Search Result
Results for "
Adverse events parp Inhibitors
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
10
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-125218
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ITK7
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PARP
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Cancer
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PARP11 inhibitor ITK7 (ITK7) is a potent and selective PARP11 inhibitor. PARP11 inhibitor ITK7 can potently inhibit PARP11 with an IC50 value of 14 nM. PARP11 inhibitor ITK7 can be used for the research of cellular localization .
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- HY-153590
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PARP
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Cancer
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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 .
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- HY-149800
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PARP
Apoptosis
Caspase
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Cancer
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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 .
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- HY-148754
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PARP
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Cancer
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PARP10-IN-3 is a selective mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 480 nM for human PARP10. PARP10-IN-3 reveals potent inhibition on PARP2 and PARP15 with IC50s of 1.7 μM for human PARP2 and human PARP15, respectively .
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- HY-162884
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β-glucuronidase
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Infection
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EcGUS-IN-1 (Compound E-9) is a non-competitive β-glucuronidase inhibitor, with an IC50 of 2.68 μM and a Ki value of 1.64 μM. EcGUS-IN-1 can improve gastrointestinal adverse events (GIAE) caused by Escherichia coli infection by inhibiting E. coli β-glucuronidase activity .
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- HY-159612
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PARP
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Cancer
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PARP1-IN-28 (compound 1) is a PARP1 inhibitor. PARP1-IN-28 can be used in the study of cancer .
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- HY-157490
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PARP
HDAC
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Cancer
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PARP/HDAC-IN-1 (compound B102) is a potent dual inhibitor of PARP and HDAC. PARP/HDAC-IN-1 inhibits PARP1, PARP2 and HDAC1 with IC50s of 19.01, 2.13, 1690 nM, respectively .
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- HY-157165
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Microtubule/Tubulin
PARP
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Cancer
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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 .
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- HY-141486A
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- HY-157137
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PARP
Caspase
Apoptosis
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Cancer
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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 .
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- HY-164475
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PARP
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Cancer
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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 .
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- HY-D1188
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PARP
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Cancer
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PARP7-probe-1 is a chemiluminescent labeled PARP7 probe. PARP7-probe-1 is a biotinylated probe binding to the PARP7 active site. PARP7-probe-1 can be used for the research of PARP7 function .
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- HY-148753
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PARP
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Cancer
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PARP10-IN-2 is a potent mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 3.64 μM for human PARP10. PARP10-IN-2 reveals potent inhibition on PARP2 and PARP15 with IC50s of 27 μM and 11 μM for human PARP2 and human PARP15, respectively .
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- HY-106029
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α-TPA
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Others
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Cancer
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4α-TPA is an inactive form of TPA, and is used as a negative control for TPA-activated events .
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- HY-151625
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PARP
Apoptosis
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Cancer
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PARP-2-IN-3 (Compound 12) is a potent PARP-2 inhibitor with an IC50 of 0.07 μM. PARP-2-IN-3 induces apoptosis and necrosis in cancer cells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability .
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- HY-164757
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- HY-102035
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PARP
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Cancer
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PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC50 of 11.5 nM.
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- HY-132297A
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PARP
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Cancer
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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 .
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- HY-132297
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PARP
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Cancer
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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 .
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- HY-163658
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PARP
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Cancer
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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 .
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- HY-147886
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PARP
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Cancer
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PARP1-IN-11 (compound 49) is a potent PARP1 inhibitor with IC50 value of 0.082 µM. PARP1-IN-11 shows complete inhibition of PARP2 and substantially inhibits PARP3, TNKS1 and TNKS2 .
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- HY-151624
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PARP
Apoptosis
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Cancer
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PARP-2-IN-2 (compound 27) is a PARP‑2 inhibitor with an IC50 value of 0.057 µM. PARP-2-IN-2 induces cell cycle arrest and apoptosis of MCF-7 breast cancer cells. PARP-2-IN-2 can be used for the research of cancer .
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- HY-168094
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PARP
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Cancer
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PARP1-IN-30 (Compound 3) is a specific and potent PARP1 inhibitor with cytotoxicity. PARP1-IN-30 allows precise inhibition of PARP1 in tumor cells with breast cancer 1 protein (BRCA1) or BRCA2 deficiencies. PARP1-IN-30 is promising for research of cancers .
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- HY-155246
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Apoptosis
PARP
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Cancer
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PARP1-IN-15 (Compound 6) is a PARP1 inhibitor. PARP1-IN-15 inhibits tankyrase (TNKS) and facilitates DNA double-strand breaks damage. PARP1-IN-15 induces tumor cell apoptosis. PARP1-IN-15 has anti-cancer activity in triple-negative breast cancer (TNBC) cells and TNBC patient-derived organoids. PARP1-IN-15 can be used for research of TNBC with or without BRCA1 mutations .
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- HY-155122
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PARP
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Cancer
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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 .
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- HY-151609
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PARP
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Cancer
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PARP7-IN-12 is a potent PARP7 Inhibitor with an IC50 value of 7.836 nM. PARP7-IN-12 can be used in research of cancer .
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- HY-163492
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PARP
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Cancer
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PARP7-IN-19 (compound 5a) is an inhibitor of PARP7 ( IC50 ≤10nM). PARP7-IN-19 can be used in the research area of tumors .
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- HY-105253
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PARP
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Neurological Disease
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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 .
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- HY-163081
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PARP
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Cancer
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PARP7-IN-17 is a potent inhibitor of PARP7 with IC50 of 4.5 nM that has oral bioavailability. PARP7-IN-17 displays antitumor effect .
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- HY-162114
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PARP
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Cancer
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PARP1-IN-18 (compound 25) is a potent PARP1 inhibitor with an IC50 value of 2.7 nM. PARP1-IN-18 has anticancer effects .
