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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
16 Results for "
NAD+ depletion
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "NAD+ depletion" in MCE Product Catalog:
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Daporinad (FK866) is a non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a Ki value of 0.3 nM. Daporinad depletes NAD+ and ATP levels, inhibits mTORC1 and MAPK/ERK pathways, and activates TFEB to induce autophagy. Daporinad causes the depletion of the endoplasmic reticulum Ca²⁺ pool, ultimately weakening the mitogen-induced Ca²⁺ signal and the activation and function of T cells. Daporinad induces cell cycle arrest and apoptosis, and inhibits cell proliferation. Daporinad can be used for the study of myeloma, liver cancer, and immunosuppression .
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2 Cited Publications
GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity .
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1 Cited Publications
Cat. No.: HY-W614507
CAS No.: 19132-12-8
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Dihydronicotinamide riboside is a potent NAD + concentration enhancer. Dihydronicotinamide riboside modulates targets BAX, PUMA, NQO2, and IκB kinase. Dihydronicotinamide riboside mediates apoptosis, induces pro-oxidant activity, mitochondrial dysfunction, metabolic dysregulation, redox modulation, and pro-inflammatory M1 phenotype induction. Dihydronicotinamide riboside increases intracellular and mitochondrial NAD + levels, maintains cell survival against NAD +-depleting genotoxins. Dihydronicotinamide riboside can be used for the research of hepatocellular carcinoma .
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1 Cited Publications
Cat. No.: HY-170620
PARP1 PROTAC 180055 is a PARP1 PROTAC degrader that recruits VHL, with DC50 values of 180 nM and 240 nM in T47D and MDA-MB-231 cells, respectively. PARP1 PROTAC 180055 selectively kills BRCA-mutant tumor cells by inducing PARP1 ubiquitination and proteasomal degradation, thereby blocking PARylation, NAD + depletion and DNA trapping. PARP1 PROTAC 180055 can be used in the research of breast cancer, ovarian cancer, colorectal cancer, acute T-lymphoblastic leukemia, prostate cancer and osteosarcoma .
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GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects .
Cat. No.: HY-178159
CAS No.: 2244341-81-7
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SA91-0178 is a METTL1 inhibitor. SA91-0178 inhibits m 7G methylation of RNA, reduces SARM1 stability, mitigates NAD + depletion and metabolic reprogramming in macrophages. SA91-0178 demonstrates excellent protective efficacy against multiple organ injury in cecal ligation and puncture (CLP)-induced and ischemia/reperfusion (I/R)-induced mice. SA91-0178 can be used for the study of systemic inflammatory diseases .
Cat. No.: HY-173679
CAS No.: 2569517-30-0
RBN012811 is a highly selective PROTAC-based PARP14 degrader. RBN012811 forms a ternary complex with cereblon by binding to the NAD + site of PARP14, and mediates the specific degradation of PARP14 via the ubiquitin-proteasome pathway (IC50=10 nM). RBN012811 effectively depletes endogenous PARP14 in various cell lines and primary human macrophages, thereby downregulating IL-10 production and IFN-β mRNA levels, increasing phosphorylated STAT1 levels to enhance inflammatory signaling, and inhibiting interferon-induced ADPr condensate formation. RBN012811 also modulates viral replication, exhibiting increased HSV1 replication while reducing VSV replication. RBN012811 has important application value in research related to cancer and viral infections .
Cat. No.: HY-125147
CAS No.: 1375557-33-7
A-1293201 is a substrate-independent NAMPT inhibitor with antitumor activity. A-1293201 effectively reduces the total cellular NAD +/NADH (NADt) level, subsequently leading to ATP depletion and cancer cell death. In addition, A-1293201 can effectively overcome the acquired resistance mechanism of the NAMPT Y18 mutant to CHS-828 (HY-10079) .
Cat. No.: HY-110319
CAS No.: 1785666-54-7
Synonyms: (E/Z)-FK866 hydrochloride; (E/Z)-APO866 hydrochloride
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(E/Z)-Daporinad hydrochloride ((E/Z)-FK866 hydrochloride) is a potent inhibitor of nicotinamide phosphoribose transferase (NAMPT). (E/Z)-Daporinad hydrochloride induces apoptosis by specifically inhibiting NAMPT to gradually deplete intracellular NAD +. (E/Z)-Daporinad hydrochloride can be used in the study of cancer biology and inflammatory diseases .
