Search Result
Results for "
PARP-IN-1
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-12022
-
PARP-IN-1
|
PARP
|
Cancer
|
3-Aminobenzamide (PARP-IN-1) is a potent inhibitor of PARP with IC50 of appr 50 nM in CHO cells, and acts as a mediator of oxidant-induced myocyte dysfunction during reperfusion.
|
-
-
- HY-161302
-
|
Apoptosis
DNA/RNA Synthesis
PARP
|
Cancer
|
Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity [1].
|
-
-
- HY-108632
-
|
PARP
|
Cancer
|
BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC50 of 7.35 (pKi=7.05), and murine PARP-2 (mPARP-2) with a pIC50 of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1 [1].
|
-
-
- HY-164475
-
|
PARP
|
Cancer
|
PARP1-IN-29 is an orally active PARP-1 inhibitor with an IC50 value of 6.3 nM. PARP1-IN-29, after being labeled with [18F], can be used for positron emission tomography (PET) imaging, specifically targeting PARP-1 in tumors. PARP1-IN-29 is applicable in the fields of oncology and imaging research, particularly for detecting PARP-1 activity in cancer [1].
|
-
-
- HY-155965
-
|
VEGFR
PARP
Apoptosis
|
Cancer
|
VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC50s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC50: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent [1].
|
-
-
- HY-157165
-
|
Microtubule/Tubulin
PARP
|
Cancer
|
Tubulin/PARP-IN-1 (compound 14) is a dual PARP-tubulin inhibitor with activity against endometrial cancer. Tubulin/PARP-IN-1 inhibits PARP and tubulin with IC50s of 74 nM (PARP1), 109 nM (PARP2), and 1.4 μM (Microtubule/Tubulin), respectively. Tubulin/PARP-IN-1 can induce apoptosis and autophagy and cause cell cycle arrest in the G2/M phase [1].
|
-
-
- HY-105253
-
|
PARP
|
Neurological Disease
|
PARP-2/1-IN-2 (Compound 4a), the enantiomer of Veliparib (HY-10129), is a potent PARP inhibitor with Kis of 2 and 5 nM against PARP-2 and PARP-1, respectively. PARP-2/1-IN-2 has an EC50 of 3 nM in a cell based assay of PARP activity .
|
-
-
- HY-15050
-
-
-
- HY-161288
-
|
PARP
|
Cancer
|
UKTT15 (compound 6) is an allosteric inhibitor of PARP1 .
|
-
-
- HY-157137
-
|
PARP
Caspase
Apoptosis
|
Cancer
|
PARP1-IN-17 is a PARP-1 inhibitor (IC50 = 19.24 nM for PARP-1 and = 32.58 nM for PARP-2) and induce apoptosis. PARP1-IN-17 shows excellent anti-proliferative activity [1].
|
-
-
- HY-13688
-
|
PARP
|
Cancer
|
PJ34 hydrochloride is an inhibitor of PARP1/2 with IC50 of 110 nM and 86 nM, respectively.
|
-
-
- HY-153590
-
|
PARP
|
Cancer
|
PARP-1-IN-4 is a PARP-1 inhibitor. PARP-1-IN-4 has inhibitory activity against PARP-1 with IC50 value of 302 μM. PARP-1-IN-4 can be used for the research of lung adenocarcinoma [1].
|
-
-
- HY-158251
-
|
Others
|
Cancer
|
BIBD-300 is a PARP-1 imaging agent with high affinity for PARP-1. BIBD-300 can accurately localize C6 and U87MG tumors, which can be used for research in the diagnosis of breast cancer, prostate cancer, glioma, and liver cancer [1].
|
-
-
- HY-116218C
-
JPI-289 hydrochloride
|
PARP
|
Cardiovascular Disease
Neurological Disease
|
Amelparib (JPI-289) hydrochloride is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib hydrochloride inhibits PARP-1 activity (IC50 = 18.5 nM) and cellular PAR formation (IC50 = 10.7 nM). Amelparib hydrochloride is a potential neuroprotective agent. Amelparib hydrochloride has the potential for the research of acute ischaemic stroke [1].