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- HY-149001
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PARP
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Cancer
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PARP1-IN-9 (Compound 5c) is a PARP1 inhibitor with an IC50 of 30.51 nM. PARP1-IN-9 induces cell apoptosis and shows anticancer activity. PARP1-IN-9 has higher potency than Olaparib (HY-10162) .
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- HY-162172
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PARP
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Cancer
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Parp7-in-18 (Compund 8) is a selective PARP7 inhibitor with an IC50 of 0.11 nM. PARP7-IN-18 exhibits good anticancer activity and pharmacokinetic properties .
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- HY-144642
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PARP
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Cancer
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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 .
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- HY-147027
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PARP
Caspase
Apoptosis
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Cancer
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PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis .
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- HY-156419
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PARP
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Cancer
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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 .
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- HY-168657
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PARP
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Others
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PARP1/2-IN-4 (compound 3) is a PARP1/2 inhibitor .
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- HY-150765
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PARP
Apoptosis
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Cancer
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PARP1-IN-12 is a potent PARP1 inhibitor with an IC50 of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells .
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- HY-146502
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PARP
Apoptosis
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Cancer
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PARP10/15-IN-3 (Compound 8a) is a potent PARP10 and PARP15 dual inhibitor with IC50 values of 0.14 µM and 0.40 µM against PARP10 and PARP15, respectively. PARP10/15-IN-3 is able to enter cells and rescue cells from apoptosis .
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- HY-156298
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PARP
Apoptosis
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Cancer
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PARP1-IN-16 (compound 12a) is a potent PARP1 inhibitor, with an IC50 of 1.89 nM. PARP1-IN-16 can arrest the cell cycle in S phase and induce apoptosis in HCT-116 cells .
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- HY-158680
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PARP
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Cancer
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PARP1-IN-21 (example 16) is a potent inhibitor of PARP1, with the IC50 of ＜ 10 nM .
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- HY-158681
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PARP
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Cancer
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PARP1-IN-22 (compound 15) is a potent inhibitor of PARP1, with the IC50 of ＜ 10 nM .
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- HY-161607
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PARP
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Cancer
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PARP7-IN-21 (compound 128) is a potent inhibitor of PARP7, with the IC50 of ＜ 10 nM .
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- HY-146501
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PARP
Apoptosis
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Cancer
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PARP10/15-IN-2 (Compound 8h) is a potent PARP10 and PARP15 dual inhibitor with IC50 values of 0.15 µM and 0.37 µM against PARP10 and PARP15, respectively. PARP10/15-IN-2 is able to enter cells and rescue cells from apoptosis .
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- HY-157320
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin/PARP-IN-2 (compound 14) is a dual PARP-Tubulin inhibitor. Tubulin/PARP-IN-2 inhibits PARP1, PARP2, and tubulin activity with IC50 values of 74 nM, 109 nM, and 1.4 µM, respectively. Tubulin/PARP-IN-2 induces apoptosis as well as autophagy. Tubulin/PARP-IN-2 causes cell cycle arrest at the G2/M phase .
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- HY-160417
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PARP
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Cancer
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PARP1-IN-19 is a PARP1 inhibitor with antitumor effects (CN107955001A; Embodiment 3) .
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- HY-143398
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PARP
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Cancer
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PARP10/15-IN-1 (compound 8l) is a potent inhibitor of dual inhibitor of PARP10 and PARP15, with IC50s of 160 nM and 370 nM, respectively. PARP10/15-IN-1 can be used for cancer .
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- HY-142657
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PARP
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Cancer
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PARP1-IN-7 is an inhibitor of poly(ADP-ribose) polymerase-1 (PARP1) as an anticancer agent.
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- HY-163719
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PARP
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Cancer
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PARP7-IN-22 (XLY-1) is a PARP7 inhibitor with an IC50 of 0.6 nM. PARP7-IN-22 (XLY-1) is orally active, enhances type I interferon signaling in vitro, restores type I interferon signaling, promotes T cell infiltration into tumor tissues, and significantly inhibits tumor growth. PARP7-IN-22 shows promise for research in the field of cancer immunotherapy .
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- HY-145328
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PARP
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Others
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PARP-1/2-IN-1 is a potent PARP-1/2 inhibitor with IC50 of 0.51 nM and 23.11 nM, respectively.
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- HY-147030
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PARP
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Cancer
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PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549 .
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- HY-155351
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PARP
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Cancer
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PARP7-IN-15 (Compound 18) is a PARP7 inhibitor with IC50 of 0.56 nM, that has antitumor activity .
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- HY-162349
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HDAC
PARP
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Cancer
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PARP7/HDACs-IN-1 (compound 9l) is a dual-target inhibitor targeting PARP7/HDAC with anti-tumor activity. PARP7/HDACs-IN-1 inhibits different subtypes of PARPs and HDACs with IC50s of 83.3 nM (PARP1), 3.1 nM (PARP7), 35 nM (HDAC1), 30.3 nM (HDAC2), 35.4 nM (HDAC3), and 6.4 nM respectively. (HDAC6) . br/ .
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- HY-169299
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PARP
Topoisomerase
Apoptosis
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Cancer
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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 .
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- HY-164926
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PARP
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Neurological Disease
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PARP1-IN-33 (Example 6) is a PARP1 inhibitor (IC50: 0.41 nM). PARP1-IN-33 has retinal cytoprotective effect, with an EC50 of 0.02 nM (inhibition on MTS activity of H2O2 induced human retinal pigment epithelial cell) .
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- HY-149003
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PARP
Apoptosis
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Cancer
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PARP1-IN-10 (compound 12c) is a no-cytotoxicity and potent PARP1 inhibitor with an IC50 value of 50.62 nM in vitro. PARP1-IN-10 causes cell cycle arrest at G2/M phase and apoptosis, and enhances the cytotoxicity of temozolomide (TMZ) .
