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in vitro functional studies

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-122351A
    Advantame

    		Taste Receptor Others
    Advantame is an N-substituted derivative of aspartame. Advantame is a high-intensity, low calorie sweetener. Advantame can interact with plasma protein. Advantame has the potential to produce hypotension and inhibit hERG K + channel to produce carditoxicity. Advantame binds to T1R2/T1R3 taste GPCR to form an oligomeric functional selectivity of biased heteromers with NMBR to induce a significant sialidase activity in vitro. Advantame has maternal toxicity (gastrointestinal disturbances) in the prenatal developmental toxicity study in rabbits .
    Advantame
  • HY-125209A
    TH5427 hydrochloride

    		Apoptosis PARP DNA/RNA Synthesis Cancer
    TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC50 of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9 .TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis .TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells .TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells .TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay .TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA) .TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells .TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells .TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines .TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer .
    TH5427 hydrochloride
  • HY-162856
    TRPV1-IN-2

    		TRP Channel Neurological Disease
    TRPV1-IN-2 ((R)-32) is a TRPV1 inhibitor. TRPV1-IN-2 has protective effects on ED epilepsy models .
    TRPV1-IN-2
  • HY-122351
    Advantame free acid

    		Drug Derivative Taste Receptor Others
    Advantame is an N-substituted derivative of aspartame. Advantame is a high-intensity, low calorie sweetener. Advantame can interact with plasma protein. Advantame has the potential to produce hypotension and inhibit hERG K + channel to produce carditoxicity. Advantame binds to T1R2/T1R3 taste GPCR to form an oligomeric functional selectivity of biased heteromers with NMBR to induce a significant sialidase activity in vitro. Advantame has maternal toxicity (gastrointestinal disturbances) in the prenatal developmental toxicity study in rabbits .
    Advantame free acid
  • HY-122351AR
    Advantame (Standard)

    		Reference Standards Taste Receptor Others
    Advantame (Standard) is the analytical standard of Advantame. This product is intended for research and analytical applications. Advantame is an N-substituted derivative of aspartame. Advantame is a high-intensity, low calorie sweetener. Advantame can interact with plasma protein. Advantame has the potential to produce hypotension and inhibit hERG K + channel to produce carditoxicity. Advantame binds to T1R2/T1R3 taste GPCR to form an oligomeric functional selectivity of biased heteromers with NMBR to induce a significant sialidase activity in vitro. Advantame has maternal toxicity (gastrointestinal disturbances) in the prenatal developmental toxicity study in rabbits .
    Advantame (Standard)
  • HY-181712
    IRAK1-IN-2

    		IRAK Cancer
    IRAK1-IN-2 is an orally active IRAK1 inhibitor and antitumor agent with high selectivity for IRAK4 and other kinases in the same group. IRAK1-IN-2 functionally inhibits IRAK1 and interferes with the TLR/IL-1R signaling pathway. IRAK1-IN-2 suppresses hepatocellular carcinoma-related cellular processes in vitro and in animal models. IRAK1-IN-2 serves as a chemical probe for IRAK1 research and is applicable to studies on hepatocellular carcinoma .
    IRAK1-IN-2
  • HY-134483
    5-HT7/5-HT2A receptor antagonist 1

    		5-HT Receptor Neurological Disease
    5-HT7/5-HT2A receptor antagonist 1 is a high-affinity, orally active, brain-penetrant 5-HT7 and 5-HT2A receptor ligand having a pKi = 8.1 at both receptors. 5-HT7/5-HT2A receptor antagonist 1 behaves as an antagonist in an in vitro functional assay for 5-HT2A and as an inverse agonist in an in vitro functional assay for 5-HT7. 5-HT7/5-HT2A receptor antagonist 1 blockade of 5-Carboxamidotryptamine (5-CT) (HY-135555) induced hypothermia in rats, and blockade of 2,5-dimethoxy-4-iodoamphetamine (DOI) induced head-twitches in mice. 5-HT7/5-HT2A receptor antagonist 1 occupied 5-HT2A receptor binding sites in the frontal cortex of the rat brain. 5-HT7/5-HT2A receptor antagonist 1 can be used for the study of Neurological diseases .
    5-HT7/5-HT2A receptor antagonist 1

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