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cellular potency

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-147193
    Nampt-IN-10 TFA

    		NAMPT Cancer
    Nampt-IN-10 TFA (compound 4) is a Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-10 TFA shows cellular potency to A2780 and CORL23 cells lines with IC50s of 5 and 19 nM, respectively. Nampt-IN-10 TFA can be used as a novel non-antimitotic payload for ADCs .
    Nampt-IN-10 TFA
  • HY-160211
    JA310

    		Hippo (MST) Cancer
    JA310 is a highly selective MST3 kinase inhibitor. JA310 has high cellular potency against MST3 with an EC50 value of 106 nM .
    JA310
  • HY-N4208
    Taccalonolide AJ

    		Microtubule/Tubulin Cancer
    Taccalonolide AJ is a semi-synthesis compound with cellular microtubule stabilizing activity. Taccalonolide AJ exhibits high potency antiproliferative activity against cancer cells, with an IC50 of 4.2 nM for HeLa cells .
    Taccalonolide AJ
  • HY-103453
    (R)-DPN

    		Estrogen Receptor/ERR Endocrinology
    (R)-DPN (compound 3) is a selective ERβ ligand with EC50s of 2.9, 0.8 nM for ERα and ERβ, respectively. (R)-DPN shows a very high affinity and potency preference for ERβ over ERα. (R)-DPN shows cytoxicity for HEC-1 and U2OS cells with EC50s of 286, 205 nM, respectively .
    (R)-DPN
  • HY-154839
    c-Myc inhibitor 10

    		c-Myc Cancer
    c-Myc inhibitor 10 (compound 17), a c-Myc inhibitor, exhibits increased cellular potency, consistent with an increase in permeability with methylation of the morpholine nitrogen .
    c-Myc inhibitor 10
  • HY-124317
    PF-06649283

    		Fluorescent Dye Others
    PF-06649283 is a drug with potential intracellular activity. The effects of PF-06649283 may be affected by factors such as cellular metabolism, protein-protein interactions, post-translational modifications, and asymmetric intracellular localization. The potency of PF-06649283 at the cellular level may show different activity compared to the recombinant enzyme, and this difference needs to be considered in the drug discovery process. Increased intracellular potency of PF-06649283 may be critical for the development of this drug as a probe or drug .
    PF-06649283
  • HY-169199
    BAY-405

    		MAP4K Cancer
    BAY-405 (compund 38) is a MAP4K1 inhibitor that exhibits nanomolar potency in biochemical and cellular assays and achieves in vivo exposure after oral administration .
    BAY-405
  • HY-151134
    HBV-IN-25

    		HBV Infection
    HBV-IN-25 is a good potency, orally active novel HBV cccDNA reducer. HBV-IN-25 has anti-HBeAg potency and anti-HBV activity with IC50 values of 0.58 μM and 1.15 μM, respectively. HBV-IN-25 has good aqueous solubility (LYSA＞452 μg/mL) and good PK property with no cellular toxicity .
    HBV-IN-25
  • HY-155813
    MPI60

    		SARS-CoV Infection
    MPI60 is a potent SARS-CoV-2 M Pro inhibitor with high antiviral potency, low cellular cytotoxicity, and high in vitro metabolic stability. MPI60 can be used for SARS-CoV-2 research .
    MPI60
  • HY-145884
    BTK-IN-8

    		Btk Inflammation/Immunology
    BTK-IN-8 is a potent and selective peripheral covalent BTK inhibitor (IC50=0.22 nM; Kd=0.91 nM). BTK-IN-8 has good whole blood CD69 cellular potency (IC50=0.029 µM) .
    BTK-IN-8
  • HY-147656
    NAMPT degrader-1

    		ATTECs NAMPT Autophagy Cancer
    NAMPT degrader-1 (Compound A3), an autophagosome-tethering compound (ATTEC), is an nicotinamide phosphoribosyltransferase (NAMPT) degrader with an IC50 of 0.023 μM. NAMPT degrader-1 significantly induces the degradation of NAMPT through the autophagy-lysosomal pathway and shows excellent cellular antitumor potency .
    NAMPT degrader-1
  • HY-147193A
    Nampt-IN-10 trihydrochloride

    		NAMPT Cancer
    Nampt-IN-10 trihydrochloride (compound 4) is a Nicotinamide Phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-10 trihydrochloride shows cellular potency to A2780 and CORL23 cell lines with IC50 values of 5 and 19 nM, respectively. Nampt-IN-10 trihydrochloride can be used as a novel non-antimitotic payload for antibody-drug conjugate (ADC) .
    Nampt-IN-10 trihydrochloride
  • HY-138568
    HPK1-IN-3

    		MAP4K Inflammation/Immunology
    HPK1-IN-3 is a potent and selective ATP-competitive hematopoietic progenitor kinase 1 (HPK1; MAP4K1) inhibitor with an IC50 of 0.25 nM. HPK1-IN-3 has IL-2 cellular potency with an EC50 of 108 nM in human peripheral blood mononuclear cells (PBMCs) .
    HPK1-IN-3
  • HY-145270
    ELOVL1-IN-2

    		ELOVL Metabolic Disease
    ELOVL1-IN-2 is an elongation of very long chain fatty acid 1 (ELOVL1) enzyme inhibitor, ELOVL1-IN-2 shows weak ELOVL1 inhibition (IC50=21 μM) and moderate potency in a primary cellular assay (HEK293 C26 IC50=6.7 μM) .
    ELOVL1-IN-2
  • HY-122882
    HOIPIN-8
    2 Publications Verification

    		 E1/E2/E3 Enzyme Inflammation/Immunology
    HOIPIN-8 is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. HOIPIN-8 is a HOIPIN-1 derivative with enhanced the potency by 255-fold in the petit-LUBAC inhibition, and 10-fold and 4-fold in the LUBAC- and TNF-α-mediated NF-κB activation, respectively than HOIPIN-1. HOIPIN-1 is a promising tool to explore the cellular functions of LUBAC .
    HOIPIN-8
  • HY-170362
    cGAS-IN-4

    		Cyclic GMP-AMP Synthase Inflammation/Immunology
    cGAS-IN-4 (Compound 36) is an orally active inhibitor for cyclic GMP-AMP synthase (cGAS) with IC50 of 32 nM and 5.8 nM for h-cGAS and m-cGAS. cGAS-IN-4 inhibits the cGAMP in THP-1 cell with an IC50 of 60 nM, which improves the cellular potency. cGAS-IN-4 exhibits anti-inflammatory efficacy in Concanavalin A (HY-P2149)-induced acute liver injury in mouse models . orally active, THP-1, C57Bl/6 mouse, orally active
    cGAS-IN-4
  • HY-111790
    M3258
    1 Publications Verification

    		 Proteasome Apoptosis Cancer
    M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .
    M3258
  • HY-15334
    CEP-5214

    		VEGFR Cancer
    CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability .
    CEP-5214
  • HY-170926
    CQ1373

    		RET Apoptosis Cancer
    CQ1373 is a potent RET inhibitor, demonstrating cellular potency with IC50 values of 13.0, 25.7 and 28.4 nM against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C and CCDC6-RET-G810R, respectively. CQ1373 exhibits good selectivity toward wild-type RET and solvent front mutants G810C/R with IC50 values of 4.2, 7.1 and 32.4 nM, respectively. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. CQ1373 induces Apoptosis and cell cycle arrest in BaF3 cells. CQ1373 exhibits anti-tumor efficacy and can be used for cancer research .
    CQ1373

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