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- HY-149398
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Apoptosis
PARP
CDK
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Cancer
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PARP-1/2-IN-2-IN-1 (Compound 12e) is a PARP1/2/CDK12 inhibitor (IC50: 34, 30 and 285 nM respectively). PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor .
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- HY-163817
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PARP
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Cancer
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PARP1/2-IN-3 (Compound 29) is an orally active inhibitor for PARP 1 and PARP 2 with IC50 of 0.2235 nM and <0.001 nM. PARP1/2-IN-3 inhibits the proliferation of Capan-1 wildtype, AZD2281 or BMN673 resistant cells with IC50 of 1.82-9.98 nM. PARP1/2-IN-3 exhibits antitumor efficacy in mice .
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- HY-139879
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PARP
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Cancer
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PARP1-IN-6 is a dual tubulin/PARP-1 inhibitor with IC50 values of 0.94 and 0.48 μM, respectively.
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- HY-161934
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PARP
Reactive Oxygen Species
Apoptosis
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Cancer
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PARP1-IN-27 (Compound 9B) is the inhibitor for PARP1 and PARP2, with IC50 of 2.53 nM and 6.45 nM in cell SUM149PT. PARP1-IN-27 inhibits the proliferation of BRCA-mutated cancer cells SUM149PT, HCC1937 and Capan-1, with IC50 of 0.62, 1.91 and 4.26 μM respectively. PARP1-IN-27 aggravates DNA double-strand breaks, increases ROS generation, arrests cell cycle at G2/M phase, and induces apoptosis in SUM149PT .
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- HY-156419A
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PARP
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Cancer
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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 .
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- HY-146160
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PARP
HDAC
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Cancer
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PARP-1/HDAC-IN-1 is a PARP-1/HDAC6 dual targeting inhibitor with IC50s of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 displays remarkable anticancer, anti-migration and anti-angiogenesis activities .
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- HY-155766
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PARP
Apoptosis
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Cancer
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PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor, with an IC50 of 0.6 ± 0.1 nM. PARP1-IN-14 exhibits antiproliferative effect against both MDA-MB-436 (BRCA1 −/−) and Capan-1 (BRCA2 −/−) cells with IC50 values below 0.3 nM .
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- HY-157212
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Apoptosis
PARP
Proteasome
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Cancer
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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 .
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- HY-164713
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Others
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Others
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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.
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- HY-148709
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PARP
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Inflammation/Immunology
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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 .
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- HY-162991
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Fluorescent Dye
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Others
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TCO-PAL-PARP is a PARP PAL probe modified with a trans-cyclooctene group, which can be utilized in live cells .
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- HY-161517
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PARP
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Cancer
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PARP1-IN-20 (compound 19A10) is a potent inhibitor of PARP1, with the IC50 of 4.62 nM and has similar low PARP-Trapping effect compared with Veliparib (HY-10129), IC50 (MDA-MB-436) >100 μM .
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- HY-161606
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PARP
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Cancer
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PARP-1/2/7-IN-1 (compound 86) is a potent inhibitor of PARP-1/2/7, with the IC50 of ＜ 10 nM .
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- HY-144338
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Epigenetic Reader Domain
PARP
Apoptosis
DNA/RNA Synthesis
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Cancer
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PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells .
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- HY-169170
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Apoptosis
DNA/RNA Synthesis
Epigenetic Reader Domain
PARP
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Cancer
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PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and PARP1 inhibitor with IC50 values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cell cycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy .
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- HY-117889
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PARP
Apoptosis
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Cancer
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PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC50=490 nM), over other PARPs (≈24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis .
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- HY-114324
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PROTACs
PARP
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Cancer
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PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
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- HY-148710
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PARP
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Inflammation/Immunology
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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 .
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- HY-114324A
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PROTACs
PARP
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Cancer
|
|
rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). ROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
|
-
- HY-153581
-
|
|
PARP
|
Others
|
|
ARTD3/PARP3-IN-1 is an unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3)/PARP3 .
|
-
- 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 .
|
-
- HY-150613
-
|
|
Epigenetic Reader Domain
PARP
Apoptosis
|
Cancer
|
|
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
|
-
- HY-161372
-
|
|
PARP
c-Met/HGFR
Apoptosis
|
Cancer
|
|
PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice .
|
-
- 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 .
|
-
- HY-161083
-
|
|
PARP
Histone Methyltransferase
|
Cancer
|
|
PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy .
|
-
- HY-158045
-
|
|
PROTACs
PARP
|
Inflammation/Immunology
Cancer
|
|
PROTAC PARP1 degrader-1 (Compound CN0) is a PROTAC degrader of PARP1. PROTAC PARP1 degrader-1 activates the cGAS/STING immunity pathway and eventually enhances T cell killing of tumor cells. PROTAC PARP1 degrader-1 inhibits DNA damage repair, resulting in highly efficient accumulation of cytosolic DNA fragments (Blue: CRBN ligand, Black: linker; Pink: PARP1 inhibitor) .
|
-
- HY-158138
-
|
|
PARP
Topoisomerase
Apoptosis
|
Cancer
|
|
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
|
-
- 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 .
|
-
- HY-D1107
-
|
|
PARP
|
Others
|
|
NCT-TFP is PARP probe used to identifying Poly(ADP-ribose) polymerases (PARP) inhibitors (extracted from patent US20190331688A1) .
|
-
- 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 .
|
-
- 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 .
|
-
- 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-132885
-
|
|
PARP
Histone Methyltransferase
|
Cancer
|
|
PARP/EZH2-IN-1 is a first-in-class dual PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM) inhibitor for triple-negative breast cancer with wild-type BRCA.
|
-
- HY-164306
-
|
|
PROTACs
PARP
|
Cancer
|
|
PROTAC PARP1 degrader-2 (Compound 72) is a PROTAC degrader for PARP with a DC50<10 nM in MDA-MB-231 cell. PROTAC PARP1 degrader-2 inhibits the cell viability of MDA-MB-436 with an IC50 <100 nM. (Blue: ligand for target protein (HY-160937); Pink: ligand for E3 ligase (HY-W998262))
|
-
- HY-141486
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
(Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP .
|
-
- 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 .
|
-
- HY-W008613A
-
|
|
Others
|
Metabolic Disease
Cancer
|
|
Amitriptyline pamoate is a common oral anticholinergic. Amitriptyline pamoate
has anticholinergic properties. Amitriptyline pamoate can be used to quantify
anticholinergic adverse reactions in patients taking amitriptyline and placebo
.
|
-
- HY-168722
-
|
|
PARP
PROTACs
|
Cancer
|
|
PROTAC PARP1 degrader-3 (Compound C6) is a PROTAC degrader for PARP1 with a DC50 of 58.14 nM. PROTAC PARP1 degrader-3 exhibits cytotoxicity in cancer cell SW-620 and LOVO with IC50 of 1.63 μM and 2.84 μM. PROTAC PARP1 degrader-3 exhibits a synergistic effect with SN-38 (HY-13704) in BRCA-mutated colon cancer cell with a combination index (CI) of 0.487. (Blue: Ligand for E3 ligase Cereblon (HY-23095); Pink: Ligand for target protein (HY-10619); Black: Linker (HY-16872))
|
-
- 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-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 .
|
-
- HY-RS10047
-
|
|
Small Interfering RNA (siRNA)
PARP
|
Others
|
|
PARP1 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PARP1 Human Pre-designed siRNA Set A
PARP1 Human Pre-designed siRNA Set A
- HY-RS10048
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Parp1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Parp1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Parp1 Mouse Pre-designed siRNA Set A
Parp1 Mouse Pre-designed siRNA Set A
- HY-RS10049
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Parp1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Parp1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Parp1 Rat Pre-designed siRNA Set A
Parp1 Rat Pre-designed siRNA Set A
- HY-RS10050
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PARP10 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP10 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PARP10 Human Pre-designed siRNA Set A
PARP10 Human Pre-designed siRNA Set A
- HY-RS10051
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Parp10 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Parp10 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Parp10 Mouse Pre-designed siRNA Set A
Parp10 Mouse Pre-designed siRNA Set A
- HY-RS10052
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Parp10 Rat Pre-designed siRNA Set A contains three designed siRNAs for Parp10 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Parp10 Rat Pre-designed siRNA Set A
Parp10 Rat Pre-designed siRNA Set A
- HY-RS10053
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PARP11 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP11 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PARP11 Human Pre-designed siRNA Set A
PARP11 Human Pre-designed siRNA Set A
- HY-RS10054
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PARP12 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP12 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PARP12 Human Pre-designed siRNA Set A
PARP12 Human Pre-designed siRNA Set A
- HY-RS10055
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PARP14 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP14 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PARP14 Human Pre-designed siRNA Set A
PARP14 Human Pre-designed siRNA Set A
- HY-RS10056
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Parp14 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Parp14 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Parp14 Mouse Pre-designed siRNA Set A
Parp14 Mouse Pre-designed siRNA Set A
- HY-RS10057
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Parp14 Rat Pre-designed siRNA Set A contains three designed siRNAs for Parp14 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Parp14 Rat Pre-designed siRNA Set A
Parp14 Rat Pre-designed siRNA Set A
- HY-RS10058
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PARP15 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP15 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PARP15 Human Pre-designed siRNA Set A
PARP15 Human Pre-designed siRNA Set A
- HY-RS10059
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PARP16 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP16 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PARP16 Human Pre-designed siRNA Set A
PARP16 Human Pre-designed siRNA Set A
- HY-RS10060
-
|
|
Small Interfering RNA (siRNA)
PARP
|
Others
|
|
PARP2 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PARP2 Human Pre-designed siRNA Set A
PARP2 Human Pre-designed siRNA Set A
- HY-RS10061
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Parp2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Parp2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Parp2 Mouse Pre-designed siRNA Set A
Parp2 Mouse Pre-designed siRNA Set A
- HY-RS10062
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Parp2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Parp2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Parp2 Rat Pre-designed siRNA Set A
Parp2 Rat Pre-designed siRNA Set A
- HY-RS10063
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PARP3 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PARP3 Human Pre-designed siRNA Set A
PARP3 Human Pre-designed siRNA Set A
- HY-RS10064
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Parp3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Parp3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Parp3 Mouse Pre-designed siRNA Set A
Parp3 Mouse Pre-designed siRNA Set A
- HY-RS10065
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Parp3 Rat Pre-designed siRNA Set A contains three designed siRNAs for Parp3 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Parp3 Rat Pre-designed siRNA Set A
Parp3 Rat Pre-designed siRNA Set A
- HY-RS10066
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PARP4 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PARP4 Human Pre-designed siRNA Set A
PARP4 Human Pre-designed siRNA Set A
- HY-RS10067
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Parp4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Parp4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Parp4 Mouse Pre-designed siRNA Set A
Parp4 Mouse Pre-designed siRNA Set A
- HY-RS10068
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Parp4 Rat Pre-designed siRNA Set A contains three designed siRNAs for Parp4 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Parp4 Rat Pre-designed siRNA Set A
Parp4 Rat Pre-designed siRNA Set A
- HY-RS10069
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PARP6 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PARP6 Human Pre-designed siRNA Set A
PARP6 Human Pre-designed siRNA Set A
- HY-RS10070
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PARP8 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP8 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PARP8 Human Pre-designed siRNA Set A
PARP8 Human Pre-designed siRNA Set A
- HY-RS10071
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PARP9 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP9 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PARP9 Human Pre-designed siRNA Set A
PARP9 Human Pre-designed siRNA Set A
- HY-158799
-
|
|
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Others
|
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 .