|
-
-
- HY-10162S
-
AZD2281-d5; KU0059436-d5
|
PARP
Autophagy
Mitophagy
|
Cancer
|
Olaparib-d5 is a deuterium labeled Olaparib. Olaparib is a potent and oral PARP inhibitor[1].
|
-
-
- HY-168657
-
|
PARP
|
Others
|
PARP1/2-IN-4 (compound 3) is a PARP1/2 inhibitor [1].
|
-
-
- HY-18954
-
|
PARP
|
Cancer
|
NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy.
|
-
-
- HY-U00223
-
|
PARP
|
Cancer
|
WD2000-012547 is a selective poly(ADP-ribose)-polymerase (PARP-1) inhibitor with a pKi of 8.221.
|
-
-
- HY-116218
-
JPI-289 free base
|
PARP
|
Cardiovascular Disease
Neurological Disease
|
Amelparib (JPI-289 free base) is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib inhibits PARP-1 activity (IC50=18.5 nM) and cellular PAR formation (IC50=10.7 nM) in the nanomolar range. Amelparib is a potential neuroprotective agent. Amelparib has the potential for the research of acute ischaemic stroke [1].
|
-
-
- HY-14478
-
|
PARP
|
Cancer
|
UPF 1069 is a PARP inhibitor, with IC50s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively.
|
-
-
- HY-108413
-
BMN 673ts
|
PARP
|
Cancer
|
Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.
|
-
-
- HY-Z0283S
-
Benzenecarboxamide-15N; Phenylamide-15N
|
Endogenous Metabolite
PARP
|
Others
|
Benzamide- 15N is a 15N-labeled Benzamide. Benzamide inhibits poly(ADP-ribose) polymerase (PARP)[1][2].
|
-
-
- HY-145328
-
|
PARP
|
Others
|
PARP-1/2-IN-1 is a potent PARP-1/2 inhibitor with IC50 of 0.51 nM and 23.11 nM, respectively.
|
-
-
- HY-149800
-
|
PARP
Apoptosis
Caspase
|
Cancer
|
PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. PARP-1-IN-3 induces apoptosis and arrest cell cycle at G2/M phase. PARP-1-IN-3 can be used in research of cancer [1].
|
-
-
- HY-132157
-
|
PARP
|
Others
|
8-Chloroquinazolin-4-ol (Compd 18) is a PARP-1 enzyme inhibitor, with an IC50 of 5.65 μM [1].
|
-
-
- HY-161606
-
|
PARP
|
Cancer
|
PARP-1/2/7-IN-1 (compound 86) is a potent inhibitor of PARP-1/2/7, with the IC50 of < 10 nM [1].
|
-
-
- HY-145734A
-
|
Microtubule/Tubulin
|
Cancer
|
AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors [1].
|
-
-
- HY-145734
-
|
Microtubule/Tubulin
|
Cancer
|
AMXI-5001 is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 induces complete regression of established tumors, including exceedingly large tumors [1].
|
-
-
- HY-12032
-
AG14361
4 Publications Verification
|
PARP
|
Cancer
|
AG14361 is a potent PARP-1 inhibitor, with a Ki of < 5 nM, and in permeabilized SW620 and intact SW620 cells, the IC50s are 29 nM and 14 nM, respectively.
|
-
-
- HY-128599
-
|
PARP
|
Cancer
|
NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a Kd of 16 nM and an IC50 of 27 nM (in Hela cells). Anti-tumor activity [1].
|
-
-
- HY-W156961
-
|
PARP
|
Neurological Disease
|
LS-75 is a PARP-1 inhibitor with blood-brain permeability and IC50 value of 18 μM. LS-75 has neuroprotective activity [1].
|
-
-
- HY-119653
-
|
PARP
|
Cancer
|
AZ9482 is a triple PARP1/2/6 inhibitor, with IC50 values of 1 nM, 1 nM and 640 nM for PARP1, PARP2 and PARP6, respectively [1].
|
-
-
- HY-137450
-
IMP4297; JS109
|
PARP
|
Cancer
|
Senaparib (IMP4297) is a highly potent, selective and orally active PARP1/2 inhibitor. Senaparib (IMP4297) exhibits strong antitumor activity in animal models [1].
