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Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162) .
Poly(ADP-ribose) Polymer/pADPr is a complex polymer of repeating ADP-ribose units, which is synthesized using poly(ADP-ribose) polymerase (PARP) in the presence of NAD +, cleaved from PARP, and subsequently purified .
FeTMPyP is an orally active poly (ADP-ribose) polymerase (PARP) inhibitor. FeTMPyP inhibits cell death, nitrotyrosine formation, and depolarization of mitochondrial transmembrane potential. FeTMPyP reduces homocysteine-induced nitrosative stress and partially restores TFEB protein and mRNA levels. FeTMPyP improves functional and behavioral deficits caused by chronic constriction injury in rats. FeTMPyP alleviates acute cerebral infarction in a rat model of middle cerebral artery occlusion with mild hyperglycemia. FeTMPyP can be used in studies related to neuropathic pain, renal aging, ischemic penumbra, and hyperglycemic stroke .
Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
Z-FF-FMK (Z-Phe-Phe-FMK) is a cell-permeable, irreversible, and cysteine protease inhibitor targeting cathepsin-L. Z-FF-FMK inhibits angiotensin II-induced MEK activation in vascular walls, aortic medial remodeling, blood pressure elevation, and upregulation of cystatin C in aortic walls. Z-FF-FMK prevents β-amyloid-mediated caspase-3 activation, poly (ADP-ribose) polymerase cleavage, DNA fragmentation, and apoptosis of cortical neurons (apoptosis). Z-FF-FMK can be used in research related to hypertension and Alzheimer's disease .
INO-1001 is a potent and selective poly (ADP-ribose) polymerase (PARP) inhibitor. INO-1001 is a potent enhancer of radiation sensitivity and enhances radiation-induced cell killing by interfering with DNA repair mechanisms, resulting in necrotic cell death . INO-1001 has anti-tumor effects .
4'-O-Methylbavachalcone is an orally active prenylated flavonoid that inhibits the activity of SARS-CoV papain-like protease (PLpro), with an IC50 of 10.1 μM and a Ki of 4.6 μM. 4'-O-Methylbavachalcone inhibits poly (ADP-ribose) polymerase-mediated cell death (parthanatos), reduces cerebral infarct volume, binds to the orthosteric site of SUCNR1, blocks the interaction between succinate and SUCNR1, inhibits SUCNR1 activity, blocks the nuclear translocation of NFATc4, suppresses the activation of the ERK1/2 signaling pathway, inhibits cardiomyocyte hypertrophy and restores the expression of α-actinin. 4'-O-Methylbavachalcone can be used in studies related to ischemic stroke, SARS-CoV and cardiomyocyte hypertrophy .
pNP-ADPr disodium is a colorimetric substrate that used for the first continuous Poly(ADP-ribose) glycohydrolase (PARG) and ADP-ribosyl hydrolase 3 (ARH3) activity assays. pNP-ADPr disodium can be used for the research of poly(ADP-ribose)polymerase (PARP) enzymes .
Nudifloramide-d3 (2PY-d3) is the deuterium labeled Nudifloramide. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
Floxuridine (Standard) is the analytical standard of Floxuridine. This product is intended for research and analytical applications. Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
2'-Fluoro-5'-O-DMT-2'-deoxyinosine-3'-CE-phosphoramidite is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
Nudifloramide (Standard) is the analytical standard of Nudifloramide. This product is intended for research and analytical applications. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
pNP-ADPr is a colorimetric substrate that used for the first continuous Poly(ADP-ribose) glycohydrolase (PARG) and ADP-ribosyl hydrolase 3 (ARH3) activity assays. pNP-ADPr can be used for the research of poly(ADP-ribose)polymerase (PARP) enzymes .
DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo .
6-O-Methylinosine is a hypoxanthine analogue. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
ARTD10/PARP10-IN-1 (compound 23) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 (ARTD1/PARP1) with IC50s of 1.7 μM, 1.6 μM, 0.8 μM, and 4.4 μM, respectively .
INH2BP is a poly(ADP-ribose) polymerase (PARP) inhibitor with antioxidant and anti-apoptotic activities. INH2BP reduces the production of intracellular reactive oxygen species (ROS), modulates the expression of apoptosis-related proteins such as Bax, Bcl-2 and cleaved caspase-3 and enhances cell survival through the activation of the ERK1/2 and p38 MAPK signaling pathways. INH2BP is promising for research of cardiovascular diseases .