|
-
- HY-132167
-
|
AZD5305
|
PARP
|
Cancer
|
|
Saruparib (AZD5305) is a potent, orally active and selective PARP inhibitor and trapper with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair .
|
-
- HY-10277
-
|
SB-424323
|
Thrombin
|
Cardiovascular Disease
|
|
Odiparcil (SB-424323) is an orally active beta-d-thioxyloside analog with antithrombotic activity associated with a reduced risk of adverse bleeding events. Odiparcil (SB-424323) is indirect thrombin inhibitor that exerts its anticoagulant effect through activation of antithrombin II (heparin cofactor II) .
|
-
- HY-145427
-
|
|
DNA-PK
|
Cancer
|
|
NU5455 is a potent, selective, and orally active inhibitor of DNA-PKcs. NU5455 administration increases both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor. NU5455 enhances the activity of Doxorubicin released locally in liver tumor xenografts without inducing any adverse effect .
|
-
- HY-121719
-
|
|
PARP
|
Cardiovascular Disease
Cancer
|
|
TIQ-A is a potent TNKS (poly-ART, PARP) inhibitor, with an IC50 of 24 nM for TNKS2. TIQ-A is a potential anti-ischemic agent .
|
-
- HY-145829
-
|
|
JAK
Apoptosis
|
Inflammation/Immunology
|
|
Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis .
|
-
- HY-131009
-
|
|
PARP
|
Others
|
|
Fluorescein-NAD+ is an alternative to radiolabeled NAD and a substrate for ADP-ribosylation. Fluorescein-NAD+ can be used in PARP assays by fluorescence microscopy. Extinction Coefficient: 262 nm.
|
-
- HY-P1812
-
AUNP-12
3 Publications Verification
NP-12
|
PD-1/PD-L1
|
Cancer
|
|
AUNP-12 (NP-12) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .
|
-
- HY-160409
-
|
|
Others
Topoisomerase
|
Cancer
|
|
TopBP1-IN-1 is a TopBP1 inhibitor. TopBP1-IN-1 has a synergistic effect with PARP inhibitors. TopBP1-IN-1 has antitumor activity .
|
-
- HY-124473
-
|
Naphthafluorescein
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Naphthofluorescein inhibits the interaction between HIF-1 and Mint3.
Naphthofluorescein suppresses Mint3-dependent HIF-1 activity and glycolysis in cancer cells and macrophages without cytotoxicity in vitro and adverse effect in vivo . Naphthofluorescein is also a fluorescent pH-sensitive probe that can be used for functional Cerenkov imaging .
|
-
- HY-P1812A
-
|
NP-12 TFA
|
PD-1/PD-L1
|
Cancer
|
|
AUNP-12 TFA (NP-12 TFA) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 TFA exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .
|
-
- HY-146731
-
|
|
PPAR
|
Cardiovascular Disease
Metabolic Disease
|
|
PPARγ agonist 1 (compound 15) is a potent agonist of PPARγ. PPARγ agonist 1 shows high efficacy to activate hPPARγ without raising a full agonism and probably avoiding adverse effects. PPARγ agonist 1 has the potential for the research of cardiovascular diseases associated with metabolic disorders .
|
-
- 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-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-120115
-
|
Olaparib-bodipy FL
|
PARP
Fluorescent Dye
|
Cancer
|
|
PARPi-FL is a small molecule and fluorescent inhibitor of PARP1. PARPi-FL is a highly selective probe and can be used as an imaging agent to detect glioblastomas in vivo. (Excitation/Emission max 507/525 nm) .
|
-
- HY-150696
-
|
|
Apoptosis
Caspase
PARP
|
Cancer
|
|
Antitumor agent-72 (compound 6w) is a potent anticancer agent. Antitumor agent-72 has anticancer activity and induces apoptosis through activation of caspase-3 and cleavage of PARP. Antitumor agent-72 can be used for cancer research .
|
-
- 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 .
|
-
- HY-W424851
-
|
6,7-Dimethoxy-2-(1-piperazinyl)-4-quinazolinamine hydrochloride
|
PARP
|
Infection
Inflammation/Immunology
|
|
DPQ hydrochloride (6, 7-dimethoxy-2 -(1-piperazinyl)-4-quinazolinamine hydrochloride) is a PARP1 inhibitor, with IC50 value of 40 nM. DPQ hydrochloride has anti-inflammatory and antiviral activity. DPQ hydrochloride is used to study acute lung injury .
|
-
- HY-13540
-
|
GPI 21016
|
PARP
|
Cancer
|
|
E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent .
|
-
- HY-143407
-
|
|
FAK
|
Cancer
|
|
FAK-IN-3 (Compound 36) is a potent inhibitor of focal adhesion kinase (FAK). FAK-IN-3 not only decreases migration and invasion of PA-1 cells, but also reduces expression of MMP-2 and MMP-9. FAK-IN-3 inhibits tumor growth and metastasis, and no obvious adverse effects. FAK-IN-3 has the potential for the research of ovarian cancer .
|
-
- HY-144874
-
|
|
PARP
|
Neurological Disease
Cancer
|
|
AZ3391 is a potent inhibitor of PARP. AZ3391 is a quinoxaline derivative. PARP family of enzymes play an important role in a number of cellular processes, such as replication, recombination, chromatin remodeling, and DNA damage repair. AZ3391 has the potential for the research of diseases and conditions occurring in tissues in the central nervous system, such as the brain and spinal cord (extracted from patent WO2021260092A1, compound 23) .
|
-
- HY-P2569
-
|
|
Apoptosis
|
Cancer
|
|
Malformin A1, a cyclic pentapeptide isolated from Aspergillus niger, possess a range of bioactive properties including antibacterial activity. Malformin A1 shows potent cytotoxic activities on human colorectal cancer cells. Malformin A1 induces apoptosis by activating PARP, caspase 3, -7, and -9 .
