Search Result
Results for "
Toxicity Model
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-138171
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Lipid 5
1 Publications Verification
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Liposome
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Others
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Lipid 5 is an amino lipid that affords efficient mRNA delivery in rodent and primate models. Lipid 5 shows optimal pharmacokinetics and non-toxic side effects .
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- HY-W010041
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Amyloid-β
Endogenous Metabolite
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Neurological Disease
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Scyllo-Inositol, an amyloid inhibitor, potentialy inhibits α-synuclein aggregation. Scyllo-Inositol stabilizes a non-fibrillar non-toxic form of amyloid-β peptide (Aβ42) in vitro, reverses cognitive deficits, and reduces synaptic toxicity and lowers amyloid plaques in an Alzheimer's disease mouse model .
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- HY-W717530
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7-Isopropyl-1-methylphenanthrene
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Others
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Others
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Retene is widely present in modern and ancient sediments, and can be extracted from fir forest soils, humus coal, continental petroleum source rocks, and deep-sea sediments. Retene can be toxic when exposed to light, and this light-induced toxicity can have lethal and sublethal effects on aquatic organisms. Retene can be used as a model compound to study the interaction between environmental pollutants and ultraviolet rays .
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- HY-169832
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Drug Intermediate
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Others
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Sulfanegen is a 3-mercaptopyruvate prodrug and cyanide antidote. Sulfanegen converts toxic cyanide into a relatively non-toxic substance. Sulfanegen, alone or in combination with Cobinamide, has detoxification effect in mouse models of cyanide poisoning .
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- HY-170949
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STING
Interleukin Related
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Inflammation/Immunology
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STING-IN-11 (Compound 42) is an orally active STING inhibitor with an IC50 of 37.8 nM. STING-IN-11 can block the palmitoylation of the STING protein and STING downstream signaling, and inhibit STING-mediated inflammation. STING-IN-11 has good in vivo safety and can be used for the research of STING-related inflammatory and autoimmune diseases .
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- HY-120407
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ENT-33266
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Insecticide
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Others
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Looplure (ENT-33266) is an insect attractant with acute toxicity studies in different animal models showing activity at oral and dermal median lethal doses (LD50) and median lethal concentrations (LC50) for fish with some values, and low toxicity in most cases except for some cases.
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- HY-139716
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NF-κB
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Inflammation/Immunology
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IMD-catechol is a novel imidazoquinolinone-NF-κB immunomodulator dimer that improves efficacy in a CT26 mouse colon carcinoma tumor model while eliciting minimal adjuvant toxicity.
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- HY-119857
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SIRT2 Inhibitor,Inactive Control
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Sirtuin
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Neurological Disease
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AGK7 is a potent inhibitor of sirtuin 2 (SIRT2). AGK7 rescues alpha-synuclein toxicity and modified inclusion morphology in a cellular model of Parkinson's disease. AGK7 protects against dopaminergic cell death both in vitro and in a Drosophila model of Parkinson's disease .
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- HY-116945
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Endogenous Metabolite
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Others
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Diphenamid is a chemical compound that exhibits herbicide activity. Diphenamid acts by inhibiting the enzyme acetyl-CoA carboxylase. Diphenamid has shown resistance as a model for mimicking organic pollutants in wastewater treatment processes, especially in the presence of multiple anions. The degradation of diphenamid is significantly affected by certain inorganic ions, such as chromium (VI) and nitrogen oxides. Diphenamid shows changes in toxicity with longer treatment times, and the results of toxicity tests on selected algae indicate higher toxicity at 240 minutes of treatment .
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- HY-P3350
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Bacterial
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Infection
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LS-BF1 is a stable and low toxic cationic antimicrobial peptide. LS-BF1 displays broad spectrum of antibacterial activity, including the challenging ESKAPE pathogens, by cell membrane disruptive mechanism. LS-BF1 shows good in vivo efficacy for elimination of bacteria in a mouse infection model[1].
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- HY-164484
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Raf
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Cancer
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IHMT-RAF-128, a highly potent pan-RAF inhibitor. IHMT-RAF-128 shows potent antitumor efficacy in xenograft mouse tumor models without causing any apparent toxicities .
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- HY-129228
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Parasite
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Infection
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Lychnopholide is a sesquiterpene lactone derived from the Asteraceae, Lychnopholide exhibits anti-trypanosomal activity against Trypanosoma cruzi. lychnopholide encapsulated in nanocapsules reduces its toxicity to mammalian cells. Lychnopholide ameliorates Chagas disease in mouse models .
