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Cytoplasm Inhibitors

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27

Inhibitors & Agonists

2

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-141609
    IK-175

    AHR antagonist 5 free base

    		 Aryl Hydrocarbon Receptor Cancer
    IK-175 is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. IK-175 effectively blocks AHR from translocating from the cytoplasm to the nucleus. IK-175 is highly selective for AHR over other receptors, transporters, and kinases .
    IK-175
  • HY-120821
    Endosidin-2
    2 Publications Verification

    ES2

    		 Exosomes Others
    Endosidin-2 (ES2) is a selective inhibitor targeting the conserved exosome subunit EXO70. Endosidin-2 binds to the C-terminal domain of EXO70, inhibiting exocytosis and endosomal recycling, while promoting vacuolar trafficking in plant cells. Endosidin-2 interferes with the EXO70-mediated vesicle-to-plasma membrane anchoring process, leading to abnormal aggregation of auxin transporters (such as PIN2) in the cytoplasm and redirected to vacuolar degradation, while causing abnormal Golgi structure (such as cup-shaped or ring-shaped vesicles cisternae formation). Endosidin-2 can inhibit exocytosis in plant and mammalian cells and is mainly used to study the dynamic regulation of membrane trafficking (such as polar growth, vesicle sorting) .
    Endosidin-2
  • HY-116044
    BCATc Inhibitor 2
    Maximum Cited Publications
    6 Publications Verification

    		 Aminotransferases (Transaminases) Neurological Disease
    BCATc Inhibitor 2 is a selective branched-chain aminotransferase (BCAT) inhibitor for research of neurodegenerative diseases. The IC50s of 0.2 μM, 0.8 μM and 3.0 μM for rat cytosolic isoenzyme rBCATc, human cytosolic isoenzyme hBCATc and rat mitochondrial isoenzyme rBCATm, respectively. BCATc, also called BCAT1, is in the cytoplasm .
    BCATc Inhibitor 2
  • HY-158420
    STL001

    		Autophagy Cancer
    STL001 is potent and selective FOXM1 inhibitor. STL001 induces the translocation of nuclear FOXM1 to the cytoplasm and promotes its autophagic degradation. STL001 sensitizes human cancers to a broad-spectrum of cancer therapies .
    STL001
  • HY-15873A
    FTI 276 TFA

    		Farnesyl Transferase Ras p38 MAPK Cancer
    FTI 276 TFA is a farnesyltransferase (FTase) inhibitor with an IC50 of 0.5 nM, and it exhibits selectivity for FTase over geranylgeranyltransferase I (GGTase I). FTI 276 TFA blocks the farnesylation of H-Ras and K-Ras4B, causes inactive Ras-Raf complexes to accumulate in the cytoplasm, and inhibits constitutive MAPK activation. FTI 276 TFA reduces the number, incidence and volume of tumors, and restricts the growth of tumors expressing activated K-ras. FTI 276 TFA can be used in research related to pulmonary adenoma .
    FTI 276 TFA
  • HY-116716
    PIN1 inhibitor API-1
    1 Publications Verification

    		 MicroRNA Cancer
    PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development .
    PIN1 inhibitor API-1
  • HY-159621
    Endosidine 5

    ES5

    		 Annexin A Endocrinology
    Endosidine 5 (ES5) inhibits EPS (extracellular polymeric substance) secretion and cell wall expansion. Endosidine 5 alters secretion of ECM (extracellular matrix) material in Penium margaritaceum by affecting the Golgi apparatus. Endosidine 5 interferes with recycling endosomes through Annexin A6, thereby promoting the release and expression of mRNA into the cytoplasm .
    Endosidine 5
  • HY-149010
    NXPZ-2

    		Keap1-Nrf2 Neurological Disease
    NXPZ-2 is an orally active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with a Ki value of 95 nM, EC50 value of 120 and 170 nM. NXPZ-2 can dose-dependently ameliorate Aβ[1-42]-Induced cognitive dysfunction, improve brain tissue pathological changes in Alzheimer’s disease (AD) mouse by increasing neuron quantity and function. NXPZ-2 can inhibit oxidative stress by increasing Nrf2 expression levels and promoting its cytoplasm to nuclear translocation, which is helpful for Keap1-Nrf2 PPI inhibitors and AD associated disease research .
    NXPZ-2
  • HY-156500
    ICMT-IN-1

    		ICMT Cancer
    ICMT-IN-1 (compound 75) is an inhibitor of ICMT (IC50=0.0013 μM). ICMT-IN-1 dose-dependently induces ICMT accumulation in the cytoplasm of HCT-116 cells and inhibits the proliferation of multiple cancer cell lines expressing K-Ras and N-Ras .
    ICMT-IN-1
  • HY-164102
    TNF-α-IN-18