|
-
- 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-148566
-
|
|
PARP
|
Cancer
|
|
OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. OUL232 is the most potent PARP10 inhibitor described to date (IC50=7.8 nM), as well as the first PARP12 inhibitor ever reported .
|
-
- HY-N8481
-
|
3,6-DHF
|
Apoptosis
|
Cancer
|
|
3,6-Dihydroxyflavone is an anti-cancer agent. 3,6-Dihydroxyflavone dose- and time-dependently decreases cell viability and induces apoptosis by activating caspase cascade, cleaving poly (ADP-ribose) polymerase (PARP). 3,6-Dihydroxyflavone increases intracellular oxidative stress and lipid peroxidation .
|
-
- 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 .
|
-
- 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 .
|
-
- 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 .
|
-
- 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 .
|
-
- 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 .
|
-
- 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 .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-13536
-
|
|
PARP
|
Cancer
|
|
AZD-2461 is a potent PARP inhibitor, with IC50s of 5 nM, 2 nM and 200 nM for PARP1, PARP2 and PARP3, respectively.
|
-
- HY-161431
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
RTx-152 traps Polθ on DNA and is an allosteric Polθ-pol inhibitor (IC50: 6.2 nM). RTx-152 selectively kills HR-deficient cancer cells, and suppresses PARP inhibitor resistance in multiple genetic backgrounds, including homologous recombination (HR)-proficient cells. RTx-152 selectively kills BRCA2-null cells .
|
-
- 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 .
|
-
- HY-143338
-
|
|
PARP
|
Cancer
|
|
ART-IN-1 (compound 7) is a selective PARP inhibitor with IC50s of 19, 22, 2.4, >100, 1.1 µM for PARP2, TNKS2, PARP10, PARP14, PARP15, respectively .
|
-
- 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 .
|
-
- HY-N10481
-
|
|
Apoptosis
Caspase
PARP
Bcl-2 Family
|
Cancer
|
|
Aviculin, a lignan glycoside, is a potent anticancer agent. Aviculin reduces metabolic activity on MCF-7 cells below 50%, with an IC50 of 75.47 μM. Aviculin induces breast cancer cell apoptosis through the intrinsic apoptosis pathway. Aviculin increases expression of initiator caspase-9, executioner caspase-7, and poly (ADP-ribose) polymerase (PARP). Aviculin shows an increase in the Bax/Bcl-2 ratio .
|
-
- 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-10129
-
|
ABT-888
|
PARP
Autophagy
|
Cancer
|
|
Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively .
|
-
- HY-137457
-
|
IDX-1197
|
PARP
|
Cancer
|
|
Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research .
|
-
- 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 .
|
-
- HY-15050
-
-
- HY-146817
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 µM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP .
|
-
- HY-16106
-
|
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 .
|
-
- HY-123316
-
|
Xenetix
|
Others
|
Others
|
|
Iobitridol (Xenetix) is a contrast agent with a higher incidence of adverse reactions in women than in men.
|
-
- HY-N6818
-
|
MTF
|
Apoptosis
Caspase
PARP
Endogenous Metabolite
CFTR
|
Cancer
|
|
5,7,4’-Trimethoxyflavone can be isolated from the medicinal plant Kaempferia parviflora (KP). 5,7,4’-Trimethoxyflavone is a CFTR activator and EC50 is 64 μM. 5,7,4’-Trimethoxyflavone induces apoptosis, increases proteolytic activation of caspase-3, and degradation of ADP-ribose polymerase (PARP) protein. 5,7,4’-Trimethoxyflavone has antitumor activity. 5,7,4’-Trimethoxyflavone can be used to prevent skin aging and oxidative stress .
|
-
- HY-13688
-
|
|
PARP
|
Cancer
|
|
PJ34 hydrochloride is an inhibitor of PARP1/2 with IC50 of 110 nM and 86 nM, respectively.
|
-
- 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) .
|
-
- 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 .
|
-
- HY-145804
-
|
|
PPAR
|
Neurological Disease
Cancer
|
|
AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6. AZD-9574 acts by selectively inhibiting and trapping PARP1 at the sites of SSBs. AZD-9574 is an anti-cancer agent and can be used for HRD +?breast cancer and advanced solid malignancies research .
|
-
- 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 .
|
-
- HY-150207
-
|
|
PARP
|
Inflammation/Immunology
|
|
RBN-3143 is a potent and NAD+-competitive catalytic PARP14 inhibitor with an IC50 value of 4 nM. RBN-3143 inhibits PARP14-mediated ADP-ribosylation and stabilizes PARP14 in cell lines. RBN-3143 can be used in research of lung inflammation .
|
-
- HY-W854549
-
|
Fondaparinux free acid
|
Factor Xa
|
Cardiovascular Disease
|
|
Heparin pentasaccharide (Fondaparinux) is a chemically synthesized selective factor Xa inhibitor with anticoagulant activity. Heparin pentasaccharide can be utilized in researches related to venous thromboembolic events .
|
-
- HY-12418
-
|
E7449; 2X-121
|
PARP
|
Cancer
|
|
Stenoparib (E7449) is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ∼50 and ∼50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD + as substrate.
|
-
- HY-104044
-
|
BGB-290
|
PARP
|
Cancer
|
|
Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor .
|
-
- 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 .
|
-
- HY-10162
-
Olaparib
Maximum Cited Publications
220 Publications Verification
AZD2281; KU0059436
|
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator .
|
-
- HY-17519
-
|
|
Insecticide
|
Infection
|
|
Novaluron is a chemical with insecticide properties, an insect growth regulator, and has adverse effects on mouse sperm .
|
-
- 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 .
|
-
- 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-123512
-
|
NSC39047
|
PARP
|
Cancer
|
|
OUL35 (NSC39047) is a potent and selective inhibitor of ARTD10 (PARP-10), with an IC50 of 329 nM .