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- HY-145388
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PROTACs
Epigenetic Reader Domain
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Cancer
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AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .
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- HY-148948
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NAMPT
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Neurological Disease
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NAMPT activator-3, a NAT derivative, is a NAMPT activator with an EC50 of 2.6 μM and a KD of 132 nM. NAMPT activator-3 effectively protects cultured cells from FK866 (HY-50876)-mediated toxicity. NAMPT activator-3 exhibits strong neuroprotective efficacy in a chemotherapy-induced peripheral neuropathy (CIPN) mouse model without any overt toxicity .
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- HY-160680
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Androgen Receptor
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Endocrinology
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AR antagonist 6 (compound 6i) is a diphenyl ether androgen receptor (AR) antagonist that binds AR at a concentration of 120 nM. AR antagonist 6 exhibits low toxicity and in vitro activity against the golden Syrian hamster ear model .
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- HY-19590
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Ro 15-1570
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Drug Derivative
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Cancer
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Etarotene (Ro 15-1570) is a derivative of Arotinoid (HY-106735). Etarotene is an orally active antitumor agent against DMBA (HY-W011845)-induced mammary tumor and causes toxic symptoms of hypervitaminosis A in rat model .
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- HY-146114
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Microtubule/Tubulin
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Cancer
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Antitumor agent-67 (compound 3) is a potent antitumor agent. Antitumor agent-67 has highly selective toxicity to cancer cells and lower damage to normal cells. Antitumor agent-67 can be activated by NQO1 and effectively liberate podophyllotoxin and kill tumor cells. Antitumor agent-67 significantly suppresses cancer growth in HepG2 xenograft models without obvious toxicity .
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- HY-127165
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HP 029 free base; Hydroxytacrine
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Cholinesterase (ChE)
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Neurological Disease
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Velnacrine (HP 029 free base) is an inhibitor for acetylcholinesterase (AChE), with an IC50 of 3.27 μM. Velnacrine reverses the Scopolamine (HY-N0296)-induced amnesia in rat models, and exhibits acute toxicity with LD50 of 65 mg/kg .
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- HY-19225
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KA-672 hydrochloride; Anseculin hydrochloride
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iGluR
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Neurological Disease
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Ensaculin is an NMDA receptor channel blocker. Ensaculin has neuroprotective effects in NMDA toxicity models and promotes neuronal growth in primary cultures of rat brain cells. Ensaculin has the potential to be developed as an anti-dementia drug that acts on various neurotransmitter systems .
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- HY-112352
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Endogenous Metabolite
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Others
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SU9518 is a tyrosine kinase inhibitor with specific activity against PDGFRα. SU9518 can inhibit the development of proliferative vitreoretinopathy (PVR) in fibroblast and Muller cell rabbit models. SU9518 showed effective inhibitory effects in these models without toxic effects. Therefore, SU9518 has the potential to be used to inhibit PVR in humans and other proliferative eye diseases involving fibrosis and gliosis .
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- HY-111054A
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MDCG sodium
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Endogenous Metabolite
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Others
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N-methyl-N-dithiocarboxyglucamine (MDCG) sodium mobilizes and promotes excretion of metallothionein-bound 109Cd in mouse model. N-methyl-N-dithiocarboxyglucamine significantly lowers the Cd content of both the liver and kidney, which is organs most susceptible to Cd-induced toxicity .
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- HY-12579
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MDM-2/p53
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Cancer
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RO 2468 is a potent, orally active and selective p53-MDM2 inhibitor. RO 2468 has anti-proliferative active. RO 2468 suppresses c growth in SJSA1 osteosarcoma models without obvious toxicity .
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- HY-149810
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Bacterial
Parasite
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Infection
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AcrB-IN-2 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. AcrB-IN-22 inhibits Nile Red (a known substrate of AcrB) efflux.AcrB-IN-2 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
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- HY-149949
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Apoptosis
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Cancer
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Anticancer agent 105 is a compound based on thienopyrimidine scaffold, with with good safety and anticancer properties. Anticancer agent 105 shows selective toxicity towards melanoma cancer, and induces apoptosis. And Anticancer agent 105 significantly inhibits the metastatic nodules, even in pulmonary metastatic melanoma mouse model .
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- HY-162650
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ClpP
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Cancer
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SL44 is an agonist for human caseinolytic protease P (HsClpP), with an EC50 of 1.30 μM. SL44 inhibits the proliferation of LM3 with an IC50 of 3.1 μM. SL44 induces apoptosis in HCC cells, through the degradation of respiratory chain complex subunits. SL44 exhibits antitumor efficacy in mouse models without obvious toxicity (LD50=400 mg/kg). SL44 exhibits good pharmacokinetic characters in rat models .