    		TNF Receptor NF-κB Inflammation/Immunology
    TNF-α-IN-18 (Compound 61) is an inhibitor for TNF-α (IC50 of 1.8 μM), that inhibits TNF signaling pathway through block of NF-kB migration from cytoplasm to nucleus. TNF-α-IN-18 exhibits slight cytotoxicity to mouse fibroblast LM cell, with a CC50 >50 μM. TNF-α-IN-18 ameliorates the TNF- or Lipopolysaccharide (HY-D1056)-induced sepsis in mouse models. TNF-α-IN-18 protects mice from rheumatoid arthritis .
    TNF-α-IN-18
  • HY-155052
    PAD4-IN-2

    		Protein Arginine Deiminase Cancer
    PAD4-IN-2 is a highly tumor-targeted and irreversible PAD4 inhibitor with an IC50 of 1.94 μM. It selectively recognizes sialic acid on tumor surfaces and accumulates in tumor tissues, with distribution in the cytoplasm of tumor cells and nuclei of neutrophils. PAD4-IN-2 inhibits the PAD4-H3cit-NETs (Neutrophil Extracellular Traps) pathway, reduces senescent tumor-associated neutrophils, and promotes M1 macrophage polarization. The compound exhibits potent anti-tumor and anti-metastatic activities and is suitable for breast cancer research .
    PAD4-IN-2
  • HY-155052A
    PAD4-IN-2 TFA

    		Protein Arginine Deiminase Cancer
    PAD4-IN-2 TFA is a highly tumor-targeted and irreversible PAD4 inhibitor with an IC50 of 1.94 μM. PAD4-IN-2 TFA selectively recognizes sialic acid on tumor surfaces and accumulates in tumor tissues, with distribution in the cytoplasm of tumor cells and nuclei of neutrophils. PAD4-IN-2 TFA inhibits the PAD4-H3cit-NETs (Neutrophil Extracellular Traps) pathway, reduces senescent tumor-associated neutrophils, and promotes M1 macrophage polarization. The compound exhibits potent anti-tumor and anti-metastatic activities and is suitable for breast cancer research .
    PAD4-IN-2 TFA
  • HY-124712
    Divin

    		Bacterial Infection
    Divin, a potent chelator of iron, is a potent inhibitor of bacterial cell division with bacteriostatic effect in Gram-negative and Gram-positive bacteria. Divin disrupts the assembly of late division proteins, reduces peptidoglycan remodeling at the division site, and blocks compartmentalization of the cytoplasm .
    Divin
  • HY-175498
    RLA-3107

    		SARS-CoV Infection
    RLA-3107 is an artemisinin regioisomer that blocks ion channels, thereby preventing cations from entering the host cytoplasm. RLA-3107 is also a viroporin inhibitor .
    RLA-3107
  • HY-N10009
    Cudraflavone B

    		NF-κB TNF Receptor COX ERK p38 MAPK Sirtuin Inflammation/Immunology
    Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells .
    Cudraflavone B
  • HY-162500
    Antifungal agent 99

    		Fungal Infection
    Antifungal agent 99 (Compound E1) is a fungal succinate dehydrogenase (SDH) inhibitor. Antifungal agent 99 reduces mycelial density and significantly increase the mitochondrial number in mycelia cytoplasm .
    Antifungal agent 99
  • HY-N10458
    Asperbisabolane L

    		NF-κB Inflammation/Immunology
    Asperbisabolane L, a sesquiterpenoid, exerts the anti-inflammatory activity by inhibiting the NF-κB-activated pathway. Asperbisabolane L inhibits the translocation of NF-κB from cytoplasm to the nucleus. Asperbisabolane L also inhibits NO production in LPS-activated BV-2 microglia cells .
    Asperbisabolane L
  • HY-149705
    ICMT-IN-7

    		ICMT Cancer
    ICMT-IN-7 (compound 74) is an inhibitor of ICMT (IC50=0.015 μM). ICMT-IN-7 dose-dependently induces ICMT accumulation in the cytoplasm of HCT-116 cells and inhibits the proliferation of multiple cancer cell lines expressing K-Ras and N-Ras .
    ICMT-IN-7
  • HY-116535B
    DL-threo-PPMP

    		Parasite Infection
    DL-threo-PPMP is an inhibitor of sphingosine synthetase in Plasmodium falciparum. DL-threo-PPMP inhibits the activity of sphingosine synthetase by mimicking the substrate sphingosine. This inhibition leads to a rapid decrease in the activity of sensitive sphingosine synthetase, selectively destroying the interconnected tubular network of TVMs in the host cell cytoplasm, and this inhibition also blocks the proliferation of Plasmodium falciparum. DL-threo-PPMP can be used for the study of Plasmodium biology and the search for new antimalarial strategies .
    DL-threo-PPMP
  • HY-113701
    CH5137291

    		Androgen Receptor Cancer
    CH5137291 is an orally active pure antagonist of the androgen receptor (AR), without generating agonist metabolites. CCH5137291 directly blocks the transfer of AR from the cytoplasm to the nucleus. H5137291 can completely inhibit tumor growth in cells and mouse models of castration-resistant prostate cancer models. CH5137291 can be used for the study of castration-resistant prostate cancer (CRPC) .
    CH5137291
  • HY-116535A
    DL-threo-PPMP hydrochloride