Mefuparib (CVL218) is a poly ADP-ribosepolymerase (PARP) inhibitor used in cancer research that exhibits potent brain penetration due to its high protein binding.
GPI 15427 is a potent inhibitor of the enzyme poly (ADP-ribose) polymerase-1 (PARP-1), which plays a harmful role during inflammation. In a rat model of gut injury and inflammation, including splanchnic artery occlusion (SAO) shock and dinitrobenzene sulfonic acid (DNBS)-induced colitis, GPI 15427 demonstrates strong anti-inflammatory effects that reduces inflammatory cell infiltration, histological injury. GPI 15427 also diminishes the accumulation of poly (ADP-ribose) in the ileum and colon of treated rats .
8-Chloroquinazolin-4-ol is a poly (ADP-ribose) polymerase-1 (PARP-1) inhibitor with an IC50 value of 5.65 μM. 8-Chloroquinazolin-4-ol can be used in cancer-related research .
Etidaligide sodium, an AsiDNA, a first-in-class DNA repair inhibitor designed to prevent the repair of DNA damage in tumour cells. It also activates DNA-dependent protein kinase (DNA-PK) and poly (ADP-ribose) polymerase enzymes that induce phosphorylation
Etidaligide, an AsiDNA, a first-in-class DNA repair inhibitor designed to prevent the repair of DNA damage in tumour cells. It also activates DNA-dependent protein kinase (DNA-PK) and poly (ADP-ribose) polymerase enzymes that induce phosphorylation of H2A
Lotixparib (Example 1) is an inhibitor of poly(ADP-ribose)polymerase-1 (PARP-1). Lotixparib has cytoprotective effect against a retinal disease. Lotixparib can be studied in research for PARP-1-associated diseases .
ARTD10/PARP10-IN-2 (compound 19) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 ARTD1/PARP1 with IC50s of 2.0 μM, and 9.7 μM, respectively .
A-620223 succinate (ABT-472) is an orally available poly(ADP-ribose) polymerase (PARP) inhibitor. A-620223 succinate (ABT-472) exhibits very good potency against the PARP-1 enzyme with a Ki value of 8 nM and an EC50 value of 3 nM in whole cell assay, making it useful in cancer research .
Benzamide-d5 (Benzenecarboxamide-d5) is deuterium labeled Benzamide. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
2'-O-Methyl-5'-O-dmt-inosine-3'-CE-phosphoramidite is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
AZ0108 is an inhibitor for poly ADP-ribosepolymerase (PARP), which inhibits PARP1, PARP2, PARP3, PARP6, TNKS1, TNKS2, with IC50s of <0.03, <0.03, 2.8, 0.083, 3.2, >3 μM, respectively. AZ0108 prevents centrosome clustering with an EC50 of 0.053 μM, and exhibits cytotoxicity in cell OCI-LY-19 with GI50 of 0.017 μM. AZ0108 exhibits good in vivo pharmacokinetic characters in rat/mouse models .
Floxuridine- 13C, 15N2 (5-Fluorouracil 2'-deoxyriboside- 13C, 15N2) is the 13C- and 15N-labeled labeled Floxuridine (HY-B0097). Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
Rolinsatamab talirine (ABBV 176) is a prolactin receptor (PRLR)-targeting antibody-drug conjugate (ADC), compoused of Rolinsatamab (HY-P99238) and SGD-1882 (HY-101127). Rolinsatamab talirine binds to PRLR to deliver a cytotoxin to tumor cells. Rolinsatamab talirine induces DNA damage, and exhibits cytotoxicity against multiple breast tumor models, including triple negative and low PRLR-expressing models. Rolinsatamab talirine demonstrates enhanced anti-tumor activity in several breast cancer models. Rolinsatamab talirine can be used for the research of breast cancer, hepatocellular carcinoma, ovarian cancer, endometrial cancer, prostate cancer, colorectal cancer, adrenocortical carcinoma, and solid tumors .
ZINC000081009201 is a potent poly(ADP-ribose) polymerase 1 (PARP1) inhibitor with an IC50 value of 1.4767 μM. ZINC000081009201 is promising for research of triple-negative breast cancer (TNBC) .