|
-
-
- HY-137450A
-
IMP4297 hydrochloride; JS109 hydrochloride
|
PARP
|
Cancer
|
Senaparib hydrochloride (IMP4297 hydrochloride) is an oral, selective PARP1/2 inhibitor with potent anti-tumor activity. Senaparib hydrochloride shows antitumor activity against advanced ovarian cancer [1].
|
-
-
- HY-169299
-
|
PARP
Topoisomerase
Apoptosis
|
Cancer
|
TOPOI/PARP-1-IN-2 (compound 6c) is a dual PARP-1 and topoisomerase 1 (TOPO-1) inhibitor with IC50s of 32.2 nM and 46.2 nM, respectively. TOPOI/PARP-1-IN-2 shows a selectivity for PARP-1 over PARP-2. TOPOI/PARP-1-IN-2 disrupts the cell cycle at the S phase and induces apoptosis in NCI-60 cancer cell lines [1].
|
-
-
- HY-113432
-
2PY
|
Endogenous Metabolite
PARP
|
Metabolic Disease
|
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 [1].
|
-
-
- HY-34386
-
|
PARP
|
Inflammation/Immunology
Cancer
|
6(5H)-Phenanthridinone is a potent PARP-1 inhibitor and immunomodulator. 6(5H)-Phenanthridinone inhibits cell proliferation and can be used in cancer research [1].
|
-
-
- HY-153581
-
|
PARP
|
Others
|
ARTD3/PARP3-IN-1 is an unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3)/PARP3 .
|
-
-
- HY-123232
-
|
PARP
|
Cancer
|
KU-0058684 is a potent PARP inhibitor, with an IC50 of 3.2 nM for PARP-1. KU-0058684 significantly reduces DNA double strand break (DSB) repair [1] .
|
-
-
- HY-164757
-
-
-
- HY-N7569
-
|
Apoptosis
Caspase
PPAR
|
Cancer
|
Demethoxyfumitremorgin C is a secondary metabolite of the marine fungus, Aspergillus fumigatus. Demethoxyfumitremorgin C induces prostate cancer cell apoptosis. Demethoxyfumitremorgin C activates caspase-3, -8, and -9, leading to PARP/ cleavage .
|
-
-
- HY-146336
-
|
PARP
Apoptosis
|
Cancer
|
PARP1/2/TNKS1/2-IN-1 (Compound I-9) is a dual PARP-1, PARP-2, TNKS1 and TNKS2 inhibitor with IC50 values of 0.25 nM, 1.2 nM, 13.5 nM and 4.15 nM against PARP-1, PARP-2, TNKS1 and TNKS2, respectively. PARP1/2/TNKS1/2-IN-1 exhibits favorable synergistic antitumor efficacy and induces apoptosis [1].
|
-
-
- HY-132297A
-
|
PARP
|
Cancer
|
PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer [1].
|
-
-
- HY-132297
-
|
PARP
|
Cancer
|
PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer [1].
|
-
-
- HY-162363
-
|
PARP
|
Neurological Disease
|
MD6a is a melatonin derivative with inhibitroy activity towards PARP-1, which maintains proteins hemostasis and improves mitochondrial function through TOR/HSF-1 signaling. MD6a a neuroprotective effect [1].
|
-
-
- HY-163658
-
|
PARP
|
Cancer
|
PARP-1-IN-23 (Compound I16 ) is an orally active and selective PARP-1 inhibitor with the IC50 of 12.38 nM. PARP-1-IN-23 inhibits tumor growth in vivo [1].
|
-
-
- HY-130644
-
|
PROTACs
PARP
|
Cancer
|
iRucaparib-AP6 is a highly efficient and specific PROTAC PARP1 degrader. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1 [1].
|
-
-
- HY-122661
-
MPH
|
PARP
Apoptosis
|
Cancer
|
Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo [1] .
|
-
-
- HY-105303
-
|
PARP
|
Cancer
|
CEP-9722, the proagent of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects [1] .
