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Results for "

phosphorylated IκBα

" in MedChemExpress (MCE) Product Catalog:

5

Inhibitors & Agonists

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-128586
    TAS4464
    5+ Cited Publications

    		 Apoptosis Carbonic Anhydrase NEDD8-activating Enzyme Cancer
    TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
    TAS4464
  • HY-128586A
    TAS4464 hydrochloride
    5+ Cited Publications

    		 NEDD8-activating Enzyme Carbonic Anhydrase Apoptosis Cancer
    TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
    TAS4464 hydrochloride
  • HY-N4308
    Hexamethylquercetagetin

    Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone

    		 NF-κB IKK Bcl-2 Family Cancer
    Hexamethylquercetagetin (Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone) is an orally active NF-κB inhibitor. Hexamethylquercetagetin inhibits NF-κB-derived luciferase activity, reduces phosphorylated p65 and IκBα, Cyclin D1, Bcl-2 and blocks TNFα-induced NF-κB activation. Hexamethylquercetagetin inhibits survival and proliferation of cervical carcinoma cells. Hexamethylquercetagetin suppresses tumor volume and weight in BALB/c nude mouse xenograft models of cervical carcinoma. Hexamethylquercetagetin can be used for the research of cancer, such as cervical carcinoma .
    Hexamethylquercetagetin
  • HY-173416
    Anti-inflammatory agent 100

    		NF-κB p38 MAPK ERK JNK Inflammation/Immunology
    Anti-inflammatory agent 100 (Compound (+)-4S-23) is an anti-inflammatory agent. Anti-inflammatory agent 100 inhibits MAPK and NF-κB signaling, and also inhibits NF-κB pathway by suppressing the phosphorylation of IκB-α and blocking nuclear translocation of phosphorylated p65. Anti-inflammatory agent 100 inhibits NO production (IC50: 0.5 μM) and TNF-α, IL-6, IL-1β secretion .
    Anti-inflammatory agent 100
  • HY-180829
    HDAC6-IN-71

    		HDAC NF-κB IKK COX NO Synthase Inflammation/Immunology
    HDAC6-IN-71 (Compound 24) is a HDAC6 inhibitor with IC50 values for HDAC6 and HDAC1 of 13.68 and 443.12 nM respectively. HDAC6-IN-71 effectively inhibits the production of NO by mouse macrophages, with its IC50 being 2.31 μM. HDAC6-IN-71 inhibits the HDAC6-NF-κB signaling pathway, reduces the levels of phosphorylated IκB-α and IKK-α/β, and suppresses the expression of downstream inflammatory proteins COX-2 and iNOS. HDAC6-IN-71 significantly alleviates ulcerative colitis in mice .
    HDAC6-IN-71

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