2. Search Result
Search Result
Pathways Recommended: Vitamin D Related/Nuclear Receptor
Results for "

Nuclear factor-��B

" in MCE Product Catalog:

251

Inhibitors & Agonists

3

Screening Libraries

7

Fluorescent Dye

26

Peptides

1

Inhibitory Antibodies

53

Natural
Products

52

Recombinant Proteins

15

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas
  • HY-D0943
    Nuclear Fast Red

    Kernechtrot

    		 Fluorescent Dye Others
    Nuclear Fast Red, an anthraquinone dye, is commonly used in conjunction with an excess of aluminum ions as a red nuclear counterstain. Nuclear fast red has been used as a histochemical and colorimetric reagent for calcium. Nuclear fast red as highly sensitive "off/on" fluorescent probe for detecting guanine.
  • HY-136556
    Factor B-IN-1

    		Complement System Inflammation/Immunology
    Factor B-IN-1 is a Factor B inhibitor extracted from patent WO2013164802A1, Example 24.
  • HY-147605
    Factor B-IN-3

    		Complement System Inflammation/Immunology
    Factor B-IN-3 (Example 3 target compound) is a potent complement factor B inhibitor. Factor B-IN-3 can be used for the research of diseases related to inflammation and immunity.
  • HY-147606
    Factor B-IN-4

    		Complement System Inflammation/Immunology
    Factor B-IN-4 (Example 13 target compound) is a potent complement factor B inhibitor, with an IC50 of 1 μM. Factor B-IN-4 can be used for the research of diseases related to inflammation and immunity.
  • HY-147607
    Factor B-IN-5

    		Complement System Inflammation/Immunology
    Factor B-IN-5 (Example 5 target compound) is a potent complement factor B inhibitor, with an IC50 of 1.2 μM. Factor B-IN-5 can be used for the research of diseases related to inflammation and immunity.
  • HY-147604
    Factor B-IN-2

    		Complement System Inflammation/Immunology
    Factor B-IN-2 (Example 1 target compound) is a potent complement factor B inhibitor, with an IC50 of 1.5 μM. Factor B-IN-2 can be used for the research of diseases related to inflammation and immunity.
  • HY-101859
    NucPE1

    Nuclear Peroxy Emerald 1

    		 Reactive Oxygen Species Others
    NucPE1 (Nuclear Peroxy Emerald 1) is a nuclear-localized fluorescent hydrogen peroxide that is specifically localized to cellular nuclei without appended targeting moieties.
  • HY-15619
    Hoechst S 769121

    Nuclear yellow

    		 Fluorescent Dye Others
    Hoechst S 769121 (Nuclear yellow) exhibits excitation/emission maxima ~335/495 nm when bound to DNA.
  • HY-146287
    Zn(BQTC)

    		DNA/RNA Synthesis Apoptosis Cancer
    Zn(BQTC) is a highly potent mitochondrial DNA (mtDNA) and nuclear DNA (nDNA) inhibitor. Zn(BQTC) causes severe damage to the mtDNA and nDNA, sequentially disruptes mitochondrial and nuclear functions. Zn(BQTC) promotes the DNA damage-induced apoptotic signaling pathway. Zn(BQTC) has selectively antiproliferative activity against A549R cells. Zn(BQTC) can be used for researching anticancer.
  • HY-D0944
    Giemsa stain

    		Fluorescent Dye Others
    Giemsa stain can stain chromatin and nuclear membrane. Giemsa stain histopathologic detection of malaria and other microorganisms, such as Histoplasma, LeishmaniaToxoplasma, and Pneumocystis .Giemsa stain can used be in histology and microbiology.
  • HY-138283
    MR837

    		Histone Methyltransferase Cancer
    MR837 is an inhibitor of NSD2-PWWP1. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain).
  • HY-110258
    ML334

    LH601A

    		 Keap1-Nrf2 Cancer
    ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.
  • HY-D0122
    6-Iodoacetamidofluorescein

    		Fluorescent Dye Others
    6-Iodoacetamidofluorescein, a sulphhydryl-specific fluorescent dye, and can be used to selectively label the -SH groups of nuclear matrix polypeptides and proteins.
  • HY-112391
    SD-1029

    		JAK STAT Cancer
    SD-1029 is a JAK2/STAT3 inhibitor. SD-1029 inhibits STAT3 nuclear translocation. SD-1029 is an inhibitor of STAT3 activation due to inhibition of JAK2 phosphorylation.
  • HY-136476
    Mg(II) protoporphyrin IX

    		Others Others
    Mg(II) protoporphyrin IX is a precursor of chlorophyll in Chlorella. Mg(II) protoporphyrin IX is a negative effector of nuclear photosynthetic gene expression. Mg(II) protoporphyrin IX can be used for the research of signaling molecule implicated in plastid-to-nucleus communication.
  • HY-P1430
    11R-VIVIT

    		Nuclear Factor of activated T Cells (NFAT) Metabolic Disease
    11R-VIVIT is a cell-permeable nuclear factor of activated T cells (NFAT) inhibitor. 11R-VIVIT can be used for the research of podocyte and diabetic nephropathy.
  • HY-50001
    Nucleozin

    		Influenza Virus Infection
    Nucleozin, a potent inhibitor of influenza A virus infection, induces the formation of nucleoprotein (NP) aggregates and antagonizes its nuclear accumulation, leading to cessation of viral replication. Nucleozin impedes influenza A virus replication in vitro with a nanomolar EC50.
  • HY-11028
    PF-02413873

    PF-2413873

    		 Progesterone Receptor Endocrinology
    PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo.
  • HY-P1430A
    11R-VIVIT TFA

    		Nuclear Factor of activated T Cells (NFAT) Metabolic Disease
    11R-VIVIT TFA is a cell-permeable nuclear factor of activated T cells (NFAT) inhibitor. 11R-VIVIT TFA can be used for the research of podocyte and diabetic nephropathy.
  • HY-N0116
    Hematoxylin

    Natural Black 1; Haematoxylin

    		 Amyloid-β Others
    Hematoxylin (Natural Black 1), a naturally occurring flavonoid compound derived from Caesalpinia sappan Linn.. Hematoxylin is a nuclear stain in histology and is also a potent Aβ42 fibrillogenesis inhibitor with an IC50 of 1.6 µM.
  • HY-120855
    CCG-100602

    		Ras Cardiovascular Disease
    CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. CCG-100602 specifically block MRTF-A nuclear localization and thus inhibit the fibrogenic transcription factor SRF.
  • HY-107404
    SID 7969543

    		Others Endocrinology
    SID 7969543 is a selective SF-1 (steroidogenic factor 1, NR5A1) inhibitor with an IC50 of 760 nM. SID 7969543 inhibits SF-1-triggered luciferase expression with IC50 of 30 nM. SF-1 is a transcription factor belonging to the nuclear receptor superfamily.
  • HY-127105A
    Iptacopan hydrochloride

    LNP023 hydrochloride

    		 Complement System Metabolic Disease Inflammation/Immunology
    LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM.
  • HY-124811
    IRES-C11

    		c-Myc Cancer
    IRES-C11 is a spectfic c-MYC internal ribosome entry site (IRES) translation inhibitor. IRES-C11 blocks the interaction of a requisite c-MYC IRES trans-acting factor, heterogeneous nuclear ribonucleoprotein A1, with its IRES. IRES-C11 does not inhibits BAG-1, XIAP and p53 IRESes.
  • HY-W009731
    Dibenzoylmethane

    		Keap1-Nrf2 Cancer Metabolic Disease
    Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2.
  • HY-118052
    BPKDi

    		PKD Cardiovascular Disease
    BPKDi is a potent bipyridyl PKD inhibitor with IC50s of 1 nM, 9 nM and 1 nM for PKD1, PKD2 and PKD3, respectively. BPKDi blocks signal-dependent phosphorylation and nuclear export of class IIa HDACs in cardiomyocytes.
  • HY-108469
    BI-6015

    		Others Cancer Metabolic Disease
    BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes.
  • HY-112055
    DIM-C-pPhOH

    		Apoptosis Cancer
    DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.
  • HY-138280
    DTHIB

    		HSP Cancer
    DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB inhibits HSF1 cancer gene signature (HSF1 CaSig) and selectively stimulates degradation of nuclear HSF1. DTHIB has potently anticancer activities and can be used for prostate cancer research.
  • HY-147924
    Keap1-Nrf2-IN-11