|
-
-
- HY-117423
-
|
PARP
|
Cancer
|
ST7710AA1 (compound 1l) is a potent PARP-1 inhibitor with an IC50 value of 0.07 µM. ST7710AA1 shows an antiproliferative activity. ST7710AA1 shows anticancer activity [1].
|
-
- HY-16106
-
Talazoparib
Maximum Cited Publications
71 Publications Verification
BMN-673; LT-673
|
PARP
|
Cancer
|
Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity [1].
|
-
- HY-134354
-
ADP-ribose-pNP
|
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Others
|
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 .
|
-
- HY-164713
-
|
Others
|
Others
|
PARP1-IN-31 (compound 11f) is a phthalazinone-based compound, an anti-lung adenocarcinoma compound with inhibitory activity against PARP-1 (IC50 value of 97 nM), inducing apoptosis and inhibiting cell proliferation in lung cancer cell lines.
|
-
- HY-113432R
-
2PY (Standard)
|
Endogenous Metabolite
PARP
|
Metabolic Disease
|
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 [1].
|
-
- HY-149348
-
|
Topoisomerase
PARP
Apoptosis
|
Cancer
|
DiPT-4 is a dual TOP1/PARP1 inhibitor that induces massive DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells. DiPT-4 has the potential to overcome cancer drug resistance [1].
|
-
- HY-134354A
-
ADP-ribose-pNP disodium
|
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Others
|
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 .
|
-
- HY-114869
-
DPQ
1 Publications Verification
|
PARP
|
Neurological Disease
|
DPQ is a potent PARP-1 inhibitor. DPQ can reduce the N-methyl-d-aspartate (NMDA)-induced PARP activation, restoring ATP to near control levels and significantly attenuating neuronal injury in the severe NMDA exposure model. DPQ can be used for researching neuroprotection [1].
|
-
- HY-14688
-
|
PARP
|
Cancer
|
CEP-8983 is a PARP-1 and PARP-2 inhibitor (IC50: 20 and 6 nM). CEP-8983 is an effective chemosensitizing agent, and can sensitize chemotherapy-resistant cell lines and subcutaneous xenografts to Temozolomide (HY-17364) and Camptothecin (HY-16560) [1].
|
-
- HY-130073
-
|
NF-κB
Apoptosis
|
Cancer
|
Amorfrutin A is the inhibition of NF-κB activation, that inhibits TNF-α-induced IκBα degradation, p65 nuclear translocation, and DNA-binding activity. Amorfrutin A promotes TNF-α-induced apoptosis in HeLa cell through promotion of caspase-3 and PARP proteolysis .
|
-
- HY-144642
-
|
PARP
|
Cancer
|
PARP-1-IN-1 is a high selective and orally active PARP-1 inhibitor (IC50=0.96 nM). PARP-1-IN-1 has well tolerance and remarkable single dose activity in the MDA-MB-436 xenotransplantation model [1].
|
-
- HY-113432S
-
|
Endogenous Metabolite
PARP
|
Metabolic Disease
|
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[1].
|
-
- HY-105692
-
|
PARP
|
Neurological Disease
|
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 [1] .
|
-
- HY-156419
-
|
PARP
|
Cancer
|
PARP7-IN-16 (compound 36) is a potent, selective and orally active inhibitor of PARP-1/2/7, with IC50s of 0.94, 0.87 and 0.21 nM, respectively. PARP7-IN-16 can be used for the research of breast cancer and prostate cancer [1].
|
-
- HY-157212
-
|
Apoptosis
PARP
Proteasome
|
Cancer
|
PARP-1/Proteasome-IN-1 (compound 42i) is a dual PARP-1 and proteasome inhibitor with significant inhibitory effects on breast cancer. PARP-1/Proteasome-IN-1 can downregulate the expression of BRCA1 and RAD51 to inhibit homologous recombination repair function and induce apoptosis [1].
|
-
- HY-W006566
-
5-AmINoisoquINolIN-1-one
|
PARP
|
Cancer
|
5-AIQ (5-Aminoisoquinolin-1-one) is a water-soluble PARP-1 inhibitor. 5-AIQ is an important functional group in various drugs. 5-AIQ reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the research conditions associated with ischemia-reperfusion of the liver [1] .