Mycophenolic Acid-d3 Acyl-Beta-D-glucuronide is the deuterium labeled Mefuparib (HY-167927). Mefuparib (CVL218) is a poly ADP-ribosepolymerase (PARP) inhibitor used in cancer research that exhibits potent brain penetration due to its high protein binding.
8-NH2-ATP tetrasodium, an inactive form of ATP, is produced by 8-NH2-Ado. 8-NH2-Ado tetrasodium induces apoptosis-related cleavage of poly (ADP-ribose) polymerase .
8-NH2-ATP, an inactive form of ATP, is produced by 8-NH2-Ado. 8-NH2-Ado is reported to be potent as shown by induction of apoptosis-related cleavage of poly (ADP-ribose) polymerase .
NU 1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitor with a Ki of 6 nM. NU 1085 shows strong cytotoxicity to cancer cells (LC50 = 83-94 μM) and can enhance the anticancer effect of Temozolomide (HY-17364). NU 1085 can be used for the research of cancer, such as lung cancer .
INO-1001 mesylate is a potent and selective poly (ADP-ribose) polymerase (PARP) inhibitor. INO-1001 mesylate is a potent enhancer of radiation sensitivity and enhances radiation-induced cell killing by interfering with DNA repair mechanisms, resulting in necrotic cell death . INO-1001 mesylate has anti-tumor effects .
Ru3 is a poly(ADP-ribose) polymerase 1 inhibitor. Ru3 induces apoptosisin MCF-7 cells by multiple modes, inclusive of inducing DNA damage, suppressing DNA damage repair, disturbing cell cycle distribution, decreasing the mitochondrial membrane potential, and increasing the intracellular reactive oxygen species levels .
Eupatorin (Standard) is the analytical standard of Eupatorin. This product is intended for research and analytical applications. Eupatorin, a naturally occurring flavone, arrests cells at the G2-M phase of the cell cycle and induces apoptotic cell death involving activation of multiple caspases, mitochondrial release of cytochrome c and poly(ADP-ribose) polymerase cleavage .
NSC745887 (compound 25) is an inhibitor that targets DNA topoisomerase cleavage, activates the caspase-8/9-caspase-3-poly (ADP-ribose) polymerase cascade, and induces apoptosis in cancer cells. NSC745887 enhances γH2AX expression and causes DNA fragmentation leading to DNA damage .
CAY10506 is a PPARγ ligand that can induce cell death and ROS production in a PPARγ-dependent manner in vitro. CAY10506 exhibits radiosensitizing effects, enhancing γ-radiations-induced apoptosis and caspase-3-mediated poly (ADP-ribose) polymerase (PARP) cleavage. CAY10506 can be used in cancer research .
DPP is a Platinum(IV) complex, bearing pterostilbene-derived axial ligand. DPP inhibit the JAK2-STAT3 pathway in breast cancer (BC) cells with antiproliferative activity, and activates caspase-3 and cleaved poly ADP-ribosepolymerase to induces apoptosis. DPP promotes the maturation and antigen presentation of dendritic cells, and exhibits in vivo safety .
Benzo[c][1,8]naphthyridin-6(5H)-one exhibits low micromolar affinity to human adenosine receptor (AR) A1 and hA2A, with Ki of 4.6 and 4.8 μM. Benzo[c][1,8]naphthyridin-6(5H)-one is inhibitor for poly ADP-ribosepolymerase-1 (PARP-1) and aurora kinase A, with IC50 of 0.311 and 5.5 μM .
PARP1-IN-37 (Compound 8) is an orally active and selective poly(ADP-ribose) polymerase 1 and 2 (PARP1/2) inhibitor with an IC50 value of 24 nM for PARP1. PARP1-IN-37 inhibits PARP activity in cells with an EC50 value of 3.7 μM. PARP1-IN-37 is promising for research of BRCA-mutated tumors, such as breast and ovarian cancers .
Benzamide (Standard) is the analytical standard of Benzamide. This product is intended for research and analytical applications. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
2-Chloro-6-methoxypurine riboside is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
2′-C-Methyl-6-O-methylinosine is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
2-Chloro-2'-deoxy-6-O-methylinosine is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
Dicentrine hydrochloride is a drug with anti-inflammatory and anti-cancer activity. Dicentrine hydrochloride exerts its effects by enhancing TNF-α-induced apoptosis in A549 lung adenocarcinoma cells. Dicentrine hydrochloride increases caspase-8, -9, -3 and poly(ADP-ribose) polymerase (PARP) activities. Dicentrine hydrochloride inhibits TNF-α-induced invasion and migration of A549 cells. Dicentrine hydrochloride significantly inhibited the TNF-α-activated TAK1, p38, JNK and Akt signaling pathways, and reduced the transcriptional activities of NF-κB and AP-1 .