Cat. No.: HY-50876A
CAS No.: 2727965-45-7
Synonyms: FK866 hydrochloride; APO866 hydrochloride
Daporinad (FK866) hydrochloride is a non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a Ki value of 0.3 nM. Daporinad hydrochloride depletes NAD+ and ATP levels, inhibits mTORC1 and MAPK/ERK pathways, and activates TFEB to induce autophagy. Daporinad hydrochloride causes the depletion of the endoplasmic reticulum Ca²⁺ pool, ultimately weakening the mitogen-induced Ca²⁺ signal and the activation and function of T cells. Daporinad hydrochloride induces cell cycle arrest and apoptosis, and inhibits cell proliferation. Daporinad hydrochloride can be used for the study of myeloma, liver cancer, and immunosuppression .
Cat. No.: HY-181578
CAS No.: 3077970-78-3
Nampt-IN-17 is an selective orally active NAMPT inhibitor with a human NAMPT IC50 of 17 nM and Ki of 25.9 nM. Nampt-IN-17 depletes intracellular NAD + and ATP, disrupts mitochondrial membrane potential, suppresses cell proliferation, self-renewal, invasion, and migration, induces cell-cycle arrest and apoptosis. Nampt-IN-17 exhibits selective activity against NAPRT-deficient gastric cancer cells. Nampt-IN-17 can be used for the research of NAPRT-deficient gastric cancer .
Cat. No.: HY-184246
CAS No.: 2791469-19-5
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SR-34831 is a NAMPT activator, NAD level stabilizer and neuroprotective agent. SR-34831 enhances the enzymatic activity of human NAMPT, prevents intracellular NAD depletion, and counteracts neuronal death induced by toxic misfolded prion proteins. SR-34831 exhibits metabolic stability in human liver microsomes and can be used for the research of protein misfolding neurodegenerative diseases .
Cat. No.: HY-184247
CAS No.: 2791469-14-0
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SR-32685 is a NAMPT activator and neuroprotective agent. SR-32685 enhances the enzymatic activity of hNAMPT, prevents intracellular NAD depletion, and protects neurons from death induced by toxic misfolded prion proteins. SR-32685 can be used in the research of protein misfolding neurodegenerative diseases and metabolic diseases .
Cat. No.: HY-50876R
CAS No.: 658084-64-1
Synonyms: FK866 (Standard); APO866 (Standard)
Daporinad (Standard) is the analytical standard of Daporinad (HY-50876). This product is intended for research and analytical applications. Daporinad (FK866) is a non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a Ki value of 0.3 nM. Daporinad depletes NAD+ and ATP levels, inhibits mTORC1 and MAPK/ERK pathways, and activates TFEB to induce autophagy. Daporinad causes the depletion of the endoplasmic reticulum Ca²⁺ pool, ultimately weakening the mitogen-induced Ca²⁺ signal and the activation and function of T cells. Daporinad induces cell cycle arrest and apoptosis, and inhibits cell proliferation. Daporinad can be used for the study of myeloma, liver cancer, and immunosuppression .
Cat. No.: HY-184396
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GR2-128 is a dual inhibitor targeting MLK3 and NAMPT with IC50 values of 84 nM and 14 nM, respectively. GR2-128 inhibits downstream JNK/c‑Jun signaling and reduces NAD + levels. GR2-128 exhibits antiproliferative and pro-apoptotic activities in triple-negative breast cancer cells without significant toxicity to normal cells. GR2-128 suppresses tumor growth, reduces macrophage and neutrophil infiltration, and increases tumor T-cell markers in a syngeneic mouse model, and can be used for triple-negative breast cancer research .
Cat. No.: HY-184918
CAS No.: 3097045-01-4
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NAMPT/PD-1/PD-L1-IN-1 is a potent the PD-1/PD-L1 interaction and NAMPT dual inhibitor with IC50s of 7.5 nM and 18.8 nM, respectively. NAMPT/PD-1/PD-L1-IN-1 enhances T cell-mediated tumor cell killing, promotes T cell proliferation and CD8 + T cell proportion and depletes intracellular NAD + biosynthesis. NAMPT/PD-1/PD-L1-IN-1 suppresses tumor progression in a mouse LLC xenograft model by disrupting tumor metabolism and activating the tumor immune microenvironment. NAMPT/PD-1/PD-L1-IN-1 can be used in research on tumor immunotherapy for non-small cell lung cancer .
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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
