antagonist. JNJ19567470 blocks NaLac-induced panic-like behaviour and cardiovascular responses. JNJ19567470 decreases regional glucose utilization in the amygdala, and attenuates anxiety responses.
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DC77538 iZMYND8-34
iZMYND8-34 is a histone reader ZMYND8 inhibitor that inhibits ZMYND8's histone recognition. iZMYND8-34 can be used for the research of neuroendocrine prostate cancer.
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DC77537 Itaconic acid prodrug-1
Itaconic acid prodrug-1 (Compound P2) is an orally active prodrug of Itaconic acid that efficiently delivers the active ingredient Itaconic acid to skin tissue following oral administration. Itaconic acid prodrug-1 possesses immunomodulatory properties, significantly inhibiting Poly(I:C)/IFNγ-induced inflammatory cytokines in human epidermal keratinocytes. Itaconic acid prodrug-1 can be utilized for the research of alopecia areata and other inflammatory skin diseases.
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DC77536 iso-WAY-260022
iso-WAY-260022 (Compound 13R) is an orally active, brain-penetrant and selective norepinephrine transporter (hNET) inhibitor with an IC50 value of 140 nM. iso-WAY-260022 also shows inhibitory effects on human serotonin (hSERT) and dopamine transporters (hDAT). iso-WAY-260022 inhibits norepinephrine reuptake and increases hypothalamic norepinephrine levels to regulate thermoregulatory center function. iso-WAY-260022 is promising for research of vasomotor symptoms, such as menopausal hot flushes, night sweats.
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DC77535 Indomethacin N-octyl amide
Indomethacin N-octyl amide (Compound 2) is a potent and selective COX-2 inhibitor with an IC50 of 40 nM. Indomethacin N-octyl amide shows >1000-fold selectivity against COX-1 (IC50 of 66 µM).
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DC77534 Ifebemtinib hydrochloride
Ifebemtinib (BI-853520) hydrochloride is an orally active and potent focal adhesion kinase (FAK) inhibitor (IC50 = 1 nM for recombinant FAK). Ifebemtinib hydrochloride exhibits antiproliferative activity against cancer cells.
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DC77533 ICD inducer-1
ICD inducer-1 (Compound Re1) is an effective immunogenic cell death (ICD) inducer that can target the endoplasmic reticulum (ER) and block ER-phagy at the late stages. ICD inducer-1 is promising for research of cancers.
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DC77532 Hydroxytyrosol 1-O-glucoside
Hydroxytyrosol 1-O-glucoside (Dopaol glucoside) is a glycoside with antioxidant activity. Hydroxytyrosol 1-O-glucoside is also an epoxide hydrolase 2 inhibitor.
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DC77531 HW161023
HW161023 (compound 5) is an orally active AP2-associated protein kinase 1 (AAK1) inhibitor with IC50 values of 5.4 nM and 11.9 μM aganist of AAK1and hERG, respectively. HW161023 inhibits the pain in chronic constriction injury of the sciatic nerve rat model.
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DC77530 HUP-55
HUP-55 is a prolyl endopeptidase inhibitor (IC50 = 5 nM). HUP-55 reduces the dimerization of α-synuclein in Neuro2a cells and induces autophagy (Autophagy) in HEK293 cells. It also decreases the increase in reactive oxygen species (ROS) production induced by hydrogen peroxide in SH-SY5Y cells at a concentration of 10 μM. In a mouse Parkinson’s disease model, HUP-55 (10 mg/kg) improves motor function (reduces the use frequency of the impaired paw) and decreases the levels of harmful oligomers of α-synuclein in the striatum caused by overexpression of α-synuclein.
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DC77529 HQY1428
HQY1428 is an orally active CDK12 inhibitor. HQY1428 inhibits DNA replication, causes G2/M arrest in SKOV3 cells, induces DNA double-strand breaks and apoptosis. HQY1428 has anti-tumor activity in the SKOV3 xenograft mouse model. HQY1428 combined with the HER2 inhibitor Lapatinib, is a neuraminidase (NA) of influenza virus inhibitor. ent-Oseltamivir is promising for research of influenza virus infections.
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DC77528 H-Gly-Pro-Hyp-OH acetate
H-Gly-Pro-Hyp-OH acetate is a dipeptidyl peptidase 4 (DPP-4) inhibitor with an IC50 value of 2.51 mM. H-Gly-Pro-Hyp-OH acetate is promising for research of diabetes.
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DC77527 Hexamidine diisethionate
Hexamidine diisethionate is an antimicrobial agent targeting Acanthamoeba protozoa. Hexamidine diisethionate is promising for research of ocular infectious diseases such as Acanthamoeba keratitis.