6-Methoxypurine-9-β-D-5’(R)-C-methylriboside is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
STAT3-IN-18 (compound SPP) is a platinum (IV) complex with an axial ligand derived from sandalwood. STAT3-IN-18 inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, with anti-proliferative activity. STAT3-IN-18 activates caspase-3 and increases cleaved polyADP-ribosepolymerase to induce apoptosis. STAT3-IN-18 promotes maturation and antigen presentation of dendritic cells and demonstrates safety in vivo.
Biotin-NAD + is a PARylation donor and also a substrate of poly (ADP-ribose) polymerase-1 (PARP1). Under the mediation of PARP1, Biotin-NAD + undergoes poly (ADP-ribosyl) ation to generate biotinylated poly (ADP-ribose) polymers. Biotin-NAD + can be used for pull-down assays of PARylated proteins in renal epithelial cells. Biotin-NAD + is applicable to cancer-related research .
PD128763 is a selective poly(ADP-ribose) polymerase inhibitor. PD128763 results in an enhancement of Streptozotocin (HY-13753)-induced cytotoxicity. PD128763 can be used in leukemia research .
8-PIP-NAD+ (sodium) (8-Piperidino-NAD+ (sodium)) is a derivative of the signaling molecule and enzyme cofactor NAD+ (HY-B0445). 8-PIP-NAD+ (sodium) can be used in the determination of poly(ADP-ribose) polymerase (PARP) target proteins. 8-PIP-NAD+ (sodium) is a synthetic intermediate in the synthesis of cyclic ADP-ribose (cADPR) derivatives .
8-DMA-NAD+ (sodium) (8-Dimethylamino-NAD+ (sodium)) is a derivative of the signaling molecule and enzyme cofactor NAD+ (HY-B0445). 8-DMA-NAD+ (sodium) can be used in the screening of analog-sensitive poly (ADP-ribose) polymerase 1 (PARP1) gatekeeper mutations .
PARP1-IN-52 is a poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor that forms stable interactions with the PARP-1 active site. PARP1-IN-52 exerts anticancer activity against breast cancer cells. PARP1-IN-52 can be used for the research of breast cancer .
8-MA-NAD+ (sodium) (8-Methylamino-NAD+ (sodium)) is a derivative of the signaling molecule and enzyme cofactor NAD+ (HY-B0445). 8-MA-NAD+ (sodium) can be used in the screening of analog-sensitive poly (ADP-ribose) polymerase 1 (PARP1) gatekeeper mutations. 8-MA-NAD+ (sodium) can be used in the synthesis of cyclic ADP-ribose (cADPR) derivatives .
PARP1-IN-56 (Compound RCY) is an I-labeled poly(ADP−ribose) polymerase (PARP1) inhibitor. PARP1-IN-56 can be radiolabeled with 211At or 125I for use as an α-emitting radiotherapeutic agent. PARP1-IN-56 can be used for the research of cancer .
Nudifloramide- 13C,d3 (2PY- 13C,d3) is the 13C- and deuterium labeled Nudifloramide (HY-113432). Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
E7974 is a selective inhibitor of α-tubulin (α-tubulin) with an IC50 of 3.9 μM. E7974 disrupts mitotic spindle formation, induces G2-M phase cell cycle arrest, initiates apoptosis, activates caspase-3, and induces poly (ADP-ribose) polymerase cleavage. E7974 reduces the area of choroidal neovascularization in mouse models, and exerts anti-angiogenic effects when loaded in modified micelles. E7974 can be used in research related to cancer and choroidal neovascularization .
Z-FF-FMK (Z-Phe-Phe-FMK) is a cell-permeable, irreversible, and cysteine protease inhibitor targeting cathepsin-L. Z-FF-FMK inhibits angiotensin II-induced MEK activation in vascular walls, aortic medial remodeling, blood pressure elevation, and upregulation of cystatin C in aortic walls. Z-FF-FMK prevents β-amyloid-mediated caspase-3 activation, poly (ADP-ribose) polymerase cleavage, DNA fragmentation, and apoptosis of cortical neurons (apoptosis). Z-FF-FMK can be used in research related to hypertension and Alzheimer's disease .