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- HY-145829
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JAK
Apoptosis
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Inflammation/Immunology
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Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis .
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- HY-149811
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Bacterial
Parasite
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Infection
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Efflux pump-IN-3 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-3 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-3 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
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- HY-149812
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Bacterial
Parasite
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Infection
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Efflux pump-IN-4 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-4 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-4 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
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- HY-157847
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STAT
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Cancer
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Phospho-STAT3-IN-2 (compound 4D) is a STAT3 inhibitor that effectively inhibits STAT3 phosphorylation. phospho-STAT3-IN-2 can significantly reduce tumor volume in mouse xenograft tumor models without drug toxicity to other organs and tissues .
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- HY-162657
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Cholinesterase (ChE)
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Cancer
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AChE-IN-74 (Compound 10) is a modulator for cholinesterase. AChE-IN-74 inhibits the proliferation of liver cancer cell Hep3B and SkHep1 with IC50 of 3.6 and 19.9 μM. AChE-IN-74 exhibits a low embryonic toxicity in zebrafish models (10-15 μM) .
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- HY-162573
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Monoamine Oxidase
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Neurological Disease
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Monoamine Oxidase B inhibitor 5 (Compound 16d) is a selective and reversible inhibitor for monoamine oxidase B (hMAO-B) with an IC50 of 67.3 nM and a Ki of 82.5 nM. Monoamine Oxidase B inhibitor 5 exhibits good pharmacokinetic characters and weak toxicity in rats model. Monoamine Oxidase B inhibitor 5 alleviates MPTP-induced (HY-15608) motor impairment in Parkinson’s mouse model. Monoamine Oxidase B inhibitor 5 is blood-brain barrier (BBB) penetrate .
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- HY-122181
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Histone Methyltransferase
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Cancer
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OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
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- HY-122181A
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Histone Methyltransferase
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Cancer
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OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells .
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- HY-122181B
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Histone Methyltransferase
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Cancer
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OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
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- HY-143585
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CDK
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Cancer
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CDK9-IN-14 is a potent and selective CDK9 inhibitor with IC50 of 6.92 nM. CDK9-IN-14 has a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and has a good selectivity and a low toxicity and few side effects .
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- HY-168733
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Lactate Dehydrogenase
Apoptosis
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Cancer
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LDHA-IN-9 (Compound 1g) is an inhibitor for LDH-A with an IC50 of 25 nM. LDHA-IN-9 inhibits the proliferation of DLD-1 cell (GI50 of 27 μM) through apoptosis induction. LDHA-IN-9 exhibits antitumor activity in mouse model without significant toxicity (25 mg/kg) .
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- HY-170506
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Others
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Inflammation/Immunology
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KB-208 is a phagocytosis inhibitor that improves immune thrombocytopenia (ITP) in mouse models at a dose of 1 mg/kg. KB-208 does not affect other blood parameters and does not elevate serum toxicity biomarkers. KB-208 can be used in immunology research .
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- HY-P3340
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iGluR
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Neurological Disease
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Leptin (116-130) is a bioactive leptin fragment. Leptin (116-130) promotes AMPA receptor trafficking to synapses and facilitate activity-dependent hippocampal synaptic plasticity. Leptin (116-130) prevents hippocampal synaptic disruption and neuronal cell death in models of amyloid toxicity. Leptin (116-130) has the potential for the research of Alzheimer's disease (AD) .
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- HY-144289
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Glucokinase
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Metabolic Disease
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BMS-820132 is an orally active and partial glucokinase (GK) activator with a AC50 of 29 nM. BMS-820132 decreases the glucose levels in glucose tolerance test (OGTT) model in normal rats, but not Zucker diabetic fatty (ZDF) rats. BMS-820132 exhibits pharmacological toxicity secondary to strong GK activation .
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- HY-N8249
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nAChR
Interleukin Related
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Inflammation/Immunology
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Cynandione A is an acetophenone that can be isolated from Cynanchum Wilfordii Radix. Cynandione A protects hepatocytes and cortical neurons from toxicity and improves neurological deficits in a rat model of cerebral ischemia. On the other hand, cynandione A has significant anti-inflammatory effects and inhibits inflammation by activating macrophage α7 nAChR and IL-10 expression .
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- HY-N0462
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-
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- HY-P10360
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α-synuclein
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Neurological Disease
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Tat-βsyn-degron is an α-synuclein knockdown peptide. Tat-βsyn-degron binds toα-synuclein and reduces α-synuclein levels in primary rat cortical neuron cultures. Tat-βsyn-degron also reduces α-synuclein levels and decreases the parkinsonian toxin-induced neuronal damage and motor impairment in a mouse toxicity model of PD .
