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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
27 Results for "
cellular potency
" in MedChemExpress (MCE) Product Catalog:
Products (27)
27 Results for "cellular potency" in MCE Product Catalog:
5
5 Cited Publications
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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 .
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4 Cited Publications
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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 .
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 .
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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) .
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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) .
Cat. No.: HY-160211
CAS No.: 3022928-90-8
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JA310, a chemical probe, is a highly selective MST3 kinase inhibitor. JA310 has high cellular potency against MST3 with an EC50 value of 106 nM .
Cat. No.: HY-N4208
CAS No.: 2230777-09-8
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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 .
Cat. No.: HY-170362
CAS No.: 2987886-49-5
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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
Cat. No.: HY-147193A
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) .
Cat. No.: HY-125209A
CAS No.: 2253744-57-7
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TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC50 of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9 .TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis .TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells .TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells .TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay .TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA) .TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells .TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells .TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines .TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer .
Cat. No.: HY-178980
CAS No.: 2830619-57-1
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APL-5125 (Compound 61f) is a potent, selective and orally active ATP-competitive CK2α inhibitor with an IC50 of 0.348 nM and a Ki of 0.095 nM. APL-5125 binds to CK2α in a bivalent manner, simultaneously interacting with the ATP-binding site and the αD pocket. APL-5125 exhibits antitumor activity and can be used for the research of cancer, such as colon cancer .
Cat. No.: HY-179219S
CAS No.: 3035072-99-9
Cat. No.: HY-154839
CAS No.: 2299227-75-9
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 .
Cat. No.: HY-147656
CAS No.: 3011778-39-2
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 .
Cat. No.: HY-175260
CAS No.: 2136606-87-4
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ZN-c5 is a selective and orally active estrogen receptor degrader. ZN-c5 exhibits high potency in the cellular assay (MCF-7, IC50 = 0.3 nM) and binds with high affinity to ERα and ERβ (IC50 = 0.4 nM and 0.8 nM, respectively). ZN-c5 inhibits tumor growth in MCF-7 mouse xenograft model and WHIM20 xenograft model. ZN-c5 can be used for the study of breast cancer .
Cat. No.: HY-103453
CAS No.: 524047-78-7
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(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 .
Cat. No.: HY-119951
CAS No.: 925218-37-7
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AKI-001 is an prototype pentacyclic inhibitor of aurora kinase with cellular potency of IC50 of less than 100 nM. AKI-001 shows low nanomolar potency against Aurora A and Aurora B enzymes .
Cat. No.: HY-124317
CAS No.: 1621585-17-8
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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 .
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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