Rolinsatamab talirine (ABBV 176) is a prolactin receptor (PRLR)-targeting antibody-drug conjugate (ADC), compoused of Rolinsatamab (HY-P99238) and SGD-1882 (HY-101127). Rolinsatamab talirine binds to PRLR to deliver a cytotoxin to tumor cells. Rolinsatamab talirine induces DNA damage, and exhibits cytotoxicity against multiple breast tumor models, including triple negative and low PRLR-expressing models. Rolinsatamab talirine demonstrates enhanced anti-tumor activity in several breast cancer models. Rolinsatamab talirine can be used for the research of breast cancer, hepatocellular carcinoma, ovarian cancer, endometrial cancer, prostate cancer, colorectal cancer, adrenocortical carcinoma, and solid tumors .
Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
4'-O-Methylbavachalcone is an orally active prenylated flavonoid that inhibits the activity of SARS-CoV papain-like protease (PLpro), with an IC50 of 10.1 μM and a Ki of 4.6 μM. 4'-O-Methylbavachalcone inhibits poly (ADP-ribose) polymerase-mediated cell death (parthanatos), reduces cerebral infarct volume, binds to the orthosteric site of SUCNR1, blocks the interaction between succinate and SUCNR1, inhibits SUCNR1 activity, blocks the nuclear translocation of NFATc4, suppresses the activation of the ERK1/2 signaling pathway, inhibits cardiomyocyte hypertrophy and restores the expression of α-actinin. 4'-O-Methylbavachalcone can be used in studies related to ischemic stroke, SARS-CoV and cardiomyocyte hypertrophy .
Nudifloramide (Standard) is the analytical standard of Nudifloramide. This product is intended for research and analytical applications. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
8-NH2-ATP tetrasodium, an inactive form of ATP, is produced by 8-NH2-Ado. 8-NH2-Ado tetrasodium induces apoptosis-related cleavage of poly (ADP-ribose) polymerase .
8-NH2-ATP, an inactive form of ATP, is produced by 8-NH2-Ado. 8-NH2-Ado is reported to be potent as shown by induction of apoptosis-related cleavage of poly (ADP-ribose) polymerase .
Eupatorin (Standard) is the analytical standard of Eupatorin. This product is intended for research and analytical applications. Eupatorin, a naturally occurring flavone, arrests cells at the G2-M phase of the cell cycle and induces apoptotic cell death involving activation of multiple caspases, mitochondrial release of cytochrome c and poly(ADP-ribose) polymerase cleavage .
Benzamide (Standard) is the analytical standard of Benzamide. This product is intended for research and analytical applications. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
Dicentrine hydrochloride is a drug with anti-inflammatory and anti-cancer activity. Dicentrine hydrochloride exerts its effects by enhancing TNF-α-induced apoptosis in A549 lung adenocarcinoma cells. Dicentrine hydrochloride increases caspase-8, -9, -3 and poly(ADP-ribose) polymerase (PARP) activities. Dicentrine hydrochloride inhibits TNF-α-induced invasion and migration of A549 cells. Dicentrine hydrochloride significantly inhibited the TNF-α-activated TAK1, p38, JNK and Akt signaling pathways, and reduced the transcriptional activities of NF-κB and AP-1 .
The TNKS1 protein is a polyADP-ribosyltransferase that is integral to multiple cellular processes, including the Wnt signaling pathway, telomere length regulation, and vesicle trafficking. In Wnt signaling, TNKS1 activates this pathway by poly-ADP-ribosylating AXIN1 and AXIN2, promoting their degradation. TNKS1 Protein, Human (His) is the recombinant human-derived TNKS1 protein, expressed by E. coli , with N-6*His labeled tag.
The TNKS1 protein is a polyADP-ribosyltransferase that is integral to multiple cellular processes, including the Wnt signaling pathway, telomere length regulation, and vesicle trafficking. In Wnt signaling, TNKS1 activates this pathway by poly-ADP-ribosylating AXIN1 and AXIN2, promoting their degradation. TNKS1 Protein, Human is the recombinant human-derived TNKS1 protein, expressed by E. coli , with tag free.