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DC77526 Herbicide safener-4
Herbicide safener-4 (Compound I-15) is a Herbicide safener, improving the herbicide resistance of crops without reducing the herbicidal effect on targeted weed species. Herbicide safener-4 competitively binds to the ALS active site with Mesosulfuron-methyl. Herbicide safener-4 enhances GSH, GST, CYP450, POD, SOD and ALS activity in plants.
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DC77525 Hellebrin
Hellebrin is a bufadienolide compound extracted from plants that can inhibit tumor cell growth. Hellebrigenin shows potential in overcoming cancer cells' resistance to apoptosis stimuli and has also demonstrated anti-proliferation effects in multidrug-resistant (MDR) cancer cell models. Hellebrin can act on Na+/K+-ATPase to regulate intracellular signaling pathways.
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DC77524 Hedgehog IN-9
Hedgehog IN-9 (compound 1) is a Hedgehog inhibitor. Hedgehog IN-9 prevents GLI1 expression and enhances cellular BRD2 protein levels. Hedgehog IN-9 inhibits growth of medulloblastoma spheroid cells and can be used for synthesis of photoaffinity labeling probe.
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DC77523 HCTZ-CH2-HCTZ
HCTZ-CH2-HCTZ is an isomer of HCTZ. Hydrochlorothiazide (HCTZ), an orally active diuretic agent of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway.
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DC77522 H117
H117 is a PROTAC target protein ligand that can be used to synthesize PROTAC HP211206-induced apoptosis. LPT99 can effectively mitigate cisplatin-induced hearing loss in rats.
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DC77521 Gumelutamide monosuccinate
Gumelutamide (monosuccinate) is a tetrahydropyridopyrimidine compound, acting as an antiandrogen, antineoplastic agent. Gumelutamide (monosuccinate) is an androgen antagonist.
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DC77520 GSK3368715 hydrochloride
GSK3368715 (EPZ019997) hydrochloride is an orally active, reversible, SAM-noncompetitive type I protein arginine methyltransferase (PRMT) inhibitor with IC50 values of 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), and 1.7 nM (PRMT8). GSK3368715 hydrochloride induces a shift in arginine methylation states, alters exon usage, and exhibits potent anticancer activity.
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DC77519 GRL093-22
GRL093-22 is a potent and selective G protein-coupled receptor kinase (GRK) inhibitor, with IC50s of 60 and 40 nM for GRK5 and GRK6, respectively. GRL093-22 has the potential for the research of heart failure and multiple myeloma.
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DC77518 GPV0057
GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel Kir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of Kir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, Kir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome.
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DC77517 GM1489
GM1489 is an MMP inhibitor that reduces degradation at the resin-dentin interface by inhibiting MMP activity, thereby enhancing bonding stability. GM1489 shows potential for researching strategies to improve bonding stability in both superficial and deep dentin.
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DC77516 Glycyl-L-Proline TFA
Glycyl-L-Proline TFA (H-Gly-Pro-OH TFA) is a dipeptide, which is composed of a glycine and a L-proline. Glycyl-L-Proline TFA can be used in research about the co-relationship between transmembrane potential/proton gradient and intestinal transport.
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DC77515 Glycerophosphorylethanolamine sodium
Glycerophosphorylethanolamine (GroPEtn) sodium is an active phosphodiester metabolite of Phosphatidylethanolamine. Glycerophosphorylethanolamine sodium promotes the aggregation of amyloid β-protein (Aβ (1-4
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DC77514 GI-Y2
GI-Y2 is an inhibitor of GSDMD and can inhibit Pyroptosis of macrophages induced by oxidized low-density lipoprotein (ox-LDL). In vivo, GI-Y2 can dose-dependently reduce atherosclerotic plaques in ApoE-/- mice and decrease the lesion size and fibrosis degree of the aortic root. GI-Y2 is expected to be used in the research of pyroptosis and cardiovascular diseases, such as atherosclerosis.
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DC77513 Gilvocarcin M
Gilvocarcin M is an antibiotic and can be isolated from S. gilvotanareus. Gilvocarcin M is active against S. aureus at a concentration of 32 µg/ml and inhibits growth of KB cells with the IC50 of 0.52 µg/ml. Gilvocarcin M intercalates into bacteriophage PM2 DNA.
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DC77512 Gigantetrocin
Gigantetrocin is a bioactive annonacetyl coenzyme from goniothalamus giganteus.
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DC77511 Gibberellenic acid
Gibberellenic acid is an intermediate gibberellin compound with a tetracyclic diterpenoid skeleton, and can be generated by thermal decomposition of Gibberellic acid in aqueous solution. Gibberellenic acid is thermally unstable in water and can further convert into allogibberic acid (approximately 80%) and 9-epiallogibberic acid (approximately 10%). It plays an important role in the degradation pathway and structural elucidation of Gibberellins.
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