    		Parasite Infection
    DL-threo-PPMP hydrochloride is an inhibitor of sphingosine synthetase in Plasmodium falciparum. DL-threo-PPMP hydrochloride inhibits the activity of sphingosine synthetase (sphingosine synthetase) by binding to a substrate that mimics sphingosine. This inhibition leads to a rapid decline in sensitive sphingomyelin synthase (SSS) activity, selectively disrupting the interconnected tubular network of TVM in the cytoplasm of the host cell, and this inhibition also blocks the proliferation of the parasite. DL-threo-PPMP hydrochloride can be used in the study of malaria parasite biology and the search for new antimalarial strategies .
    DL-threo-PPMP hydrochloride
  • HY-163896
    β-Catenin modulator-7

    		β-catenin Cancer
    β-Catenin modulator-7 (Compound 5) is a modulator for β-catenin. β-Catenin modulator-7 inhibits the expression of β-catenin in HCT-116 cytoplasm and nucleus, suppresses the phosphorylation of GSK 3β. β-Catenin modulator-7 promotes NO release in HCT-116, and inhibits the proliferation of cancer cell HCT-116 with IC50 of 0.6-0.9 μM. β-Catenin modulator-7 can be used in reasearch about colon cancer .
    β-Catenin modulator-7
  • HY-119009
    TM-233

    		JAK STAT NF-κB Bcl-2 Family Cancer
    TM-233 is an inhibitor of the JAK/STAT and NF-κB signaling pathways, exhibiting significant antitumor activity. TM-233 reduces the expression of the anti-apoptotic protein Mcl-1 by inhibiting the phosphorylation of JAK2 and STAT3, and regulates its transcription by directly binding to the Mcl-1 gene promoter. Additionally, TM-233 prevents the translocation of NF-κB from the cytoplasm to the nucleus by inhibiting its DNA-binding activity, thereby reducing nuclear NF-κB expression. TM-233 shows potential in overcoming Bortezomib (HY-10227) resistance and can be applied in research related to multiple myeloma .
    TM-233
  • HY-185344
    Ratutrelvir

    TRX01

    		 NF-κB Cancer
    Ratutrelvir is a NF-κB p65 inhibitor. Ratutrelvir blocks the translocation of NF-κB p65 from the cytoplasm to the nucleus, reduces the phosphorylation levels of NF-κB p65 and IκBα, and inhibits the DNA-binding activity of NF-κB p65. Ratutrelvir inhibits the migration and invasion abilities of breast cancer cells, and reduces their viability and colony-forming capacity. Ratutrelvir can be used for the research of luminal A breast cancer .
    Ratutrelvir
  • HY-182566
    ITI-367

    		HIV Infection
    ITI-367 is a HIV-1 inhibitor that targets the nuclear localization signal 1 (NLS-1) of HIV-1 matrix protein and the interaction between HIV-1 pre-integration complex (PIC) and importin-β. ITI-367 inhibits HIV-1 replication at the pre-integration stage, reduces the formation of 2-LTR circles, and sequesters viral DNA in the cytoplasm. ITI-367 can be used for the research of HIV infection .
    ITI-367
  • HY-W714183
    Dinitramine

    		Herbicide ERK p38 MAPK JNK PI3K Akt Apoptosis Microtubule/Tubulin Metabolic Disease
    Dinitramine is a herbicide. Dinitramine activates the Erk/P38/JNK/MAPK pathway and inactivates the PI3k/Akt pathway in testicular cells. Dinitramine induces endoplasmic reticulum stress, dysregulation of calcium homeostasis in the cytoplasm and mitochondria, apoptosis, and downregulated expression of cell cycle genes in testicular cells. Dinitramine reduces the viability and proliferation capacity of testicular cells, and inhibits cell division by suppressing the synthesis of tubulin. Dinitramine induces abnormal heart development, inhibited angiogenesis, inflammatory responses, apoptosis, and impaired embryonic growth in zebrafish embryos .
    Dinitramine
  • HY-182383
    VMY-1-101

    		CDK Apoptosis Cancer
    VMY-1-101 is a fluorescent cyclin-dependent kinase (CDK) inhibitor, with an excitation of 410 nm and emission of 512 nm. VMY-1-101 competitively inhibits ATP binding to CDKs. VMY-1-101 induces G2/M cell cycle arrest in human breast cancer cells. VMY-1-101 induces modest apoptosis in human breast cancer cells. VMY-1-101 blocks proliferation of human breast cancer cells, including multidrug resistance-positive cells, and is not a substrate for p-glycoprotein. VMY-1-101 localizes to the cytoplasm of human breast cancer cells. VMY-1-101 shows increased binding to human breast cancer tissue compared to fluorophore alone. VMY-1-101 can be used for the research of breast cancer .
    VMY-1-101

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