|
-
- HY-155122
-
|
PARP
|
Cancer
|
PARP-1-IN-13 (Compound 19c) is a PARP-1 inhibitor (IC50: 26 nM). PARP-1-IN-13 inhibits DNA single-strand breakage repair and aggravates DNA double-strand breakage. PARP-1-IN-13 promotes the apoptosis of cancer cells through the mitochondrial apoptosis pathway [1].
|
-
- HY-10885
-
ABT-472
|
PARP
|
Cancer
|
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 [1].
|
-
- HY-10617
-
AG-014699 phosphate; PF-01367338 phosphate
|
PARP
|
Cancer
|
Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
|
-
- HY-10617A
-
AG014699; PF-01367338
|
PARP
|
Cancer
|
Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research [1] .
|
-
- HY-10617D
-
AG014699 acetate; PF-01367338 acetate
|
PARP
|
Cancer
|
Rucaparib (AG014699) acetate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib acetate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib acetate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
|
-
- HY-10617B
-
AG014699 hydrochloride; PF-01367338 hydrochloride
|
PARP
|
Cancer
|
Rucaparib (AG014699) hydrochloride is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib hydrochloride is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib hydrochloride has the potential for castration-resistant prostate cancer (CRPC) research [1] .
|
-
- HY-102003
-
AG014699 monocamsylate; PF-01367338 monocamsylate
|
PARP
|
Cancer
|
Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib monocamsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib monocamsylate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
|
-
- HY-102003A
-
AG014699 camsylate; PF-01367338 camsylate
|
PARP
|
Cancer
|
Rucaparib (AG014699) camsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib camsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib camsylate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
|
-
- HY-10617C
-
AG-014699 tartrate; PF-01367338 tartrate
|
PARP
|
Cancer
|
Rucaparib (AG014699) tartrate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
|
-
- HY-107545
-
|
Dynamin
|
Cancer
|
Dynole 34-2 is a dynamin GTPase inhibitor (IC50s=6.9 and 14.2 µM for dynamin1 and dynamin2 GTPase activity, respectively) with antimitotic effect. Dynole 34-2 induces apoptosis, as revealed by cell blebbing, DNA fragmentation, and PARP cleavage . Dynole 34-2 also potently inhibits receptor mediated endocytosis (RME) .
|
-
- HY-148710
-
|
PARP
|
Inflammation/Immunology
|
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 [1].
|
-
- HY-149735
-
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC50=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage .
|
-
- HY-155458
-
|
PARP
|
Inflammation/Immunology
Cancer
|
HYDAMTIQ is a PARP-1/2 inhibitor (IC50: 29-38 nM) with anticancer, anti-inflammatory, and ischemic protective effects. HYDAMTIQ inhibits pulmonary PARP activity, is effective against allergen-induced cough and dyspnea, and inhibits bronchial hyperresponsiveness to methacholine. HYDAMTIQ has broad-spectrum tumor suppressor effects, including ovarian and breast cancers, prostate and pancreatic tumors, and glioblastoma multiforme. HYDAMTIQ has demonstrated in vivo efficacy in animal models of cerebral ischemia, asthma, cancer, and more [1].
|
-
- HY-161868
-
|
PARP
HDAC
Apoptosis
|
Cancer
|
DLC-50 is a dual inhibitor for PARP-1 and HDAC-1 with IC50 of 1.2 nM and 31 nM. DLC-50 inhibits the proliferation of cancer cells MDA-MB-436, MDA-MB-231, and MCF-7 with IC50 of 0.3, 2.7 and 2.41 μM. DLC-50 induces apoptosis in MDA-MB-231, arrests the cell cycle at G2 phase [1].
|
-
- HY-156419A
-
|
PARP
|
Cancer
|
PARP7-IN-16 free base is the free base form of PARP7-IN-16 (HY-156419). PARP7-IN-16 free base is a selective and orally active inhibitor of PARP-1/2/7, with IC50s of 0.94, 0.87 and 0.21 nM, respectively. PARP7-IN-16 can be used for the research of breast cancer and prostate cancer [1].