|
-
- HY-12975
-
AZ6102
1 Publications Verification
|
PARP
|
Cancer
|
|
AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, respectively, and alao has 100-fold selectivity against other PARP family enzymes, with IC50s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively.
|
-
- HY-W321446
-
|
|
Fluorescent Dye
|
Others
|
|
Dansyl ethylenediamine is a fluorescent probe. Dansyl ethylenediamine can be used for synthesis of protein-imprinted polymers which is capable of specific transduction of protein binding events into fluorescent signal change .
|
-
- HY-N6818R
-
|
MTF (Standard)
|
Apoptosis
Caspase
PARP
Endogenous Metabolite
CFTR
|
Cancer
|
|
5,?7,?4'-Trimethoxyflavone (Standard) is the analytical standard of 5,?7,?4'-Trimethoxyflavone. This product is intended for research and analytical applications. 5,7,4’-Trimethoxyflavone can be isolated from the medicinal plant Kaempferia parviflora (KP). 5,7,4’-Trimethoxyflavone is a CFTR activator and EC50 is 64 μM. 5,7,4’-Trimethoxyflavone induces apoptosis, increases proteolytic activation of caspase-3, and degradation of ADP-ribose polymerase (PARP) protein. 5,7,4’-Trimethoxyflavone has antitumor activity. 5,7,4’-Trimethoxyflavone can be used to prevent skin aging and oxidative stress .
|
-
- 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 .
|
-
- HY-139678
-
|
|
Opioid Receptor
|
Others
|
|
SC13 is a novel mitragynine analog with low-efficacy Mu opioid receptor agonism that displays antinociception with attenuated adverse effects.
|
-
- HY-100225
-
|
|
PARP
|
Cancer
|
|
ME0328 is a potent and selective ARTD3/PARP3 inhibitor with an IC50 of 0.89±0.28 μM.
|
-
- 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-10162S1
-
|
AZD2281-d8; KU0059436-d8
|
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib-d8 is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
|
-
- HY-104044R
-
|
|
PARP
|
Cancer
|
|
Pamiparib (Standard) is the analytical standard of Pamiparib. This product is intended for research and analytical applications. Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor .
|
-
- HY-P4928
-
|
|
Amylin Receptor
|
Metabolic Disease
|
|
Biotinyl-Amylin (mouse, rat) is a biotinylated Amylin (mouse, rat). Amylin (mouse, rat) is a 37-aminoacid pancreatic protein that exerts control over several metabolic events such as glycemia and lacticemia .
|
-
- HY-10614
-
|
|
PARP
|
Cancer
|
|
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
|
-
- HY-132157
-
|
|
PARP
|
Others
|
|
8-Chloroquinazolin-4-ol (Compd 18) is a PARP-1 enzyme inhibitor, with an IC50 of 5.65 μM .
|
-
- HY-23399
-
|
|
Apoptosis
|
Others
|
|
Dibromoacetic acid, a haloacetic acid found in drinking water as a disinfection by-product, can cause many adverse effects, including immunotoxicity and apoptosis .
|
-
- HY-100847
-
|
|
PARP
|
Cancer
|
|
AZ0108 is an inhibitor for poly ADP-ribose polymerase (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 .
|
-
- 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 .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-P0271
-
|
|
CaMK
Autophagy
|
Neurological Disease
|
|
Syntide 2, a Ca 2+- and calmodulin (CaM)-dependent protein kinase II (CaMKII) substrate peptide, selectively inhibits the gibberellin (GA) response, leaving constitutive and abscisic acid-regulated events unaffected .
|
-
- HY-P4928A
-
|
|
Amylin Receptor
|
Metabolic Disease
|
|
Biotinyl-Amylin (mouse, rat) TFA is a biotinylated Amylin (mouse, rat). Amylin (mouse, rat) is a 37-aminoacid pancreatic protein that exerts control over several metabolic events such as glycemia and lacticemia .
|
-
- HY-10162S3
-
|
AZD2281-d4-1; KU0059436-d4-1
|
Isotope-Labeled Compounds
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib-d4-1 is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
|
-
- HY-10162R
-
|
|
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib (Standard) is the analytical standard of Olaparib. This product is intended for research and analytical applications. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator .
|
-
- HY-10130
-
|
ABT-888 dihydrochloride
|
PARP
Autophagy
|
Cancer
|
|
Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.
|
-
- 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 .
|
-
- HY-P0271A
-
|
|
CaMK
|
Neurological Disease
|
|
Syntide 2 (TFA), a Ca 2+- and calmodulin (CaM)-dependent protein kinase II (CaMKII) substrate peptide, selectively inhibits the gibberellin (GA) response, leaving constitutive and abscisic acid-regulated events unaffected .
|
-
- HY-16106S
-
|
BMN-673-13C,d4; LT-673-13C,d4
|
Isotope-Labeled Compounds
|
Others
|
|
Talazoparib- 13C,d4 is 13C and deuterated labeled Talazoparib (HY-16106). Talazoparib is an orally active PARP 1/2 inhibitor with Ki values of 1.2 nM and 0.87 nM for inhibiting PARP1 and PARP2 enzymatic activities, respectively. Has anti-tumor activity.
|
-
- HY-13990
-
|
TNKS656
|
PARP
Apoptosis
|
Cancer
|
|
NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.
|
-
- HY-111271
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
L 888607 is a potent, selective, stable and orally active CRTH2 agonist. L 888607 has high affinity for the human CRTH2 receptor with a Ki value of 4 nM. L 888607 can be used for the research of several physiological events and metabolite .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-122359
-
|
L-Centchroman; L-Ormeloxifene
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
Levormeloxifene (L-Centchroman) is a selective estrogen receptor modulator (SERM), which prevents and ameliorates postmenopausal osteoporosis. Levormeloxifene causes multiple adverse gynecological effects .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-B0589H
-
|
|
HMG-CoA Reductase (HMGCR)
Autophagy
|
Cardiovascular Disease
|
|
Strontium atorvastatin is a cholesterol-lowering drug with activity in ameliorating cardiovascular disease-related events. Strontium atorvastatin exerts its biological activity by inhibiting HMG-CoA reductase in liver tissue. Strontium atorvastatin is also used to suppress dyslipidemia .