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- HY-163763
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G2A (GPR132)
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Neurological Disease
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T-10418 is an agonist for G2 accumulation protein (G2A) (also known as G protein-coupled receptor GPR132) with an EC50 of 0.82 μM. T-10418 exhibits a sensitizing effect on mouse primary sensory neurons. T-10418 exhibits good pharmacokinetic characteristics, and no obvious toxicity (at 100 μM) in mouse models .
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- HY-168043
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STAT
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Cancer
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STAT3-IN-35 is a STAT3 inhibitor that binds to SH2 domain. STAT3-IN-35 inhibits the phosphorylation of STAT3 and possesses antiproliferative activities against triple-negative breast cancer (TNBC) cell lines. STAT3-IN-35 also has a toxicity and potent antitumor activity in a TNBC xenograft model .
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- HY-108467
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GGsTop
3 Publications Verification
Nahlsgen
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Others
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Cardiovascular Disease
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GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ-GGT inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150 and 51 M -1 s -1 against E.coli GGT and human GGT, respectively. GGsTop protects hepatic ischemia-reperfusion injury in rat model .
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- HY-W008719
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MPP+ iodide
Maximum Cited Publications
14 Publications Verification
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Mitochondrial Metabolism
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Neurological Disease
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MPP+ iodide, a toxic metabolite of the neurotoxin MPTP, causes symptom of Parkinson's disease in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ iodide is taken up by the dopamine transporter into dopaminergic neurons where it exerts its neurotoxic action on mitochondria by affecting complex I of the respiratory chain. MPP+ iodide is also a high affinity substrate for the serotonin transporter (SERT) .
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- HY-156483
-
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Others
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Cancer
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TT-012 specifically binds to dynamic MITF and destroys the latter's dimer formation and DNA-binding ability. TT-012 inhibits the transcriptional activity of MITF in B16F10 melanoma cells. TT-012 inhibits the growth of high-MITF melanoma cells, and inhibits the tumor growth and metastasis with tolerable toxicity to liver and immune cells in animal models .
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- HY-158160
-
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Sodium Channel
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Metabolic Disease
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LBA-3 is a selective, orally active inhibitor for sodium-coupled citrate transporter SLC13A5, with an IC50 of 67 nM. LBA-3 decreases levels of triglyceride and total cholesterol in oleic and palmitic acid (OPA)-stimulated AML12 cells, PCN-stimulated primary mouse hepatocytes and in mouse models, without detectable toxicity. LBA-3 is blood-brain barrier permeable .
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- HY-162646
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Thrombin
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Cardiovascular Disease
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FXIIa-IN-5 (Compound 4J) is an orally active, selective inhibitor for factor XIIa (FXIIa), with IC50 of 21 nM. FXIIa-IN-5 inhibits the intrinsic coagulation pathways, and exhibits anti-inflammatory and antithrombotic activity in Carrageenan (HY-125474)-induced mice thrombosis models. FXIIa-IN-5 exhibits moderate pharmacokinetic characteristics and slightly toxicity (at 100 mg/kg) .
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- HY-162818
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Bacterial
Reactive Oxygen Species
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Infection
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Antibacterial agent 237 (compound Ru-8) is a bacteriostatic agent for Staphylococcus aureus, with MIC of 0.78-1.56 μg/mL. Antibacterial agent 237 destroys bacterial cell membranes, changes their permeability, and induces bacteria to produce Reactive Oxygen Species, leading to bacterial death without causing drug resistance. Antibacterial agent 237 has low hemolytic toxicity to rabbit red blood cells and Raw 264.7 cells, and has significant antibacterial effects against Staphylococcus aureus in mouse skin wound infection models and Bacillus major larvae infection models .
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- HY-150636
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Autophagy
Apoptosis
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Cancer
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Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer .
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- HY-151933
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HIV
Reverse Transcriptase
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Infection
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HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model .
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- HY-161518
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PD-1/PD-L1
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Cancer
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PD-1/PD-L1-IN-44 (Compound 22) selectively inhibits PD-1/PD-L1 proteins (IC50=1.21 nM). PD-1/PD-L1-IN-44 inhibits tumor growth without toxicity in animal models and increases CD8 + cell infiltration .