PARP6 protein, a mono-ADP-ribosyltransferase, specializes in mediating the mono-ADP-ribosylation of target proteins. PARP6 Protein, Human (sf9, His-GST) is the recombinant human-derived PARP6 protein, expressed by Sf9 insect cells , with His-GST labeled tag.
The PARP14 protein is an ADP-ribosyltransferase that uniquely mono-ADP-ribosylates glutamic acid residues on target proteins such as STAT1 and STAT6, unlike PARP1 and PARP2. It catalyzes STAT1 mono-ADP ribosylation at “Glu-657” and “Glu-705”, reduces STAT1 phosphorylation and inhibits the production of pro-inflammatory cytokines in macrophages following IFNG stimulation. PARP14 Protein, Human is the recombinant human-derived PARP14 protein, expressed by E. coli , with tag free.
PARP15 protein, acting as a mono-ADP-ribosyltransferase, facilitates the mono-ADP-ribosylation of target proteins. It also functions as a transcriptional negative regulator, impacting cellular processes and gene expression. PARP15 Protein, Human (His) is the recombinant human-derived PARP15 protein, expressed by E. coli , with N-6*His labeled tag.
The PARP14 protein is an ADP-ribosyltransferase that uniquely mono-ADP-ribosylates glutamic acid residues on target proteins such as STAT1 and STAT6, unlike PARP1 and PARP2. It catalyzes STAT1 mono-ADP ribosylation at “Glu-657” and “Glu-705”, reduces STAT1 phosphorylation and inhibits the production of pro-inflammatory cytokines in macrophages following IFNG stimulation. PARP14 Protein, Human (His, Strep) is the recombinant human-derived PARP14 protein, expressed by E. coli , with N-Strep, N-8*His labeled tag.
PARP, a poly-ADP-ribosyltransferase, catalyzes poly-ADP-ribosylation, crucial for DNA repair. This protein irreversibly binds to DNA breaks, disrupting repair processes and triggering DNA damage-induced apoptosis. PARP1 Protein, Mouse (sf9, His) is the recombinant mouse-derived PARP protein, expressed by Sf9 insect cells , with N-His labeled tag.
The PARP1 protein is a polyADP-ribosyltransferase that crucially mediates polyADP-ribosylation (PARsylation) in DNA repair, including base excision and double-strand breaks. By interacting with factors such as HPF1 and NMNAT1, the specificity of PARP1 extends to various amino acids. PARP1 Protein, Human (sf9, His) is the recombinant human-derived PARP1 protein, expressed by Sf9 insect cells , with C-His labeled tag.
Nudifloramide-d3 (2PY-d3) is the deuterium labeled Nudifloramide. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
Benzamide-d5 (Benzenecarboxamide-d5) is deuterium labeled Benzamide. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
Floxuridine- 13C, 15N2 (5-Fluorouracil 2'-deoxyriboside- 13C, 15N2) is the 13C- and 15N-labeled labeled Floxuridine (HY-B0097). Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
Mycophenolic Acid-d3 Acyl-Beta-D-glucuronide is the deuterium labeled Mefuparib (HY-167927). Mefuparib (CVL218) is a poly ADP-ribosepolymerase (PARP) inhibitor used in cancer research that exhibits potent brain penetration due to its high protein binding.
Nudifloramide- 13C,d3 (2PY- 13C,d3) is the 13C- and deuterium labeled Nudifloramide (HY-113432). Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
2'-Fluoro-5'-O-DMT-2'-deoxyinosine-3'-CE-phosphoramidite is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
6-O-Methylinosine is a hypoxanthine analogue. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
Etidaligide sodium, an AsiDNA, a first-in-class DNA repair inhibitor designed to prevent the repair of DNA damage in tumour cells. It also activates DNA-dependent protein kinase (DNA-PK) and poly (ADP-ribose) polymerase enzymes that induce phosphorylation
Etidaligide, an AsiDNA, a first-in-class DNA repair inhibitor designed to prevent the repair of DNA damage in tumour cells. It also activates DNA-dependent protein kinase (DNA-PK) and poly (ADP-ribose) polymerase enzymes that induce phosphorylation of H2A
2'-O-Methyl-5'-O-dmt-inosine-3'-CE-phosphoramidite is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
2′-C-Methyl-6-O-methylinosine is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
2-Chloro-2'-deoxy-6-O-methylinosine is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
6-Methoxypurine-9-β-D-5’(R)-C-methylriboside is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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