    		Keap1-Nrf2 NO Synthase ROS Kinase Inflammation/Immunology
    Keap1-Nrf2-IN-11 (compound 6k) is a Keap1-Nrf2 inhibitor with KD2 value of 0.21 nM. Keap1-Nrf2-IN-11 inhibits the productions of ROS and NO and the expression of TNF-α. Keap1-Nrf2-IN-11 relieves inflammations by increasing the Nrf2 nuclear translocation. Keap1-Nrf2-IN-11 can be used for anti-inflammatory research.
  • HY-13811
    NSC697923

    		E1/E2/E3 Enzyme Apoptosis Cancer
    NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity.
  • HY-N0866
    20-Deoxyingenol

    		Autophagy Inflammation/Immunology
    20-Deoxyingenol, a diterpene, is isolated from the roots of Euphorbia kansui. 20-Deoxyingenol can promote autophagy and lysosomal biogenesis by promoting the nuclear translocation of transcription factor EB (TFEB) in vitro. 20-Deoxyingenol can be used for the research of osteoarthritis (OA).
  • HY-133552
    RORγt Inverse agonist 10

    		ROR Inflammation/Immunology
    RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R
  • HY-16909
    Leptomycin B

    CI 940; LMB

    		 CRM1 Fungal Antibiotic Cancer Infection
    Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
  • HY-15614A
    SC144 hydrochloride

    		Interleukin Related Apoptosis Cancer
    SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells.
  • HY-15614
    SC144

    		Interleukin Related Apoptosis Cancer
    SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells.
  • HY-105037
    Forigerimod

    IPP-201101

    		 Autophagy Inflammation/Immunology
    Forigerimod (IPP-201101) is a CD4 T-cell modulator. Forigerimod is a 21-amino-acid fragment of U1 small nuclear ribonucleoprotein 70 kDa that is phosphorylated at Ser140. Forigerimod can potently inhibit autophagy. Forigerimod can be used for the research of autoimmune disorders, such as systemic lupus erythematosus (SLE) .
  • HY-127105
    Iptacopan

    LNP023

    		 Complement System Metabolic Disease Inflammation/Immunology
    Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G).
  • HY-105037A
    Forigerimod TFA

    IPP-201101 TFA

    		 Autophagy Inflammation/Immunology
    Forigerimod TFA (IPP-201101 TFA) is a CD4 T-cell modulator. Forigerimod TFA is a 21-amino-acid fragment of U1 small nuclear ribonucleoprotein 70 kDa that is phosphorylated at Ser140. Forigerimod TFA can potently inhibit autophagy. Forigerimod can be used for the research of autoimmune disorders, such as systemic lupus erythematosus (SLE) .
  • HY-10035
    TTA-P2

    T-Type calcium channel inhibitor

    		 Calcium Channel Neurological Disease
    TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease.
  • HY-115613
    ML-180

    SR1848

    		 Others Cancer
    ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 µM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 µM). ML-180 has the potential for LRH-1-dependent cancers.
  • HY-133924
    18-Deoxyherboxidiene

    RQN-18690A

    		 Others Cancer Cardiovascular Disease
    18-Deoxyherboxidiene (RQN-18690A) is a potent angiogenesis inhibitor. 18-Deoxyherboxidiene targets SF3b, a spliceosome component that is a subcomplex of the U2 small nuclear ribonucleoprotein (snRNP) in the spliceosome. 18-Deoxyherboxidiene inhibits the migration and tube formation of human umbilical vein endothelial cells (HUVECs) without significant cell toxicity. 18-Deoxyherboxidiene has the potential for cancer research.
  • HY-W107024
    BMS-986260

    		TGF-β Receptor Cancer Inflammation/Immunology
    BMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC50 of 350 nM and 190 nM, respectively.
  • HY-147914
    NSD2-IN-1

    		Apoptosis Cancer
    NSD2-IN-1 (compound 38) is a potent and high selective NSD2-PWWP1 (nuclear receptor-binding SET domain 2-PWWP1) inhibitor, with an IC50 of 0.11 μM. NSD2-IN-1 can bind to NSD2-PWWP1 and then affect the expression of genes regulated by NSD2. NSD2-IN-1 induces apoptosis and cell cycle arrest.
  • HY-44062
    G9a-IN-1

    		Histone Methyltransferase Inflammation/Immunology Cancer
    G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer.
  • HY-N1427A
    Glycodeoxycholic acid monohydrate

    		Endogenous Metabolite Cancer
    Glycodeoxycholic acid monohydrate is a nuclear receptor ligand.
  • HY-14799
    Palovarotene

    R 667; Ro 3300074

    		 RAR/RXR Autophagy Others
    Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.
  • HY-101091
    Importazole

    		Apoptosis Cancer
    Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.
  • HY-14909
    Bardoxolone

    CDDO; RTA 401

    		 Keap1-Nrf2 Cancer
    Bardoxolone is a novel nuclear regulator factor (Nrf-2) activator.
  • HY-152037
    AChE/Nrf2 modulator 1

    		Cholinesterase (ChE) Keap1-Nrf2 Neurological Disease
    AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease.
  • HY-124500
    AC-4-130

    		STAT Apoptosis Cancer
    AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML).
  • HY-136741
    BOT-64

    		IKK Inflammation/Immunology
    BOT-64 is an inhibitory κB (IκB) kinase β (IKKβ) inhibitor with an IC50 of 1 µM. BOT-64 blocks lipopolysaccharide-induced nuclear factor-κB activation and nuclear factor-κB-regulated inflammatory gene transcription.
  • HY-76847
    Chenodeoxycholic Acid

    CDCA

    		 FXR Endogenous Metabolite Autophagy Metabolic Disease Cancer
    Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
  • HY-N6795
    Leptomycin A

    		CRM1 HIV Antibiotic Infection
    Leptomycin A, a Streptomyces metabolite, is an inhibitor of CRM1 (exportin 1) that blocks CRM1 interaction with nuclear export signals, preventing the nuclear export of a broad range of proteins. Leptomycin A suppresses HIV-1 replication. Less potent than Leptomycin B.
  • HY-B1058A
    Benfluorex

    JP-992

    		 Others Metabolic Disease Cardiovascular Disease
    Benfluorex (JP-992) is a hepatic nuclear factor 4 alpha (HNF4α) activator.
  • HY-B1058
    Benfluorex hydrochloride

    JP-992 hydrochloride

    		 Others Metabolic Disease Cardiovascular Disease
    Benfluorex hydrochloride (JP-992 hydrochloride) is a hepatic nuclear factor 4 alpha (HNF4α) activator.
  • HY-148370
    IONIS-FB-LRx

    RG6299

    		 Complement System Others
    IONIS-FB-LRx is a specific antisense oligonucleotide (ASO) targeting complement factor B (CFB). IONIS-FB-LRx effectively reduces circulating levels of CFB. IONIS-FB-LRx can be used for geographic atrophy (GA) research.
  • HY-N0277
    Aconine

    Jesaconine

    		 NF-κB Inflammation/Immunology Cancer
    Aconine inhibits receptor activator of nuclear factor (NF)-κB ligand (RANKL)-induced NF-κB activation.
  • HY-N10512
    Gangliotetraose

    Gg4

    		 Others Neurological Disease
    Gangliotetraose (Gg4) is a tetrasccharide, exhibits major components including GM1 and its sialylated derivatives. GM1 facilitates efflux of nuclear Ca 2+ and reduces the level of nuclear Ca 2+ that characterizes the differentiated neuron. GM1 affects neuronal plasticity and repair mechanisms, as well as neurotrophin release in the brain.
  • HY-B0470
    Neomycin sulfate

    		Bacterial Antibiotic Phospholipase Infection
    Neomycin sulfate, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin sulfate is a known phospholipase C (PLC) inhibitor. Neomycin sulfate potently inhibits both nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis.
  • HY-P99298
    Lampalizumab

    RG 7417; TNX 234; Anti-CFD Recombinant Antibody

    		 Complement System Inflammation/Immunology
    Lampalizumab (RG 7417) is a humanised monoclonal antibody targeting complement Factor D in the alternative complement pathway. Lampalizumab binds an exosite and sterically blocks Factor B access to the active site. Lampalizumab can be used for age-related macular degeneration (AMD) research.
  • HY-129492
    GNF4877

    		DYRK GSK-3 Metabolic Disease
    GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells).
  • HY-P3657A
    Biotin-KKKRKV acetate

    		Fluorescent Dye Cancer
    Biotin-KKKRKV acetate is the biotinylated KKKRKV acetate. KKKRKV is a nuclear localization signal (NLS) peptide derived from simian virus 40.
  • HY-112125A
    KRN2 bromide

    		Nuclear Factor of activated T Cells (NFAT) Inflammation/Immunology
    KRN2 (bromide) is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 0.1 μM.
  • HY-U00429
    NOT Receptor Modulator 1

    		Others Neurological Disease
    NOT Receptor Modulator 1 is a nuclear receptor NOT modulator extracted from patent WO 2008034974 A1, Example 39 in table1.
  • HY-123984
    LTβR-IN-1

    		NF-κB Metabolic Disease
    LTβR-IN-1 is a potent, selective lymphotoxin β receptor (LTβR) inhibitor. LTβR-IN-1 also selectively inhibits the nuclear translocation of p52 depended on TNF12A, instead of the nuclear translocation of p65 mediated by TNF-α receptor. LTβR-IN-1 regulates the NF-kB signaling pathway IN a ligand-independent manner.
  • HY-100523
    ML385

    		Keap1-Nrf2 Ferroptosis Cancer
    ML385 is a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM.
  • HY-107494A
    all-trans-4-Oxoretinoic acid

    all-trans 4-Keto Retinoic Acid

    		 Endogenous Metabolite Metabolic Disease
    all-trans-4-Oxoretinoic acid, an active metabolite of vitamin A, induces gene transcription via binding to nuclear retinoic acid receptors (RARs).
  • HY-122700
    Factor D inhibitor 6

    		Complement System Inflammation/Immunology
    Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.
  • HY-76847S
    Chenodeoxycholic Acid-d4

    CDCA-d4

    		 FXR Endogenous Metabolite Autophagy Metabolic Disease Cancer
    Chenodeoxycholic Acid-d4 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
  • HY-U00200
    Dicirenone

    SC26304

    		 Mineralocorticoid Receptor Metabolic Disease
    Dicirenone (SC26304) inhibits the effects of Aldosterone on urinary K +:Na + ratios and the binding of [ 3H]Aldosterone to renal cytoplasmic and nuclear receptors.
  • HY-76847S3
    Chenodeoxycholic acid-d5

    CDCA-d5

    		 FXR Endogenous Metabolite Autophagy Metabolic Disease Cancer
    Chenodeoxycholic acid-d5 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
  • HY-76847S2
    Chenodeoxycholic acid-13C

    CDCA-13C

    		 FXR Endogenous Metabolite Autophagy Metabolic Disease Cancer
    Chenodeoxycholic acid- 13C is the 13C-labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
  • HY-76847S1
    Chenodeoxycholic Acid-d9

    CDCA-d9

    		 FXR Endogenous Metabolite Autophagy Metabolic Disease Cancer
    Chenodeoxycholic Acid-d9 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
  • HY-N3269
    Methyl p-hydroxyphenyllactate

    		Others Others
    Methyl p-hydroxyphenyllactate (MeHPLA) is an important cell growth-regulating agent which binds to nuclear type II binding sites in normal and malignant cells.
  • HY-112056
    DIM-C-pPhCO2Me

    		Others Cancer
    DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist. Antineoplastic activity.
  • HY-N10062
    Amakusamine

    		RANKL/RANK Others
    Amakusamine inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced formation of multinuclear osteoclasts with an IC50 value of 10.5 μM in RAW264 cells.
  • HY-111498A
    RGX-104

    		LXR Cancer Inflammation/Immunology
    RGX-104 is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • HY-P1026
    NFAT Inhibitor-1

    VIVIT peptide

    		 Nuclear Factor of activated T Cells (NFAT) Inflammation/Immunology
    NFAT Inhibitor (VIVIT peptide) is a cell-permeable peptide inhibitor of nuclear factor of activated Tcells (NFAT) that selectively inhibits calcineurin-mediated dephosphorylation of NFAT.
  • HY-N2253
    Neoruscogenin

    		ROR Infection Neurological Disease
    Neoruscogenin, a member of the steroidal sapogenin family, is a bioavailable, potent, and high-affinity agonist of the nuclear receptor RORα (NR1F1).
  • HY-111492
    DIM-C-pPhOCH3

    		Others Cancer
    DIM-C-pPhOCH3 is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.
  • HY-A0162
    Quinupristin

    		Bacterial Infection
    Quinupristin is a streptogramin antibiotic. Quinupristin blocks peptide bond synthesis to prevent the extension of polypeptide chains and promote the detachment of incomplete protein chains in the bacterial ribosomal subunits .
  • HY-A0162A
    Quinupristin mesylate

    		Bacterial Infection
    Quinupristin mesylate is a streptogramin antibiotic. Quinupristin mesylate blocks peptide bond synthesis to prevent the extension of polypeptide chains and promote the detachment of incomplete protein chains in the bacterial ribosomal subunits.
  • HY-129610
    KB02-SLF

    		PROTACs FKBP Cancer
    KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF.
  • HY-N2148
    Cytosporone B

    Csn-B; Dothiorelone G

    		 Others Cancer
    Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC50 of 0.278 nM.
  • HY-120384
    AZD-0284

    		ROR Inflammation/Immunology
    AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis vulgaris and respiratory tract disorders treatment.
  • HY-N6774
    Cytochalasin C

    		Others Infection
    Cytochalasin C is a cell-permeable fungal toxin and induces the formation of nuclear rodlets. Cytochalasin C is 10 times less toxic in mice than is cytochalasin D.
  • HY-147533
    RORγt inverse agonist 30

    		ROR Inflammation/Immunology
    RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist with the IC50 of 46 nM. Targeting the nuclear receptor RORγt is effective in autoimmune disorders.
  • HY-14383
    Vosilasarm

    RAD140

    		 Androgen Receptor Endocrinology Neurological Disease
    Vosilasarm (RAD140) is a potent, orally active, nonsteroidal selective androgen receptor modulator (SARM) with a Ki of 7 nM. Vosilasarm shows good selectivity over other steroid hormone nuclear receptors.
  • HY-146494
    Androgen receptor antagonist 5

    		Androgen Receptor Cancer
    Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer.
  • HY-N4053
    Heraclenin

    		Nuclear Factor of activated T Cells (NFAT) Inflammation/Immunology
    Heraclenin, a natural furanocoumarin, significantly inhibits T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT).
  • HY-113212
    Ursocholic acid

    		Endogenous Metabolite Metabolic Disease
    Ursocholic acid, a bile acid found predominantly in bile of mammals, is transformed into deoxycholic acid by the intestinal microflora in mice. Ursodeoxycholic acid is an inhibitor of 7α-hydroxysteroid dehydrogenase and hepatocyte nuclear factor 1α.
  • HY-14645
    (-)-DHMEQ

    Dehydroxymethylepoxyquinomicin

    		 NF-κB Cancer Inflammation/Immunology
    (-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversible NF-κB inhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation of NF-κB and shows anti-inflammatory and anticancer activity.
  • HY-108529
    BMS493

    		RAR/RXR Metabolic Disease
    BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist. BMS493 increases nuclear corepressor interaction with RARs. BMS493 also could prevent retinoic acid-induced differentiation.
  • HY-112125
    KRN2

    		Nuclear Factor of activated T Cells (NFAT) Inflammation/Immunology
    KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 100 nM. KRN2 has potential to treat NFAT5-mediated Chronic Arthritis.
  • HY-N2682A
    (E)-Dehydrodiconiferyl alcohol

    		Carbonic Anhydrase Cancer
    (E)-Dehydrodiconiferyl alcohol behaves as good hCA IX and hCA XII dual inhibitors. And (E)-Dehydrodiconiferyl alcohol suppresses the NF-κB nuclear translocation in connective tissue of healing area.
  • HY-N4171
    Dihydrocucurbitacin B

    		Apoptosis Inflammation/Immunology
    Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activated T cells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity.
  • HY-120515
    7-Oxostaurosporine

    		PKC Cancer
    7-Oxostaurosporine is a potent protein kinase C (PKC) inhibitor that effectively inhibits tumor growth by inducing apoptosis and inhibiting the nuclear factor (NF)-κB/p-p65 pathway.
  • HY-N0290
    Mangiferin

    		NF-κB Keap1-Nrf2 Apoptosis Cancer
    Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50. Mangiferin exhibits antioxidant, antidiabetic, antihyperuricemic, antiviral, anticancer and antiinflammatory activities.
  • HY-101025
    Nrf2-IN-1

    		Keap1-Nrf2 Cancer
    Nrf2-IN-1 is an inhibitor of nuclear factor-erythroid 2-related factor 2 (Nrf2). Nrf2-IN-1 is developed for the research of acute myeloid leukemia (AML).
  • HY-110111
    T2AA

    		DNA/RNA Synthesis Cancer
    T2AA is a monoubiquitinated proliferating cell nuclear antigen (PCNA) inhibitor that prevents DNA repair, increases double-strand break (DSB) formation and promotes necroptosis and cell cycle arrest in G1 phase.
  • HY-148765
    CLK8

    		Cryptochrome Cancer Metabolic Disease
    CLK8 is a potent and specific CLOCK inhibitor that can disrupt the interaction between CLOCK and BMAL1 and interfere with nuclear translocation of CLOCK. CLK8 can be used for the research of disorders associated with dampened circadian rhythms.
  • HY-126245A
    Keap1-Nrf2-IN-1 TFA

    		Keap1-Nrf2 Metabolic Disease Inflammation/Immunology
    Keap1-Nrf2-IN-1 TFA (compound35) is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. Keap1-Nrf2-IN-1 TFA activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models.
  • HY-121607
    INI-43

    		Others Cancer
    INI-43, a Kpnβ1 inhibitor, interferes with the nuclear localization of Kpnβ1 and known Kpnβ1 cargoes, NFAT, NFκB, AP-1 and NFY.
  • HY-15731
    Estetrol

    		Estrogen Receptor/ERR Endogenous Metabolite Cardiovascular Disease
    Estetrol, a natural estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast.
  • HY-124012
    PCNA-I1

    		DNA/RNA Synthesis Cancer
    PCNA-I1 is a potent PCNA (proliferating cell nuclear antigen) inhibitor. PCNA-I1 directly binds PCNA trimers with a Kd of 0.41 μM and exhibits antitumor activity both in vitro and in vivo.
  • HY-P3838
    Protein Kinase C (gamma) Peptide

    		PKC Others
    Protein Kinase C γ Peptide is a peptide fragment of Protein Kinase Cγ. Protein Kinase Cγ is a protein causative for dominant ataxia, that can negatively regulate nuclear import of recessive-ataxia-related aprataxin.
  • HY-N0001
    (-)-Epicatechin

    (-)-Epicatechol; Epicatechin; epi-Catechin

    		 COX Ferroptosis Endogenous Metabolite Cancer Inflammation/Immunology
    (-)-Epicatechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 3.2 μM. (-)-Epicatechin inhibits the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.
  • HY-17363S
    Dimethyl fumarate-d6

    		Keap1-Nrf2 Inflammation/Immunology
    Dimethyl fumarate-d6 is a deuterium labeled Dimethyl fumarate. Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression[1][2][3][4][5][6].
  • HY-12825
    BHPI

    		Estrogen Receptor/ERR Cancer
    BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.
  • HY-143891
    Chromenone 1

    		TGF-β Receptor Others
    Chromenone 1 is a potent osteogenic bone morphogenetic protein (BMP) potentiator. Chromenone 1 exhibits a unique mode of action as it induces a pronounced, kinase-independent, negative TGFβ feedback that enhances nuclear BMP-Smad signaling outputs.
  • HY-135366
    HPN-01

    		IKK Inflammation/Immunology
    HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2.
  • HY-12684
    CH-223191

    		Aryl Hydrocarbon Receptor Cancer
    CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM.
  • HY-112126
    KRN5

    		Nuclear Factor of activated T Cells (NFAT) Inflammation/Immunology
    KRN5, a derivative of KRN2, is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM. KRN5 has potential to treat NFAT5-mediated Chronic Arthritis.
  • HY-135572
    TLX agonist 1

    		Others Cancer Neurological Disease
    TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity.
  • HY-12054
    Hesperadin

    		Aurora Kinase Autophagy Influenza Virus Parasite Cancer
    Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.
  • HY-103244
    CITCO

    		Apoptosis Cancer
    CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors.
  • HY-N0045
    Ginsenoside Rg1

    Panaxoside A; Panaxoside Rg1

    		 Amyloid-β NF-κB Apoptosis Inflammation/Immunology Neurological Disease Cancer
    Ginsenoside Rg1 is one of the major active components of Panax ginseng. Ginsenoside Rg1 ameliorates the impaired cognitive function, displays promising effects by reducing cerebral Aβ levels. Ginsenoside Rg1 also reduces NF-κB nuclear translocation.
  • HY-151101
    MS159

    		PROTACs Cancer
    MS159 is a potent nuclear receptor binding SET structural domain protein 2 (NSD2) PROTACdegrader. MS159 inhibits the growth of tumour cells. MS159 is a useful chemical tool for exploring the role of NSD2 in health and disease.
  • HY-151970
    STING-IN-4

    		STING Inflammation/Immunology
    STING-IN-4 (Compound 1) is a STING inhibitor that inhibits STING expression and hence reducing activation of STING and nuclear factor-κB (NF-κB) signaling. STING-IN-4 shows anti-inflammatory activity and can be used for the research of sepsis.
  • HY-14649G
    Retinoic acid

    Vitamin A acid; all-trans-Retinoic acid; ATRA; Vitamin A Acid

    		 RAR/RXR Cancer
    Retinoic acid (Vitamin A acid) (GMP) is Retinoic acid (HY-14649) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Retinoic acid is an agonist of RAR nuclear receptors.
  • HY-N6747
    Stauprimide

    		c-Myc Autophagy Cancer
    Stauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation. Stauprimide is a non-broad spectrum inhibitor that binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, which results in down-regulation of MYC transcription.
  • HY-144745
    HSR1304

    		NF-κB Cancer
    HSR1304 (Compound 5d) is a potent inhibitor of NFκB. The multifunctional transcription factor, nuclear factor-κB (NF-κB), is broadly involved in multiple human diseases, such as cancer and chronic inflammation. HSR1304 has the potential for the research of cancer diseases.
  • HY-135784
    OSMI-2

    		Acyltransferase Metabolic Disease
    OSMI-2 (Compound 1b) is a cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-2 increases detained intron splicing in cells.
  • HY-N10431
    Stigmane B

    		Keap1-Nrf2 Neurological Disease
    Stigmane B (Compound 2) is a nuclear factor E2-related factor (Nrf2) activator. Stigmane B downregulates apoptosis and reactive oxygen species (ROS) generation, and increases antioxidant enzyme activities. Stigmane B shows neuroprotective effects.
  • HY-100581
    CORM-3

    		NF-κB NOD-like Receptor (NLR) Inflammation/Immunology
    CORM-3, a carbon monoxide-releasing molecule, attenuates NF-κB p65 nuclear translocation, reduces ROS generation and enhances intracellular glutathione and superoxide dismutase levels. CORM-3 reduces NLRP3 inflammasome activation.
  • HY-14454
    TPh A

    Triphenyl Compound A

    		 Others Cancer
    TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells.
  • HY-113313
    Aldosterone

    		Endogenous Metabolite Cardiovascular Disease
    Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level.
  • HY-139464
    Q134R

    		Nuclear Factor of activated T Cells (NFAT) Neurological Disease
    Q134R, a neuroprotective hydroxyquinoline derivative that suppresses nuclear factor of activated T cell (NFAT) signaling. Q134R can across blood-brain barrier. Q134R has the potential for Alzheimer's disease (AD) and aging-related disorders research.
  • HY-N1956
    Rubiadin-1-methyl ether

    		NF-κB Metabolic Disease
    Rubiadin-1-methyl ether is a natural anthraquinone isolated from Morinda officinalis How, and inhibits osteoclastic bone resorption via inhibition on the phosphorylation of NF-κB p65 and the degradation of IκBα as well as decrease in the nuclear translocation of p65.
  • HY-135825
    TFEB activator 1

    		Autophagy Neurological Disease
    TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment.
  • HY-125355
    SEC

    		Apoptosis Cancer
    SEC induces activation of ANXA7 GTPase via the AMPK/mTORC1/STAT3 signaling pathway. SEC selectively promotes apoptosis in cancer cells, expressing a high level of ITGB4 by inducing ITGB4 nuclear translocation.
  • HY-N2166
    Tomatine

    α-Tomatine; Lycopersicin; Tomatin

    		 Proteasome Apoptosis Neurological Disease
    Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine also inhibits 20S proteasome activity.
  • HY-N10578
    Genkwadaphnin

    		Others Cancer
    Genkwadaphnin is a daphnane diterpenoid, targeting of importin-β1 to reduce the nuclear accumulation of key CRPC drivers, and shut down their downstream oncogenic signaling. Genkwadaphnin shows potent anti-tumor activity and inhibits castration-resistant prostate cancer (CRPC) in vivo in mice.
  • HY-P1566
    MPG, HIV related

    		HIV Infection
    MPG, HIV related is 27-aa peptide, derived from both the nuclear localisation sequence of SV40 large T antigen and the fusion peptide domain of HIV-1 gp41 and is a potent delivery agent for the generalised delivery of nucleic acids and of oligonucleotides into cultured cells.
  • HY-103394
    TC HSD 21

    		Others Cancer
    TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC50 of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.
  • HY-N0613
    Sauchinone

    		NF-κB Inflammation/Immunology
    Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity.
  • HY-13676
    Megestrol acetate

    		Progesterone Receptor Autophagy HIV Endocrinology Cancer
    Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway.
  • HY-N0191
    Andrographolide

    Andrographis

    		 NF-κB SARS-CoV Influenza Virus Autophagy Parasite Cancer Infection Inflammation/Immunology
    Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.
  • HY-135785
    OSMI-3

    		Acyltransferase Metabolic Disease
    OSMI-3 (Compound 2b) is a potent, long-lasting, and cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-3 increases detained intron splicing in cells.
  • HY-15731S
    Estetrol-d4

    		Estrogen Receptor/ERR Endogenous Metabolite Cardiovascular Disease
    Estetrol-d4 is the deuterium labeled Estetrol. Estetrol, a natural estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast[1][2].
  • HY-13593
    Chlorambucil

    CB-1348; WR-139013

    		 DNA Alkylator/Crosslinker Cancer
    Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease.
  • HY-146275
    LXRβ agonist-3

    		LXR Cancer
    LXRβ agonist-3 (compound 4-13) is a potent and selective LXRβ (liver X receptor β) agonist, with an EC50 of 0.095 μM. LXRβ agonist-3 efficiently inhibits U87EGFRvIII cell, with an IC50 of 3.75 μM. LXRβ agonist-3 shows antitumor activity, and can inhibit glioblastoma.
  • HY-125218
    PARP11 inhibitor ITK7

    ITK7

    		 PARP Cancer
    PARP11 inhibitor ITK7 (ITK7) is a potent and selective PARP11 inhibitor. PARP11 inhibitor ITK7 can potently inhibit PARP11 with an IC50 value of 14 nM. PARP11 inhibitor ITK7 can be used for the research of cellular localization.
  • HY-15310
    Ivermectin

    MK-933

    		 Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Bacterial Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
  • HY-136427
    KRM-III

    		Nuclear Factor of activated T Cells (NFAT) Inflammation/Immunology
    KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity.
  • HY-P4101
    Cys(Npys)-TAT (47-57)

    		HIV Infection
    Cys(Npys)-TAT (47-57) is a peptide fragment of TAT peptide and it is able to interact with plasmid DNA electrostatically. Cys(Npys)-TAT (47-57) is corresponding to the transduction domain of TAT with an activated cysteine residue C. TAT is a small nuclear transcriptional activator protein encoded by HIV-1.
  • HY-139833
    Anti-inflammatory agent 6

    		NF-κB IKK Inflammation/Immunology
    Anti-inflammatory agent 6 blocks the phosphorylation of I kappa b kinase α/β (IKKα/β), IκBα, and nuclear factor kB p65 (NF-κB p65) which is a key controller of inflammation, thereby showing anti-inflammatory potential.
  • HY-W019721
    Cyclosporin D

    		Nuclear Factor of activated T Cells (NFAT) Inflammation/Immunology
    Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A. Cyclosporin A is a potent immunosuppressant drug, suppress T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc).
  • HY-114597
    PKF050-638

    		HIV CRM1 Cancer
    PKF050-638 is a potent and selective inhibitor of HIV-1 Rev (IC50=0.04 μM). PKF050-638 inhibits the CRM1-mediated Rev nuclear export by disrupting CRM1-NES interaction.
  • HY-N2112
    Glaucocalyxin A

    		PI3K Akt Apoptosis Cancer
    Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect.
  • HY-144339
    AhR agonist 2

    		Aryl Hydrocarbon Receptor Others
    AhR agonist 2 (Compound 12a) is a potent agonist of aryl hydrocarbon receptor (AhR) with an EC50 of 0.03 nM. AhR agonist 2 induces rapid nuclear enrichment of AhR, triggers the transcription of downstream genes and promote skin barrier repair. AhR agonist 2 has the potential for the research of psoriasis.
  • HY-P2657
    Verucopeptin

    		HIF/HIF Prolyl-Hydroxylase Proton Pump Endogenous Metabolite Cancer
    Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
  • HY-B0356B
    Ciprofloxacin hydrochloride monohydrate

    Bay-09867 hydrochloride monohydrate

    		 Topoisomerase Apoptosis Antibiotic Bacterial Mitochondrial Metabolism Reactive Oxygen Species Infection Cancer
    Ciprofloxacin (Bay-09867) hydrochloride monohydrate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin hydrochloride monohydrate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin hydrochloride monohydrate has anti-proliferative activity and induces apoptosis. Ciprofloxacin hydrochloride monohydrate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
  • HY-147228
    NR2F6 modulator-1

    		Others Cancer Inflammation/Immunology
    NR2F6 modulator-1 is a potent nuclear receptor subfamily 2, group F, member 6 (NR2F6) modulator. NR2F6 modulator-1 can be used for researching immune modulation and modulation of cancer stem cell activity.
  • HY-122958
    Peucedanocoumarin III

    		α-synuclein Neurological Disease
    Peucedanocoumarin III is an inhibitor of α-synuclein and Huntington protein aggregates that enhances the clearance of nuclear and cytoplasmic β23 aggregates and prevents cytotoxicity induced by disease-associated proteins (i.e., mutant Huntington proteins and α-synuclein). Peucedanocoumarin III may be used in Parkinson's disease research.
  • HY-13982
    JSH-23

    		NF-κB Cancer Metabolic Disease Inflammation/Immunology
    JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation.
  • HY-101402
    Cyclo(his-pro)

    Cyclo(histidyl-proline); Histidylproline diketopiperazine

    		 NF-κB Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
  • HY-N0643
    Carnosol

    		Ribosomal S6 Kinase (RSK) Keap1-Nrf2 Endogenous Metabolite Cancer
    Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM. Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1).
  • HY-B0356
    Ciprofloxacin

    Bay-09867

    		 Topoisomerase Apoptosis Antibiotic Bacterial Mitochondrial Metabolism Reactive Oxygen Species Cancer Infection
    Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and induces apoptosis. Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
  • HY-N2106
    Dehydroevodiamine

    		NF-κB COX PGE synthase NO Synthase Inflammation/Immunology
    Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.
  • HY-19979
    RCM-1

    		Others Cancer
    RCM-1 is a forkhead box M1 (FOXM1) inhibitor with an EC50 of 0.72 μM in U2OS cells. RCM-1 blocks the nuclear localization and increased the proteasomal degradation of FOXM1. RCM-1 can be used for asthma and other chronic airway diseases research.
  • HY-30267
    4-Hydroxyphenyl acetate

    4-HPA; 4-Acetoxyphenol

    		 Endogenous Metabolite Others
    4-Hydroxyphenyl acetate (4-HPA) is a natural antioxidant and protects cells from oxidative stress-induced necrosis. 4-Hydroxyphenyl acetate blocks the increase of cellular ROS induced by oxidative stress, and up-regulates NQO1 and HO-1 genes by stabilizing and inducing the nuclear translocation of NRF2 transcription factor.
  • HY-118482
    Sauristolactam

    Saurolactam

    		 Others Neurological Disease
    Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells. Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation.
  • HY-113313S1
    Aldosterone-d7

    		Endogenous Metabolite Cardiovascular Disease
    Aldosterone-d7 is the deuterium labeled Aldosterone. Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level[1][2].
  • HY-115579
    MALAT1-IN-1

    		Others Cancer
    MALAT1-IN-1 (compounds 5) is a potent and specific Malat1 (Metastasis-associated lung adenocarcinoma transcript 1) inhibitor. MALAT1-IN-1 modulated Malat1 downstream genes in a dose-dependent manner without affecting expression of nuclear enriched abundant transcript 1 (Neat1) .
  • HY-152093
    YL-939

    		Ferroptosis Cancer
    YL-939 is a potent ferroptosis inhibitor. YL-939 inhibits ferroptosis by targeting the PHB2/ferritin/iron axis.
  • HY-W002299
    Boc-D-Leucine monohydrate

    Boc-D-Leu-OH hydrate

    		 Amino Acid Derivatives Neurological Disease
    Boc-D-Leucine monohydrate (Boc-D-Leu-OH hydrate) is an N-Boc-protected form of D-Leucine (L330150). D-Leucine is an unnatural isomer of L-Leucine (L330110) that acts as an auto-inhibitor of lactic streptococci. D-Leucine shows potent anti-seizure effect.
  • HY-N0001S
    (±)-Epicatechin-13C3

    		Ferroptosis Endogenous Metabolite COX Cancer Inflammation/Immunology
    (±)-Epicatechin- 13C3 is the 13C labeled (±)-Epicatechin. (-)-Epicatechin (HY-N0001) inhibits cyclooxygenase-1 (COX-1) with an IC50 of 3.2 μM. (-)-Epicatechin inhibits the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB[1].
  • HY-111226
    GSK5182

    		Estrogen Receptor/ERR Reactive Oxygen Species Cancer Cardiovascular Disease
    GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC).
  • HY-13676S
    Megestrol acetate-d3

    		Progesterone Receptor Autophagy HIV Endocrinology Cancer
    Megestrol acetate-d3 is the deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
  • HY-122054
    BPK-29

    		Others Cancer
    BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
  • HY-101402A
    Cyclo(his-pro) TFA

    Cyclo(histidyl-proline) TFA; Histidylproline diketopiperazine TFA

    		 NF-κB Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) TFA could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) TFA can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
  • HY-146027
    Androgen receptor antagonist 4

    		Androgen Receptor Cancer
    Androgen receptor antagonist 4 (Compound AT2) is an androgen receptor (AR) antagonist with an IC50 of 0.15 μM. Androgen receptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgen receptor antagonist 4 shows anticancer activities.
  • HY-W040298
    Ciprofloxacin lactate

    Bay-09867 lactate

    		 Topoisomerase Apoptosis Antibiotic Bacterial Mitochondrial Metabolism Reactive Oxygen Species Cancer Infection
    Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
  • HY-125209A
    TH5427 hydrochloride

    		DNA/RNA Synthesis Cancer
    TH5427 hydrochloride is a potent, selective NUDT5 inhibitor (IC50=29 nM). TH5427 hydrochloride shows an apparent 690-fold selectivity for NUDT5 over MTH1. TH5427 hydrochloride blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells.
  • HY-B0356A
    Ciprofloxacin monohydrochloride

    Bay-09867 monohydrochloride

    		 Topoisomerase Apoptosis Antibiotic Bacterial Mitochondrial Metabolism Reactive Oxygen Species Infection Cancer
    Ciprofloxacin (Bay-09867) monohydrochloride is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin monohydrochloride induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin monohydrochloride has anti-proliferative activity and induces apoptosis. Ciprofloxacin monohydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.
  • HY-146384
    CRM1 degrader 1

    		CRM1 Cancer
    CRM1 degrader 1 (1l) is a low toxic chromosome region maintenance 1 (CRM1) degrader. CRM1 is the sole nuclear exporter of several tumor suppressor, a growth regulatory protein as an attractive cancer drug target. CRM1 degrader 1 induces the apoptosis in gastric carcinoma and selectively inhibits proliferation of gastric cancer.
  • HY-122054A
    BPK-29 hydrochloride

    		Others Cancer
    BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
  • HY-14649
    Retinoic acid

    Vitamin A acid; all-trans-Retinoic acid; ATRA

    		 RAR/RXR PPAR Endogenous Metabolite Autophagy Cancer
    Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
  • HY-P3229
    SN52

    		NF-κB Cancer
    SN52 is a potent, competitive, and cell-permeable inhibitor of NF-κB2. SN52 is a variant of the SN50 peptide and inhibits the nuclear translocation of p52-RelB heterodimers. SN52 has a strong radiosensitization effect on prostate cancer cells. SN52 can be used for cancer research.
  • HY-100468
    REV7/REV3L-IN-1

    		Others Cancer
    REV7/REV3L-IN-1 is a REV7/REV3L interaction inhibitor with an IC50 of 78 μM, which directly binds to REV7 in nuclear magnetic resonance analyses, and inhibits the reactivation of a reporter plasmid containing an interstrand crosslink (ICL) in between the promoter and reporter regions.
  • HY-13676S1
    Megestrol acetate-d3-1

    		Progesterone Receptor Autophagy HIV Endocrinology Cancer
    Megestrol acetate-d3-1 is deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
  • HY-16079
    AZD3514

    		Androgen Receptor Cancer
    AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer.
  • HY-126113
    KIN101

    		Influenza Virus HCV Infection
    KIN101 is a potent RNA viral inhibitor with IC50s of 2 μM, >5 μM for influenza virus and Dengue virus (DNV), respectively. KIN101, an isoflavone agonist of IRF-3 dependent signaling, induces IRF-3 nuclear translocation. KIN101 has broad-spectrum activity against RNA viruses.
  • HY-121523
    MIND4-17

    		Keap1-Nrf2 Metabolic Disease
    MIND4-17 is a potent NRF2 activator that covalently modifies a C151 residue of Keap1. MIND4-17 disrupts Keap1-Nrf2 association, leading to Nrf2 protein stabilization and nuclear translocation. MIND4‐17 exerts potent antioxidant activity.
  • HY-120087
    KG-548

    		HIF/HIF Prolyl-Hydroxylase Cancer
    KG-548 is an ARNT/TACC3 disruptor and a HIF-1α inhibitor. KG-548 directly interferes with ARNT/TACC3 complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is the aryl hydrocarbon receptor nuclear translocator, also known as HIF-β.
  • HY-16466
    Spliceostatin A

    		Others Cancer
    Spliceostatin A, the FR901464 (HY-16212) methylated derivative, is a potent anti-tumor agent. Spliceostatin A inhibits splicing and promotes pre-mRNA accumulation by binding SF3B1. SF3B1 is a subcomplex of U2 small nuclear ribonucleoprotein in the spliceosome. Spliceostatin A induces Apoptosis in chronic lymphocytic leukemia (CLL) cells.
  • HY-147369
    NFATc1-IN-1

    		Nuclear Factor of activated T Cells (NFAT) Others
    NFATc1-IN-1 (compound A04) is a potent inhibitor of RANKL-induced osteoclast formation, with an IC50 of 1.57 μM. NFATc1-IN-1 shows anti-osteoclastogenic effects through reducing the RANKL-induced nuclear translocation of NFATc1. NFATc1-IN-1 can be used for osteoclastic diseases research.
  • HY-B0589C
    (3S,5S)-Atorvastatin

    		Cytochrome P450 Metabolic Disease
    (3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
  • HY-D0093
    Ethidium homodimer

    EthD-1

    		 DNA Stain Others Others
    Ethidium homodimer (EthD-1) is a cell-membrane impermeant nucleic acid fluorochrome with high affinity for DNA. Ethidium homodimer can be used to test cell viability.
  • HY-120785
    SR1555

    		ROR Inflammation/Immunology
    SR1555 is a specific retinoic acid receptor-related orphan nuclear receptor γ (RORγ) inverse agonist with an IC50 value of 1 μM. SR1555 not only inhibits TH17 cell development and function but also increases the frequency of T regulatory cells, as well as inhibits the expression of IL-17. SR1555 can be used for researching autoimmune diseases.
  • HY-125209
    TH5427

    		Others Cancer
    TH5427 is a promising, targeted inhibitor that can be used to further study NUDT5 activity and ADP-ribose metabolism. TH5427, blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells. NUDT5 is recently identified as a rheostat of hormone-dependent gene regulation and proliferation in breast cancer cells.
  • HY-N1987
    Cucurbitacin IIb

    		Apoptosis Inflammation/Immunology
    Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α.
  • HY-N7434
    N-Nitrosodiethylamine

    Diethylnitrosamine

    		 DNA/RNA Synthesis Cancer
    N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
  • HY-114413
    YZ129

    		HSP Apoptosis Cancer
    YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation. YZ129-induced GBM cell-cycle arrest at the G2/M phase promotes apoptosis and inhibited tumor cell proliferation and migration.
  • HY-135691
    hnRNPK-IN-1

    		c-Myc Apoptosis Cancer
    hnRNPK-IN-1 is a heterogeneous nuclear ribonucleoprotein K (hnRNPK) binding ligand with Kd values of 4.6 μM and 2.6 μM measured with SPR and MST, respectively. hnRNPK-IN-1 inhibits c-myc transcription by disrupting the binding of hnRNPK and c-myc promoter. hnRNPK-IN-1 induces Hela cells apoptosis and has strongly anti-tumor activities.
  • HY-P1439A
    RS 09 TFA

    		Toll-like Receptor (TLR) Inflammation/Immunology
    RS 09 TFA is a TLR4 agonist. RS 09 TFA promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 TFA acts as an adjuvant in vivo; RS 09 TFA enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.
  • HY-131236
    EBNA1-IN-SC7

    		EBV Cancer
    EBNA1-IN-SC7 (compound SC7) is a selective Epstein-Barr nuclear antigen 1 (EBNA1) inhibitor that interferes with EBNA1-DNA binding activity with an IC50 value of 23 μM. EBNA1-IN-SC7 is used in EBV (Epstein-Barr virus)-related cancer research.
  • HY-112338
    C188

    CPD188

    		 STAT Cancer
    C188 is a STAT3 inhibitor that inhibits IL-6-stimulated STAT3 phosphorylation and nuclear translocation in HepG2 cells by targeting STAT3 SH2 domain peptide-binding pocket. C188, in particular, was highly active in inducing apoptosis of the breast cancer cell line MB-MDA-468 in vitro (EC50= 0.7 μM).
  • HY-P1832
    PTD-p65-P1 Peptide

    		NF-κB Apoptosis Cancer Inflammation/Immunology
    PTD-p65-P1 Peptide is a potent, selective nuclear transcription factor NF-κB inhibitor and derives from the p65 subunit of NF-κB amino acid residues 271-282, which selectively inhibits NF-κB activation induced by various inflammatory stimulation, down-regulate NF-κB-mediated gene expression and up-regulate apoptosis.
  • HY-N6979
    Crustecdysone

    20-Hydroxyecdysone

    		 Caspase Autophagy Endogenous Metabolite Cardiovascular Disease
    Crustecdysone (20-Hydroxyecdysone) is a naturally occurring ecdysteroid hormone isolated from Serratula coronata which controls the ecdysis (moulting) and metamorphosis of arthropods, it inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP. Crustecdysone exhibits regulatory or protective roles in the cardiovascular system. Crustecdysone is an active metabolite of Ecdysone (HY-N0179).
  • HY-113439
    12-HETE

    		Apoptosis Inflammation/Immunology Cardiovascular Disease
    12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway.12-HETE has both anti-thrombotic and pro-thrombotic effects. 12-HETE is a neuromodulator.
  • HY-P1832A
    PTD-p65-P1 Peptide TFA

    		NF-κB Apoptosis Cancer Inflammation/Immunology
    PTD-p65-P1 Peptide TFA is a potent, selective nuclear transcription factor NF-κB inhibitor and derives from the p65 subunit of NF-κB amino acid residues 271-282, which selectively inhibits NF-κB activation induced by various inflammatory stimulation, down-regulate NF-κB-mediated gene expression and up-regulate apoptosis.
  • HY-120836
    AOH1160

    		DNA/RNA Synthesis Apoptosis Cancer
    AOH1160 is a potent, first-in-class, orally available small molecule proliferating cell nuclear antigen (PCNA) inhibitor, interferes with DNA replication, blocks homologous recombination-mediated DNA repair, causes cell-cycle arrest and induces apoptosis. AOH1160 selectively kills many types of cancer cells (mean GI50=330 nM) without causing significant toxicity to a broad range of nonmalignant cells.
  • HY-10496
    SC75741

    		NF-κB Influenza Virus Infection Cancer
    SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65. SC75741 blocks influenza viruses (IV) replication. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins.
  • HY-W011220
    Ciglitazone

    ADD-3878; U-63287

    		 PPAR Cancer Cardiovascular Disease
    Ciglitazone is a potent and selective PPARγ agonist (EC50=3 μM). Ciglitazone inhibits proliferation and differentiation of th17 cells. Ciglitazone is a hypoglycemic agent orally active in the obese-hyperglycemic animal models. Ciglitazone induces apoptosis accompanied by activation of p38 MAPK and nuclear translocation of apoptosis inducing factor (AIF) in opossum kidney (OK) renal epithelial cells.
  • HY-139562
    BMS-986318

    		FXR Metabolic Disease
    BMS-986318 is a potent nonbile acid FXR agonist with EC50s of 53 and 350 nM in the FXR Gal4 and SRC-1 recruitment assays, respectively. BMS-986318 has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis.BMS-986318 can be used for the research of nonalcoholic steatohepatitis.
  • HY-108694
    γ-Tocotrienol

    		Endogenous Metabolite NF-κB Metabolic Disease Inflammation/Immunology
    γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment.
  • HY-131445
    RJW100

    		MicroRNA Cancer Endocrinology
    RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC50s of 6.6 and 7.5, respectively. RJW100 also causes strong activation of the miR-200c (miRNA-200c, microRNA-200c) promoter.
  • HY-151263
    G4/HDAC-IN-1

    		HDAC G-quadruplex Cancer
    G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer.
  • HY-N6953
    Garcinone D

    		STAT Keap1-Nrf2 Reactive Oxygen Species Neurological Disease
    Garcinone D, a natural xanthone from mangosteen, promotes the proliferation of C17.2 neural stem cell. Garcinone D increases the protein levels of phosphorylated signal transducer and activator of transcription 3 (p-STAT3), Cyclin D1 and nuclear factor erythroid 2-related factor (Nrf2), heme oxygenase-1 (HO-1) in concentration- and time- dependent manners.
  • HY-100609
    4-P-PDOT

    		Melatonin Receptor Neurological Disease
    4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity).
  • HY-123611
    Supinoxin

    RX-5902

    		 DNA/RNA Synthesis Apoptosis Cancer
    Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM.
  • HY-148418
    TUG-499

    		Free Fatty Acid Receptor Metabolic Disease
    TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes.
  • HY-N7434S
    N-Nitrosodiethylamine-d4

    Diethylnitrosamine-d4

    		 DNA/RNA Synthesis Cancer
    N-Nitrosodiethylamine-d4 is the deuterium labeled N-Nitrosodiethylamine[1]. N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
  • HY-12276
    MALT1 inhibitor MI-2

    		MALT1 Cancer
    MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals.
  • HY-N7434S1
    N-Nitrosodiethylamine-d10

    Diethylnitrosamine-d10

    		 DNA/RNA Synthesis Cancer
    N-Nitrosodiethylamine-d10 is the deuterium labeled N-Nitrosodiethylamine[1]. N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
  • HY-P1920
    CEF19, Epstein-Barr Virus latent NA-3A (458-466)

    		EBV Inflammation/Immunology
    CEF19, Epstein-Barr Virus latent NA-3A (458-466) is a single peptide epitope, YPLHEQHGM, representing residues 458-466 of the type 1 Epstein-Barr Virus (EBV) nuclear antigen 3A protein (B95.8 strain). CEF19, Epstein-Barr Virus latent NA-3A (458-466) can significantly affect cytotoxic T-lymphocyte (CTL) recognition.
  • HY-N2056
    11-​Keto-​beta-​boswellic acid

    11-Keto-β-boswellic acid

    		 Lipoxygenase Leukotriene Receptor NF-κB Cancer
    11-Keto-beta-boswellic acid (11-Keto-β-boswellic acid) is a pentacyclic triterpenic acid of the oleogum resin from the bark of the Boswellia serrate tree, popularly known as Indian Frankincense. 11-Keto-beta-boswellic acid has the anti-inflammatory activity is primarily due to inhibit 5-lipoxygenase (5-LOX) and subsequent leukotriene and nuclear factor-kappa B (NF-κB) activation and tumor necrosis factor alpha generation production.
  • HY-133807
    Benpyrine

    		TNF Receptor Inflammation/Immunology
    Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 µM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.
  • HY-137818
    SR19881

    		Estrogen Receptor/ERR Cardiovascular Disease
    SR19881 is a potent dual agonist of ERRγ and ERRβ, with EC50 values of 0.39 and 0.63 μM, respectively.
  • HY-151380
    LANA-DNA-IN-1

    		Others Infection
    LANA-DNA-IN-1 is a potent LANA-DNA inhibitor. LANA-DNA-IN-1 has inhibition activity for LBS2, LBS1 and LBS3 with IC50 values of 8 μM, 9μM and 8μM. LANA-DNA-IN-1shows against wild-type LANA with IC50 value of 53 μM. LANA-DNA-IN-1 can be used for the research of infection.
  • HY-14649S2
    11-cis-Retinoic Acid-d5

    		RAR/RXR PPAR Endogenous Metabolite Autophagy Cancer
    11-cis-Retinoic Acid-d5 is the deuterium labeled Retinoic acid. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[1][2].
  • HY-126245
    Keap1-Nrf2-IN-1