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- HY-169290
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JAK
HDAC
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Inflammation/Immunology
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JAK/HDAC-IN-4 (compound 11 i) is a JAK/HDAC inhibitor with the IC50 values of 0.49 nM and 12 nM for JAK2 and HDAC6, respectively. JAK/HDAC-IN-4 inhibits the cell proliferation and the production of nitric oxide. JAK/HDAC-IN-4 ameliorates psoriasis-like skin lesions in an Imiquimod (HY-B0180)-induced murine model with low toxicity .
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- HY-117049
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CDK
DYRK
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Neurological Disease
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Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively) . Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model .
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- HY-101855
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Anle138b
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Amyloid-β
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Neurological Disease
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Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology .
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- HY-121495
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Parasite
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Infection
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BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves .
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- HY-145799
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5A2-SC8
1 Publications Verification
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Liposome
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Cancer
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5A2-SC8 is an ionizable amino lipid in lipid nanoparticles (LNPs) that shows high delivery potential and low in vivo toxicity, enabling efficient delivery of small RNAs such as siRNA and miRNA into tumor cells. 5A2-SC8 LNPs can confer a unique delivery fate of RNA within the liver, thereby changing the therapeutic outcomes in cancer models .
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- HY-161618
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JAK
EGFR
PI3K
IGF-1R
GSK-3
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Inflammation/Immunology
Endocrinology
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MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg) .
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- HY-161936
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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Z21115 is an orally active inhibitor for phosphodiesterase 4 (PDE4), that inhibits PDE4D7 with IC50 of 10.5 nM. Z21115 inhibits Lipopolysaccharide (HY-D1056)-induced expression of IL-6, TNF-α and iNOS. Z21115 exhibits anti-inflammatory activity in DSS (HY-116282)-induced mouse colitis models without significant toxicity (1 g/kg) .
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- HY-119200
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Endogenous Metabolite
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Cancer
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LY-195448 hydrochloride is a phenethanolamine that exhibits anti-tumour activity across various murine tumour models. LY-195448 hydrochloride acts by blocking cells at metaphase. LY-195448 hydrochloride has demonstrated a lack of "standard" side effects commonly associated with cancer treatments, such as myelosuppression and gastrointestinal toxicity. LY-195448 hydrochloride was evaluated in a phase I trial, where it showed only mild and reversible side effects like hypotension, tachycardia, and tremor.
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- HY-158156
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NF-κB
Apoptosis
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Cancer
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NF-κB-IN-16 (compound 9) is a complex (Pt(IV) complex) of NF-κB inhibitor and Cisplatin (HY-17394), which has high efficacy and low toxicity in anti-tumor activity. active. NF-κB-IN-16 can cause DNA damage, induce mitochondrial dysfunction, produce reactive oxygen species, and induce apoptosis through the mitochondrial pathway and endoplasmic reticulum stress. NF-κB-IN-16 potently inhibits the NF-κB/MAPK signaling pathway and disrupts PI3K/AKT signaling. NF-κB-IN-16 also exhibits excellent in vivo antitumor efficiency and low toxicity in A549 or A549/CDDP xenograft models .
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- HY-W008719S
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Mitochondrial Metabolism
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Neurological Disease
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MPP+-d3 (iodide) is deuterium labeled MPP+ (iodide). MPP+ iodide, a toxic metabolite of the neurotoxin MPTP, causes symptom of Parkinson's disease in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ iodide is taken up by the dopamine transporter into dopaminergic neurons where it exerts its neurotoxic action on mitochondria by affecting complex I of the respiratory chain. MPP+ iodide is also a high affinity substrate for the serotonin transporter (SERT)[1][2].
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- HY-155525
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PPAR
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Metabolic Disease
Inflammation/Immunology
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Anti-NASH agent 1 (compound 3d),a derivative of Elafibranor (HY-16737),is a potent agonist of PPAR-α/δ,targeting to nonalcoholic steatohepatitis (NASH). Anti-NASH agent 1 (3-10 mg/kg; 4 weeks) improves hyperlipidemia,liver fat degeneration and liver inflammation in Methionine-choline deficiency (MCD) induced NASH mice model. Anti-NASH agent 1 shows low liver toxicity and potent liver protection effect .
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- HY-162074
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HIV
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Infection
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Nipamovir is a nitroimidazole prodrug. Nipamovir shows comparable antiviral activity to SAMT-247 (HY-102077) and NS-1040 in both cellular assays and a human ex vivo model of HIV infection, along with low toxicity. Nipamovir has EC50 values of 3.64±3.28 and 3.23±2.81 μM for CEM-SS/HIV-1RF and hPBMC/HIV-192HT599, respectively .
