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CAR Inhibitors

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製品番号 製品名 Target 研究分野 構造式
  • HY-103244
    CITCO
    3 Publications Verification

    		 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 .
    CITCO
  • HY-B0349
    Meclizine dihydrochloride
    4 Publications Verification

    Meclozine dihydrochloride

    		 Histamine Receptor Apoptosis Neurological Disease Endocrinology Cancer
    Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .
    Meclizine dihydrochloride
  • HY-119459
    Fluopyram
    1 Publications Verification

    		 Environmental Pollutants Constitutive Androstane Receptor Parasite Caspase Fungal NF-κB Succinate Dehydrogenase Pregnane X Receptor (PXR) Infection Cancer
    Fluopyram is an orally active succinate dehydrogenase inhibitor, antifungal and nematicide. Fluopyram inhibits succinate dehydrogenase activity, activates CAR/PXR nuclear receptors, and increases caspase-3, TNF-α and NF-κB. Fluopyram inhibits the growth of F. virguliforme, Botrytis cinerea and Alternaria solani with EC50 values of 3.35, 5.389 and 0.244 µg/mL, respectively. Fluopyram induces liver and thyroid tumor formation. Fluopyram is nephrotoxic and embryotoxic .
    Fluopyram
  • HY-163028
    ML-T7

    		Tim3 Cancer
    ML-T7 is a potent Tim-3 inhibitor. ML-T7 blocks Tim-3 interactions with PtdSer and CEACAM1. ML-T7 not only enhances the antitumor activity of adoptive transfer therapy with cytotoxic T lymphocytes (CTLs) and CAR T cells but also increases the effector function of T cell. ML-T7 promotes NK cells’ killing activity against tumor cells and DC antigen-presenting capacity. ML-T7 directly exerts antitumor efficacy in preclinical tumor models either alone or in combination with Nivolumab (HY-P9903A). ML-T7 can be used for tumor immunotherapy research .
    ML-T7
  • HY-164899
    2A3

    2-aminopyridine-3-CARboxylic acid imidazolide

    		 Transmembrane Glycoprotein Cancer
    2A3 (2-aminopyridine-3-carboxylic acid imidazolide) is a T cell activator that specifically binds to CEACAM6 and CEACAM5. 2A3 exhibits enzymatic activity that catalyzes the glucuronidation of specific substrates (e.g., 1-naphthol), and possesses significant cytotoxic activity. When integrated into CAR T cells or used alone, 2A3 acts by inducing cytokine release, degranulation, and direct cytotoxicity. 2A3 kills pancreatic and breast cancer cells with high target antigen expression in vitro, and significantly inhibits the growth of pancreatic cancer xenografts in vivo. 2A3 broadly targets malignant tumors with overexpressed CEACAM5, CEACAM6, or co-expressed both, and shows high expression mainly in tissues such as the liver and colon. 2A3 serves as an important research tool for the immunotherapy of pancreatic and breast cancer . 2A3 is a novel SHAPE reagent, which can be used for the analysis of RNA structure both in vitro and in vivo . 2A3 is an electrophilic chemical probe that acylates the 2'-OH in the RNA backbone. 2A3 can be used for RNA SHAPE-MaP experiments and is capable of analyzing the RNA secondary structures at single nucleotide resolution.
    2A3
  • HY-144987
    RBN013209
    1 Publications Verification

    		 CD38 LAG-3 Tim3 PD-1/PD-L1 Inflammation/Immunology Cancer
    RBN013209 is an orally active small molecule inhibitor of CD38 with an IC50 of 0.01 to 0.1 μM for human CD38. RBN013209 prevents the conversion of extracellular NAD + to ADPR or cADPR in tumor cells and PBMCs. RBN013209 can be used in the study of tumor. In addition, RBN013209 enables CAR-T cells to maintain the naive state and central memory state, and decreases the expression of cell activation markers and exhaustion-related inhibitory receptors .
    RBN013209
  • HY-P99157
    Omburtamab

    		CD276/B7-H3 Cancer
    Omburtamab is a humanized monoclonal antibody targeting B7-H3 (CD276). Omburtamab selectively binds to B7-H3 highly expressed on the surface of tumor cells and activates anti-tumor immune responses mediated by T cells and natural killer (NK) cells. Omburtamab can promote the specific infiltration of CAR-T cells into tumors, enhance the killing function of NK cells through the CD16 signaling pathway, and regulate tumor cell glucose metabolism (such as inhibiting the Warburg effect). Omburtamab has the potential to inhibit solid tumors such as non-small cell lung cancer (NSCLC) .
    Omburtamab
  • HY-157959
    Orphenadrine

    (±)-Orphenadrine

    		 iGluR Cytochrome P450 Cholinesterase (ChE) Neurological Disease Cancer
    Orphenadrine ((±)-Orphenadrine) is a skeletal muscle relaxant and NMDA antagonist that also has antiparkinsonian, antihistamine, antitremor, antispasmodic, and analgesic effects. Orphenadrine inhibits the binding of [3H]MK-801 to the phencyclidine (PCP) binding site of the NMDA receptor. Orphenadrine is also an anticholinergic and CYP2B inducer. Orphenadrine may exert pro-tumor effects, causing CAR nuclear translocation, resulting in microsomal reactive oxygen species (ROS) production and oxidative stress. Orphenadrine also exerts neuronal protection, protecting rat cerebellar granule cells (CGC) from 3-NPA-induced death and has inhibitory potential against neurodegenerative diseases mediated by NMDA receptor overactivation .
    Orphenadrine
  • HY-110249
    CINPA1
    1 Publications Verification

    		 Constitutive Androstane Receptor Metabolic Disease
    CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function .
    CINPA1
  • HY-119459R
    Fluopyram (Standard)

    		Reference Standards Succinate Dehydrogenase Fungal Parasite Constitutive Androstane Receptor Caspase NF-κB Infection Cancer
    Fluopyram (Standard) is the analytical standard of Fluopyram (HY-119459). This product is intended for research and analytical applications. Fluopyram is an orally active succinate dehydrogenase inhibitor, antifungal and nematicide. Fluopyram inhibits succinate dehydrogenase activity, activates CAR/PXR nuclear receptors, and increases caspase-3, TNF-α and NF-κB. Fluopyram inhibits the growth of F. virguliforme, Botrytis cinerea and Alternaria solani with EC50 values of 3.35, 5.389 and 0.244 µg/mL, respectively. Fluopyram induces liver and thyroid tumor formation. Fluopyram is nephrotoxic and embryotoxic .
    Fluopyram (Standard)
  • HY-139678
    SC13

    		FLAP Opioid Receptor Apoptosis STING Neurological Disease Cancer
    SC13 is an orally active, selective Flap structure-specific endonuclease 1 (FEN1) inhibitor and mu opioid receptor (MOR) activator. SC13 impairs DNA damage repair and induces apoptosis in cancer cells. SC13 activates cGAS-STING signaling, increases chemokine secretion, and promotes CAR-T cell infiltration at solid tumour sites. SC13 can be used for the research of solid tumours and pain .
    SC13
  • HY-B0349A
    Meclizine

    Meclozine

    		 Histamine Receptor Apoptosis Neurological Disease Inflammation/Immunology
    Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease .
    Meclizine
  • HY-W709413
    Panaxytriol

    		NF-κB TNF Receptor Interleukin Related Pregnane X Receptor (PXR) Constitutive Androstane Receptor Cytochrome P450 Neurological Disease
    Panaxytriol is an active component of ginseng. Panaxytriol inhibits the nuclear translocation of NF-κB, thereby reducing the production of pro-inflammatory factors (such as TNF-α, IL-1β, IL-6) and nitric oxide (NO) induced by LPS (HY-D1056). Panaxytriol upregulates CYP3A4 by activating the nuclear receptor PXR/CAR. Panaxytriol improves motor dysfunction in a mouse model of brain inflammation. Panaxytriol can be used in the research of neurodegenerative diseases (such as Alzheimer's disease) .
    Panaxytriol
  • HY-W722556
    5α-Androstan-3α-ol

    3α,5α-Androstanol

    		 GABA Receptor Constitutive Androstane Receptor Metabolic Disease
    5α-Androstan-3α-ol is a γ-aminobutyric acid (GABA) receptor agonist. 5α-Androstan-3α-ol can inhibit the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor). 5α-Androstan-3α-ol negatively regulates the activity of CAR by binding to CAR and promoting its dissociation from coactivator proteins. 5α-Androstan-3α-ol can be used to study nuclear receptor-mediated hormone metabolism and drug detoxification mechanisms .
    5α-Androstan-3α-ol
  • HY-173033
    MI-883

    		Pregnane X Receptor (PXR) Constitutive Androstane Receptor Cytochrome P450 Metabolic Disease
    MI-883 is the orally active agonist for Constitutive Androstane Receptor (CAR, EC50=73 nM) and the antagonist for Pregnane X Receptor (PXR, IC50=0.1 μM). MI-883 stimulates CAR LBD assembly (EC50=0.38 µM) and CAR3 variant activation (EC50=0.074 µM), induces CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. MI-883 inhibits basal PXR activity IC50=2.03 µM) in transiently transfected HepG2 cells, blocks CYP3A4 mRNA expression in HepG2. MI-883 regulates cholesterol metabolism and bile acid excretion, improves hypercholesterolemia in mouse models .
    MI-883
  • HY-P10417
    RTDLDSLRTYTL

    		Integrin IFNAR Cancer
    RTDLDSLRTYTL is an Alpha (v) beta (6) integrin (avb6) inhibitor with high affinity and specificity. RTDLDSLRTYTL binds to avb6 integrin, a peptide sequence that activates cytotoxicity and cytokine production in T cells, such as interferon-gamma. RTDLDSLRTYTL is designed through a chimeric T cell antigen receptor (CAR) so that T cells can be redirected to specifically recognize and attack tumor cells. RTDLDSLRTYTL can be used in the research of cancer immunotherapy and targeted drug development .
    RTDLDSLRTYTL
  • HY-180888
    Lck-IN-5

    		Src CD3 Inflammation/Immunology
    Lck-IN-5 (example C10) is a potent and selective lymphocyte-specific protein tyrosine kinase (LCK) inhibitor. Lck-IN-5 selectively disrupts the interaction between the SH3 domain of LCK and the RK motif of CD3ε, thereby impairing LCK recruitment to the TCR. Lck-IN-5 modulates the activity of CD3ε-containing CAR and TRuC T cells, attenuating cytokine production and promoting a central-memory-like phenotype associated with enhanced persistence. Lck-IN-5 can be used for autoimmune diseases and graft-versus-host disease research .
    Lck-IN-5
  • HY-B0349B
    Meclizine dihydrochloride monohydrate

    Meclozine dihydrochloride monohydrate

    		 Histamine Receptor Apoptosis Neurological Disease Inflammation/Immunology
    Meclizine (Meclozine) dihydrochloride monohydrate, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride monohydrate is an effective anti-motion sickness agent. Meclizine dihydrochloride monohydrate crosses the blood-brain barrier. Meclizine dihydrochloride monohydrate is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine dihydrochloride monohydrate can be used for the research of polyQ toxicity disorders, such as Huntington's disease .
    Meclizine dihydrochloride monohydrate
  • HY-B0349R
    Meclizine dihydrochloride (Standard)

    Meclozine dihydrochloride (Standard)

    		 Reference Standards Histamine Receptor Apoptosis Neurological Disease Endocrinology Cancer
    Meclizine (dihydrochloride) (Standard) is the analytical standard of Meclizine (dihydrochloride). This product is intended for research and analytical applications. Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .
    Meclizine dihydrochloride (Standard)
  • HY-183912
    PY-4Car2

    		Topoisomerase ADC Payload Cancer
    PY-4Car2 is a Camptothecin (HY-16560) derivative and a topoisomerase I inhibitor. PY-4Car2 functions as a warhead conjugated via a cleavable linker to the bispecific ADC TJ101. PY-4Car2 can be used as an ADC payload for the research of cancers .
    PY-4Car2
  • HY-103244R
    CITCO (Standard)

    		Reference Standards Apoptosis Cancer
    CITCO (Standard) is the analytical standard of CITCO (HY-103244). This product is intended for research and analytical applications. 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 .
    CITCO (Standard)
  • HY-P10417B
    RTDLDSLRTYTL TFA

    		Integrin IFNAR Cancer
    RTDLDSLRTYTL TFA is an Alpha (v) beta (6) integrin (avb6) inhibitor with high affinity and specificity. RTDLDSLRTYTL TFA binds to avb6 integrin, a peptide sequence that activates cytotoxicity and cytokine production in T cells, such as interferon-gamma. RTDLDSLRTYTL TFA is designed through a chimeric T cell antigen receptor (CAR) so that T cells can be redirected to specifically recognize and attack tumor cells. RTDLDSLRTYTL TFA can be used in the research of cancer immunotherapy and targeted drug development .
    RTDLDSLRTYTL TFA

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