    		Keap1-Nrf2 Metabolic Disease Inflammation/Immunology
    Keap1-Nrf2-IN-1 is a Keap1 (Kelch-like ECH-associated protein 1)-Nrf2 (nuclear factor erythroid 2-related factor 2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. Keap1-Nrf2-IN-1 activates Nrf2-regulated cytoprotective response and antagonizes Acetaminophen-induced liver injury.
  • HY-131445A
    SS-RJW100

    		Others Metabolic Disease Inflammation/Immunology
    SS-RJW100 is a enantiomer of RJW100, which is a racemic agonist of nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). SS-RJW100 promotes recruitment of coregulator protein fragments in vitro, recruits the transcriptional intermediary factor 2 (Tif2) coactivator to LRH-1. SS-RJW100 diminishes LRH-1 allosteric activation networks, shows poor thermal stability.
  • HY-148552
    Anti-inflammatory agent 35

    		p38 MAPK ERK NF-κB Interleukin Related TNF Receptor Inflammation/Immunology
    Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue with anti-inflammatory activity. Anti-inflammatory agent 35 blocks mitogen-activated protein kinase (MAPK) signaling and p65 nuclear translocation of NF-kB. Anti-inflammatory agent 35 also inhibits yellow neutrophil infiltration and pro-inflammatory cytokine production. Anti-inflammatory agent 35 significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI) in vivo.
  • HY-N10264
    Avrainvillamide

    (+)-Avrainvillamide; CJ-17,665

    		 Antibiotic Cancer Infection
    Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-drug resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively.
  • HY-147082
    GA-017

    		YAP Cancer
    GA-017 is a potent and selective LATS1 and LATS2 (large tumor suppressor kinase 1/2) inhibitor, with IC50 values of 4.10 and 3.92 nM, respectively. GA-017 is an activator of cell proliferation. GA-017 promotes YAP/TAZ activation and nuclear translocation. GA-017 promotes cell growth under 3D culture conditions. GA-017 enhances the ex vivo formation of mouse intestinal organoids.
  • HY-114263
    NXT629

    		PPAR Cancer
    NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models.
  • HY-N2118
    Bilobetin

    		PPAR PKA Metabolic Disease
    Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.
  • HY-15586
    L67

    DNA Ligase Inhibitor

    		 DNA/RNA Synthesis Caspase Apoptosis Reactive Oxygen Species Cancer
    L67 (DNA Ligase Inhibitor) is a competitive DNA ligase inhibitor that effectively inhibits DNA ligases I/III (both IC50 are 10 μM). L67 (DNA Ligase Inhibitor) can cause nuclear DNA damage by reducing levels of mitochondrial DNA and increasing levels of mitochondrially-generated ROS. L67 (DNA Ligase Inhibitor) also activates the Caspase 1-dependent apoptosis pathway in cancer cells, can be used in cancer research.
  • HY-14649S3
    Retinoic acid-d6

    		RAR/RXR PPAR Autophagy Endogenous Metabolite Cancer
    Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[2][3][4][5][6][7].
  • HY-113439S
    12-HETE-d8

    		Apoptosis Inflammation/Immunology Cardiovascular Disease
    12-HETE-d8 is the deuterium labeled 12-HETE. 12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway[1].12-HETE has both anti-thrombotic and pro-thrombotic effects[2]. 12-HETE is a neuromodulator[3].
  • HY-N0811
    Anemarsaponin B

    		NO Synthase COX NF-κB MEK Inflammation/Immunology
    Anemarsaponin B is a steroidal saponin. Anemarsaponin B decreases the protein and mRNA levels of iNOS and COX-2. Anemarsaponin B reduces the expressions and productions of pro-inflammatory cytokines, including TNF-a and IL-6. Anemarsaponin B inhibits the nuclear translocation of the p65 subunit of NF-κB by blocking the phosphorylation of IκBα. Anemarsaponin B also inhibits the phosphorylation of MAP kinase kinases 3/6 (MKK3/6) and mixed lineage kinase 3 (MLK3). Anti-inflammatory effect .
  • HY-131445B
    RR-RJW100

    		Others Metabolic Disease
    RR-RJW100, the enantiomer of RJW100, is an nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1) agonist. RJW100 can be synthesized as two enantiomers, RR-RJW100 and SS-RJW100, with RR-RJW100 shown to be the more potent LRH-1 agonist. RR-RJW100 is involved in the regulation of metabolic homeostasis and is used in studies of diabetes, liver disease and inflammatory bowel disease.
  • HY-N0632
    Esculentoside A

    		COX NF-κB Inflammation/Immunology
    Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta. Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models, has selective inhibitory activity towards cyclooxygenase-2 (COX-2). Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways.
  • HY-114208
    BI-9321

    		Histone Methyltransferase Cancer
    BI-9321 is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells.
  • HY-114208A
    BI-9321 trihydrochloride

    		Histone Methyltransferase Cancer
    BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells.
  • HY-N1445
    Isoquercetin

    Quercetin 3-glucoside

    		 NF-κB NO Synthase Inflammation/Immunology Cancer
    Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway. Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies.
  • HY-143243
    Antioxidant agent-5

    		Apoptosis NF-κB Keap1-Nrf2 Reactive Oxygen Species Cardiovascular Disease
    Antioxidant agent-5 (compound D-6) is a potent antioxidant agent. Antioxidant agent-5 can inhibit oxLDL (oxidized low-density lipoprotein)-induced apoptosis and the expression of ICAM-1 and VCAM-1 in VECs. Antioxidant agent-5 suppresses oxLDL-induced increase of ROS level and nuclear translocation of NF-κB. Antioxidant agent-5 protects against oxLDL-induced endothelial injury by activating Nrf2/HO-1 anti-oxidation pathway.
  • HY-147105
    LRH-1 modulator-1

    		Others Inflammation/Immunology
    LRH-1 modulator-1 (compound 6N) is a potent LRH-1 (liver receptor homolog-1) modulator/agonist. LRH-1 modulator-1 shows anti-inflammatory effects in intestinal organoids. LRH-1 modulator-1 induces anti-inflammatory cytokine IL-10, and reduces inflammatory cytokine IL-1b and TNFa.
  • HY-149913
    NR2F1 agonist 1

    		Others Cancer
    NR2F1 agonist 1, a nuclear receptor NR2F1 agonist, specifically activates dormancy programs in malignant cells. NR2F1 agonist 1 up-regulates NR2F1 and downstream target genes that regulate dormancy. NR2F1 agonist 1 induces neural crest-like and growth suppression in head and neck squamous cell carcinoma (HNSCC) via NR2F1 activation. NR2F1 agonist 1 inhibits tumor growth in a mouse primary tumor model.
  • HY-100008
    Peretinoin

    NIK333

    		 RAR/RXR SphK Autophagy HCV Cancer Infection
    Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM.
  • HY-10108
    LY294002

    		PI3K Casein Kinase DNA-PK Apoptosis Autophagy Cancer Infection
    LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator.
  • HY-N6769
    Radicicol

    Monorden

    		 HSP Bacterial Antibiotic Parasite Infection
    Radicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation. Radicicol exhibits inhibition on PDK with IC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB. Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM.
  • HY-120072
    PF-3450074

    PF-74

    		 HIV Infection
    PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle. CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
  • HY-N0515
    Ophiopogonin D

    		PPAR NF-κB Calcium Channel Inflammation/Immunology Cardiovascular Disease
    Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca 2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.
  • HY-121900
    LT175

    		PPAR Endocrinology Metabolic Disease
    LT175, a dual PPARα/γ ligand, is an orally active partial agonist against PPARγ(hPPARα:EC50=0.22 μm; mPPARα:EC50=0.26 μm; hPPARγ:EC50=0.48 μm). LT175 interacts with PPARγ and affects the recruitment of the coregulators cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). LT175 interacts with PPARγ in a hydrophobic region called “diphenyl pocket”. LT175 has potent insulin-sensitizing effects and reduced adipogenic properties.
  • 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.
  • HY-10108A
    LY294002 hydrochloride

    		PI3K Casein Kinase DNA-PK Apoptosis Cancer
    LY294002 hydrochloride is a potent and broad-spectrum PI3K inhibitor, with IC50 values of 0.5, 0.57, and 0.97 μM for P110α, P110δ and P110β, respectively. LY294002 hydrochloride also inhibits CK2 with an IC50 of 98 nM. LY294002 hydrochloride can be used for pancreatic cancer research.