|
-
- HY-155993
-
|
PARP
|
Cancer
|
YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats [1].
|
-
- HY-163983
-
|
Microtubule/Tubulin
Apoptosis
PARP
Caspase
|
Cancer
|
Tubulin polymerization-IN-68 (compound 32) is a tubulin inhibitor that can inhibit tubulin polymerization and destroy the cellular microtubule network. Tubulin polymerization-IN-68 can upregulate the expression of PARP-1 and caspase-3 and induce cell apoptosis, and has anticancer activity. Tubulin polymerization-IN-68 can effectively inhibit HepG2 (IC50=93 nM) and significantly inhibit the growth of HepG2 xenograft tumors in nude mice by oral administration [1].
|
-
- HY-115552
-
|
PARP
|
Cancer
|
Simmiparib is a highly potent and orally active PARP1 and PARP2 inhibitor with IC50 values of 1.75 nM and 0.22 nM, respectively. Simmiparib has more potent PARP1/2 inhibition than its parent Olaparib (HY-10162). Simmiparib induces DNA double-strand breaks (DSB) accumulation and G2/M arrest in homologous recombination repair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts [1].
|
-
- HY-145749
-
|
PARP
|
Cancer
|
PARPYnD is a PARP enzyme photoaffinity probe (AfBP) based on the triple PARP1/2/6 inhibitor AZ9482 (HY-119653), which induces breast cancer Formation of multipolar spindles (MPS) in cells. PARPYnD inhibits PAPR wih IC50 of 38 nM (PARP1), 6 nM (PARP2), 230 nM (PARP6), respectively. PARPYnD enriches recombinant PARP6 incorporated into cell lysates and inhibits PARP6 in cell-free assays, but it does not label PARP6 in intact cells [1].
|
-
- HY-115862
-
|
Adenosine Receptor
PARP
Aurora Kinase
|
Cardiovascular Disease
Cancer
|
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-ribose polymerase-1 (PARP-1) and aurora kinase A, with IC50 of 0.311 and 5.5 μM [1] .
|
-
- HY-148709
-
|
PARP
|
Inflammation/Immunology
|
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 [1].
|
-
- HY-15048
-
|
PARP
|
Inflammation/Immunology
|
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 demonstrated strong anti-inflammatory effects. It reduced inflammatory cell infiltration, histological injury, and delayed clinical signs of inflammation. GPI 15427 also diminished the accumulation of poly (ADP-ribose) in the ileum and colon of treated rats. These results suggest GPI 15427 could be useful for treating intestinal ischemia and inflammation [1].
|
-
- HY-133124
-
|
PARP
PI3K
Apoptosis
|
Cancer
|
PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases [1].
|
-
- HY-N3584
-
Chonglou SaponIN VII
|
Akt
p38 MAPK
P-glycoprotein
Bcl-2 Family
Caspase
PARP
Autophagy
Apoptosis
|
Cancer
|
Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia [1].
|
-
- HY-N3584R
-
|
Akt
p38 MAPK
P-glycoprotein
Bcl-2 Family
Caspase
PARP
Autophagy
Apoptosis
|
Cancer
|
Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia [1].
|
-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10162S
-
|
Olaparib-d5 is a deuterium labeled Olaparib. Olaparib is a potent and oral PARP inhibitor[1].
|
-
-
- HY-Z0283S
-
|
Benzamide- 15N is a 15N-labeled Benzamide. Benzamide inhibits poly(ADP-ribose) polymerase (PARP)[1][2].
|
-
-
- HY-113432S
-
|
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[1].
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-145749
-
|
|
Alkynes
|
PARPYnD is a PARP enzyme photoaffinity probe (AfBP) based on the triple PARP1/2/6 inhibitor AZ9482 (HY-119653), which induces breast cancer Formation of multipolar spindles (MPS) in cells. PARPYnD inhibits PAPR wih IC50 of 38 nM (PARP1), 6 nM (PARP2), 230 nM (PARP6), respectively. PARPYnD enriches recombinant PARP6 incorporated into cell lysates and inhibits PARP6 in cell-free assays, but it does not label PARP6 in intact cells [1].
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: