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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
28 Results for "
CAR Inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (28)
28 Results for "CAR Inhibitors" in MCE Product Catalog:
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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 .
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3 Cited Publications
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 .
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1 Cited Publications
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 .
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1 Cited Publications
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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 .
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1 Cited Publications
Cat. No.: HY-155978A
Purity: 99.80%
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RDN2150 TFA is a ZAP-70 inhibitor with an IC50 of 14.6 nM, and it exhibits selectivity for Syk over other kinases. RDN2150 TFA inhibits signal transduction and activation of T cells/CAR-T cells, reduces the phosphorylation level of Erk1/2, suppresses the induction of CD69 and IL-2, and downregulates phosphotyrosine signaling pathways including hnRNP sites in T cells. RDN2150 TFA can be used for psoriasis-related research .
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1 Cited Publications
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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 .
Cat. No.: HY-163028
CAS No.: 459789-75-4
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 .
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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 .
Cat. No.: HY-119459R
CAS No.: 658066-35-4
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 .
Cat. No.: HY-163168
CAS No.: 2412985-00-1
Synonyms: CFT-4531
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aTAG 4531 (CFT-4531) is a PROTAC-class degrader that induces the degradation of the MTH1/aTAG fusion protein by recruiting cereblon, with a DC50 of 0.28 nM in Jurkat cells. aTAG 4531 inhibits MTH1 enzymatic activity, with a Ki of 1.8 nM. aTAG 4531 rapidly, selectively and reversibly regulates SMART-CAR protein levels, CAR-mediated target cell killing and IL-2 release, and is applicable both in vitro and in vivo. aTAG 4531 can be used in studies of targeted protein degradation, target validation and CAR-T activity regulation .
Cat. No.: HY-139678
CAS No.: 2839142-69-5
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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 .
Cat. No.: HY-146231
CAS No.: 2636072-62-1
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SS47 is a hematopoietic progenitor kinase HPK1 PROTAC-class degrader and immune activator. SS47 promotes the proliferation of CD4+ and CD8+ T cells as well as IFN-γ secretion, and enhances the anti-tumor cytotoxicity and in vivo efficacy of BCMA CAR-T cells. SS47 also inhibits tumor growth in mouse models, and when combined with anti-PD-1 therapy, it improves the immune response of 4T1 tumor-bearing mice. SS47 can be used in breast cancer-related research .
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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 .
Cat. No.: HY-155978
CAS No.: 2839429-51-3
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RDN2150 is a ZAP-70 inhibitor with an IC50 of 14.6 nM, and it exhibits selectivity for Syk over other kinases. RDN2150 inhibits signal transduction and activation of T cells/CAR-T cells, reduces the phosphorylation level of Erk1/2, suppresses the induction of CD69 and IL-2, and downregulates phosphotyrosine signaling pathways including hnRNP sites in T cells. RDN2150 can be used for psoriasis-related research .
Cat. No.: HY-W709413
CAS No.: 87005-03-6
Cat. No.: HY-173033
CAS No.: 2530027-71-3
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MI-883 is orally active constitutive androstane receptor (CAR) (EC50 of 73 nM) agonist and pregnane X Receptor (PXR) (IC50 of 100 nM) antagonist. MI-883 binds to CAR and PXR ligand-binding domains, promotes CAR LBD assembly, activates CAR3 variant, stimulates CAR cytoplasmic-nuclear translocation, upregulates CAR target genes, recruits coactivators NCOA1, NCOA2, NCOA3, inhibits basal and agonist-induced PXR activation, downregulates PXR target genes, disrupts PXR-NCOR2 interaction, blocks agonist-mediated PXR-NCOA1 recruitment. MI-883 reduces plasma total cholesterol, LDL cholesterol, and hepatic free cholesterol levels, increases fecal bile acid excretion, regulates genes involved in xenobiotic metabolism, cholesterol homeostasis, and bile acid homeostasis. MI-883 exhibits metabolic stability, liver-predominant distribution, a safety profile with no observed toxicity, and does not stimulate human hepatocyte hypertrophy or hyperplasia. MI-883 can be used for the research of diet-induced hypercholesterolemia .
Cat. No.: HY-W722556
CAS No.: 7657-50-3
Synonyms: 3α,5α-Androstanol
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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 .
Cat. No.: HY-P10417
CAS No.: 222557-93-9
Cat. No.: HY-180888
CAS No.: 1356734-45-6
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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 .
Cat. No.: HY-B0349B
CAS No.: 31884-77-2
Synonyms: Meclozine dihydrochloride monohydrate
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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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