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- HY-163538
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PI3K
Apoptosis
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Cancer
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TYM-3-98 is a selective inhibitor for PI3Kδ, with an IC50 of 7.1 nM. TYM-3-98 inhibits proliferationso of B-lymphoma cells. TYM-3-98 inhibits PI3K/AKT/mTOR signaling pathway through induction of apoptosis. TYM-3-98 exhibits good pahrmacokinetic characters and antitumor efficacy in mouse/rat model, without significant toxicity .
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- HY-101447
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EPH 116
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Src
Apoptosis
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Cancer
|
SI-2 (EPH 116) is an inhibitor for steroid receptor coactivator-3 (SRC-3), which reduces the transcriptional activity and protein concentration of SRC-3 in cells, exhibits cytotoxicity in cancer cell, inhibits migration of MDA-MB-468, induces apoptosis of MDA-MB-468. SI-2 inhibits the tumor growth in mouse models, without significant toxicity for heart and other major organs (20 mg/kg) .
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- HY-N0462R
-
|
Toll-like Receptor (TLR)
Reverse Transcriptase
Bacterial
Apoptosis
Autophagy
|
Infection
Inflammation/Immunology
Cancer
|
Corilagin (Standard) is the analytical standard of Corilagin. This product is intended for research and analytical applications. Corilagin, a gallotannin, has anti-tumor, anti-inflammatory and hepatoprotective activities. Corilagin inhibits activity of reverse transcriptase of RNA tumor viruses. Corilagin also inhibits the growth of Staphylococcus aureus with a MIC of 25 μg/mL. Corilagin shows anti-tumor activity on hepatocellular carcinoma and ovarian cancer model. Corilagin shows low toxicity to normal cells and tissues .
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- HY-162962
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Indoleamine 2,3-Dioxygenase (IDO)
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Cancer
|
IDO1/TDO-IN-7 (Compound 43b), an isoquinoline derivative, is a potent dual IDO1/TDO inhibitor, with IC50s of 0.31 μM and 0.08 μM, respectively. IDO1/TDO-IN-7 displays acceptable pharmacokinetic profiles and potent antitumor efficacy with low toxicity in B16-F10 tumor model .
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- HY-116202
-
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Keap1-Nrf2
Reactive Oxygen Species
|
Neurological Disease
|
PACA is an enhancer of nerve growth factor-induced neurite outgrowth, enhancing nerve growth factor (NGF)-induced neurite outgrowth and attenuating 6-hydroxydopamine (6-OHDA)-induced toxicity by activating the Nrf2/HO-1 pathway. PACA has neuroprotective and neurogenic activities. PACA can be used to improve dopaminergic neuron loss and motor dysfunction in MPTP mouse models of Parkinson's disease and MPP +-induced neurons .
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-
- HY-146711
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Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 24 is a potent tubulin inhibitor. Tubulin inhibitor 24 inhibits tubulin polymerization. Tubulin inhibitor 24 induces cell cycle arrest at the G2/M phase in a concentration-dependent manner. Tubulin inhibitor 24 shows antitumor activity with no obvious toxicity .
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- HY-143264
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|
FAAH
MAGL
|
Neurological Disease
|
FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC50s of 11 nM and 36 nM (Kis of 28 nM and 60 nM), respectively . FAAH/MAGL-IN-2 has the potential to research neuropathic pain without causing locomotion impairment .
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- HY-147696
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HSP
AMPK
Reactive Oxygen Species
|
Cancer
|
SMTIN-T140 (compound 6a) is a potent TRAP1 (tumor-necrosis-factor-receptor associated protein 1) inhibitor, with an IC50 of 1.646 μM. SMTIN-T140 shows anticancer activity. SMTIN-T140 leads to mitochondrial dysfunction, increases mitochondrial ROS production and activates AMPK. SMTIN-T140 potently suppressed tumor growth without any noticeable in vivo toxicity in a mouse model xenografted with PC3 prostate cancer cells .
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- HY-150596
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|
Apoptosis
Bcl-2 Family
JNK
|
Cancer
|
CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity .
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- HY-155740
-
|
PD-1/PD-L1
|
Cancer
|
PD-1/PD-L1-IN-32 (compound A56) is a potent PD-1/PD-L1 inhibitor (IC50=2.4 nM), with anticancer activity. PD-1/PD-L1-IN-32 significantly inhibits tumor growth in hPD-L1 MC38 humanized mouse model, without obvious toxicity against mouse normal ability .
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- HY-161515
-
|
NAMPT
Epigenetic Reader Domain
|
Cancer
|
BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects .
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-
- HY-169940
-
|
HDAC
|
Inflammation/Immunology
|
Fibrostat (Compound 5n) is a selective HDAC6 inhibitor that exerts antifibrotic effects by inhibiting HDAC6 activity, with an IC50 value of 63 nM. It also exhibits good selectivity over HDAC1, HDAC3, HDAC5, HDAC8, HDAC10, and HDAC11. Fibrostat significantly downregulates fibrotic markers (fibronectin and collagen 1) in fibroblasts. Additionally, Fibrostat demonstrated no toxicity in rat-perfused heart and zebrafish larvae models. Fibrostat shows potential for research into fibrosis-related diseases .
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-
- HY-130625
-
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
PD-1/PD-L1-IN 6 (compound A13) is a potent PD-1/PD-L1 interaction inhibitor, with an IC50 of 132.8 nM. PD-1/PD-L1-IN 6 exhibits outstanding immunoregulatory activity. PD-1/PD-L1-IN 6 significantly elevates interferon-γ secretion in a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, without significant toxic effect. PD-1/PD-L1-IN 6 restores the immune response in a T cell-tumor co-culture model .
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-
- HY-145737
-
|
PROTACs
Ras
|
Cancer
|
PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .
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-
- HY-145737A
-
|
PROTACs
Ras
|
Cancer
|
PROTAC SOS1 degrader-1 (TFA) is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .
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-
- HY-155732
-
|
Parasite
|
Infection
|
NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection. NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC500 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19, respectively .
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-
- HY-168102
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Antiproliferative agent-59 (Compound 14u) is an inhibitor for tubulin polymerization. Antiproliferative agent-59 exhibits antiproliferative activities against cancer cells Huh7, SGC-7901, and MCF-7 with IC50 of 0.03, 0.18, and 0.13μM. Antiproliferative agent-59 arrests the cell cycle at G2/M phase and induces apoptosis in Huh7 cell. Antiproliferative agent-59 exhibits antitumor efficacy against liver cancer in Huh7 xenograft mouse models, without significant toxicity .
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-
- HY-145814
-
|
HSP
Fungal
|
Infection
|
HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2) .
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-
- HY-144643
-
|
Fungal
HDAC
Cytochrome P450
|
Inflammation/Immunology
|
CYP51/HDAC-IN-1 is a potent, orally active CYP51/HDAC dual inhibitor. CYP51/HDAC-IN-1 inhibits important virulence factors and down-regulated resistance-associated genes. CYP51/HDAC-IN-1 exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis .
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-
- HY-143881
-
|
FGFR
|
Cancer
|
FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity . FGFR4-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-147081
-
AGRO-100
|
Histone Methyltransferase
Bcl-2 Family
|
Cancer
|
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
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-
- HY-124832
-
|
Caspase
Amyloid-β
|
Neurological Disease
|
δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research .
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-
- HY-144658
-
|
Factor Xa
|
Cardiovascular Disease
|
FXIa-IN-8 is a potent and selective FXIa inhibitor with an IC50 of 14.2 nM. FXIa-IN-8 shows antithrombotic activity without increasing the bleeding risk and obvious toxicitysup>[1].
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-
- HY-116673
-
|
Histone Acetyltransferase
|
Neurological Disease
|
TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory .CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function . CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model .
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-
- HY-121081
-
|
CDK
|
Cancer
|
BAY-958 is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated in vitro, particularly within the CDK family. It shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. In pharmacokinetic studies, BAY-958 exhibited good metabolic stability but had low aqueous solubility and moderate permeability, leading to challenges in bioavailability. Despite these limitations, BAY-958 hydrochloride effectively inhibited tumor growth in mouse xenograft models without significant toxicity, indicating promising efficacy in vivo. However, its suboptimal physicochemical properties prompted further development efforts to identify compounds with improved overall characteristics for potential clinical use .
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-
- HY-118243
-
|
Amyloid-β
|
Others
|
KMS88009 is a potent small molecule that directly interferes with the formation of amyloid-β oligomers, thereby preserving cognitive behavior when used preventively and reversing cognitive behavior decline when used therapeutically. Oral administration of KMS88009 around the onset of Alzheimer's disease symptoms significantly reduced the assembly of amyloid-β oligomers and improved cognitive behavior in the APP/PS1 double transgenic mouse model. This unique dual mode of action suggests that KMS88009 may be a powerful therapeutic candidate for the treatment of Alzheimer's disease. In an evaluation, the physicochemical properties, pharmacokinetics and toxicity of this anti-amyloidogenic small molecule KMS88009 were studied, as well as post-mortem analysis of APP/PS1 TG mice after behavioral testing.
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-
- HY-169938
-
|
HDAC
Histone Demethylase
Apoptosis
|
Cancer
|
LSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC, that inhibits LSD1, HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity .
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-
- HY-139062
-
C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea; D-erythro-Urea-C6-Ceramide
|
Apoptosis
Ceramidase
Autophagy
β-catenin
|
Cancer
|
C6 Urea Ceramide (Cer(d18:1/6:0) Urea) is an inhibitor of neutral ceramidase. C6 Urea Ceramide increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and HT-29 colon cancer cells. C6 Urea Ceramide (5-10 μM) inhibits proliferation of HT-29 cells and induces apoptosis and autophagy, but is not toxic to non-cancerous cells. C6 Urea Ceramide decreases total and phosphorylated β-catenin levels in HT-29 and HCT116 cells, and induces colocalization of β-catenin with the 20S proteasome. C6 Urea Ceramide (1.25, 2.5, and 5 mg/kg) reduced tumor growth and increased C16, C18, C20, and C24 ceramide levels in tumor tissues in the HT-29 mouse xenograft model.
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-
Cat. No. |
Product Name |
Type |
-
- HY-138171
-
Lipid 5
1 Publications Verification
|
Drug Delivery
|
Lipid 5 is an amino lipid that affords efficient mRNA delivery in rodent and primate models. Lipid 5 shows optimal pharmacokinetics and non-toxic side effects .
|
-
- HY-145799
-
5A2-SC8
1 Publications Verification
|
Drug Delivery
|
5A2-SC8 is an ionizable amino lipid in lipid nanoparticles (LNPs) that shows high delivery potential and low in vivo toxicity, enabling efficient delivery of small RNAs such as siRNA and miRNA into tumor cells. 5A2-SC8 LNPs can confer a unique delivery fate of RNA within the liver, thereby changing the therapeutic outcomes in cancer models .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3350
-
|
Bacterial
|
Infection
|
LS-BF1 is a stable and low toxic cationic antimicrobial peptide. LS-BF1 displays broad spectrum of antibacterial activity, including the challenging ESKAPE pathogens, by cell membrane disruptive mechanism. LS-BF1 shows good in vivo efficacy for elimination of bacteria in a mouse infection model[1].
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-
- HY-P3340
-
|
iGluR
|
Neurological Disease
|
Leptin (116-130) is a bioactive leptin fragment. Leptin (116-130) promotes AMPA receptor trafficking to synapses and facilitate activity-dependent hippocampal synaptic plasticity. Leptin (116-130) prevents hippocampal synaptic disruption and neuronal cell death in models of amyloid toxicity. Leptin (116-130) has the potential for the research of Alzheimer's disease (AD) .
|
-
- HY-P10360
-
|
α-synuclein
|
Neurological Disease
|
Tat-βsyn-degron is an α-synuclein knockdown peptide. Tat-βsyn-degron binds toα-synuclein and reduces α-synuclein levels in primary rat cortical neuron cultures. Tat-βsyn-degron also reduces α-synuclein levels and decreases the parkinsonian toxin-induced neuronal damage and motor impairment in a mouse toxicity model of PD .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-W008719S
-
|
MPP+-d3 (iodide) is deuterium labeled MPP+ (iodide). MPP+ iodide, a toxic metabolite of the neurotoxin MPTP, causes symptom of Parkinson's disease in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ iodide is taken up by the dopamine transporter into dopaminergic neurons where it exerts its neurotoxic action on mitochondria by affecting complex I of the respiratory chain. MPP+ iodide is also a high affinity substrate for the serotonin transporter (SERT)[1][2].
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-
Cat. No. |
Product Name |
|
Classification |
-
- HY-138171
-
Lipid 5
1 Publications Verification
|
|
Cationic Lipids
|
Lipid 5 is an amino lipid that affords efficient mRNA delivery in rodent and primate models. Lipid 5 shows optimal pharmacokinetics and non-toxic side effects .
|
-
- HY-145799
-
5A2-SC8
1 Publications Verification
|
|
Cationic Lipids
|
5A2-SC8 is an ionizable amino lipid in lipid nanoparticles (LNPs) that shows high delivery potential and low in vivo toxicity, enabling efficient delivery of small RNAs such as siRNA and miRNA into tumor cells. 5A2-SC8 LNPs can confer a unique delivery fate of RNA within the liver, thereby changing the therapeutic outcomes in cancer models .
|
-
- HY-147081
-
AGRO-100
|
|
Aptamers
|
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
|
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