|
-
- 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 .
|
-
- HY-N11948
-
|
|
Endogenous Metabolite
|
Others
|
|
Simmondsin, derived from the jojoba plant (Simmondsia chinensis), has been shown to decrease food intake and body weight in rats without any noticeable adverse effects.
|
-
- HY-E70128
-
|
|
Others
|
Others
|
|
Leucyl aminopeptidase is a metallopeptidase that cleave N-terminal residues from proteins and peptides. Leucyl aminopeptidase serves as transcriptional repressors to control pyrimidine, alginate and cholera toxin biosynthesis, as well as mediate site-specific recombination events in plasmids and phages .
|
-
- HY-14477
-
|
|
PARP
|
Neurological Disease
|
|
UPF-1035 is a selective PARP-2 inhibitor with an IC50 value of 0.15 μM. UPF-1035 increases CA1 pyramidal cell loss in hippocampal and has neuroprotective activity .
|
-
- HY-111329
-
|
ILS-JGB-1741
|
Sirtuin
Apoptosis
|
Cancer
|
|
JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research .
|
-
- HY-B0847
-
|
|
Fungal
Reactive Oxygen Species
|
Infection
|
|
Propiconazole is an orally active N-substituted triazole used as a fungicide. Propiconazole is a mouse liver hepatotoxicant and a hepatocarcinogen that has adverse reproductive and developmental toxicities in experimental animals .
|
-
- 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 .
|
-
- HY-136213
-
|
|
Fluorescent Dye
|
Others
|
|
Endoplasmic reticulum dye 1 is a promising live cell imaging agent for the detection of exocytotic events at the plasma membrane. Endoplasmic reticulum dye 1 shows low cytotoxicity, resistance to photobleaching , which is ideal for imaging either short- or long-time courses .
|
-
- HY-118168
-
|
Galosfen
|
Others
|
Others
|
|
A9387 is an inhibitor of the Tn3 Resolvase, which promotes site-specific recombination reactions between two directly repeated recombination sites. Several inhibitors have been isolated that inhibit this event. A9387 inhibits the binding of resolvase to the res site .
|
-
- 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 .
|
-
- HY-W294889
-
|
|
PARP
|
Cancer
|
|
OUL245 is a 7-Hydroxy derivative, and a selectively PARP2 inhibitor (IC50=44 nM). OUL245 also inhibits other PARP and TNKS enzymes with IC50s of 2.9-8.8 μM .
|
-
- 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 .
|
-
- HY-156623
-
|
|
PARP
|
Cancer
|
|
Lerzeparib is an (ADP-ribose) polymerase (PARP) inhibitor, with antineoplastic activity .
|
-
- HY-161288
-
|
|
PARP
|
Cancer
|
|
UKTT15 (compound 6) is an allosteric inhibitor of PARP1 .
|
-
- HY-B2209B
-
|
Vitamin B12a acetate
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hydroxocobalamin acetate is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the research of vitamin B12 deficiency including pernicious anemia .
|
-
- HY-148564
-
|
|
Bacterial
|
Infection
|
|
TBI-166, a riminophenazine analogue, is an orally active anti-tuberculosis agent with fewer adverse reactions than the lead riminophenazine compound, Clofazimine (HY-B1046) .
|
-
- 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 .
|
-
- HY-P99019
-
|
TEV-48125
|
CGRP Receptor
|
Neurological Disease
|
|
Fremanezumab (TEV-48125) is a humanized IgG2a monoclonal antibody that selectively and potently binds to calcitonin gene-related peptide (CGRP). CGRP is a 37-amino acid neuropeptide involved in central and peripheral pathophysiological events of migraine. Fremanezumab has the potential for chronic migraine research .
|
-
- HY-100828
-
-
- HY-Y0304
-
|
|
Biochemical Assay Reagents
|
Neurological Disease
Cancer
|
|
Dibutyl phthalate is a commonly used plasticizer commonly found in some food packaging materials, personal care products, and the coating of oral medications . May cause toxicity and adverse neurobehavioral effects .
|
-
- HY-121388
-
|
(+)-Ledol
|
Fungal
|
Infection
|
|
Ledol ((+)-Ledol) is an antifungal agent that can be isolated from the essential oil fractions of Rhododendron tomentosum. Ledol is also the expectorant and antitussive agent, which is simultaneously responsible for adverse reactions such as dizziness, nausea and vomiting .
|
-
- HY-10619B
-
|
MK-4827 tosylate
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- 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 .
|
-
- 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 .
|
-
- HY-125877
-
|
|
PROTACs
Bcl-2 Family
|
Cancer
|
|
PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM .
|
-
- HY-127040
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Talastine hydrochloride is an antihistamine with antiallergic activity. Talastine hydrochloride is used to relieve allergic symptoms. Talastine hydrochloride may cause adverse reactions such as rash, indicating differences in individual sensitivity. Talastine hydrochloride is considered a potential option for inhibiting allergic reactions .
|
-
- HY-23399R
-
|
|
Apoptosis
|
Others
|
|
Dibromoacetic acid (Standard) is the analytical standard of Dibromoacetic acid. This product is intended for research and analytical applications. Dibromoacetic acid, a haloacetic acid found in drinking water as a disinfection by-product, can cause many adverse effects, including immunotoxicity and apoptosis .
|
-
- HY-137849
-
|
|
PARP
|
Cancer
|
|
RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model .
|
-
- HY-10619
-
|
MK-4827
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-10619A
-
|
MK-4827 hydrochloride
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-10619E
-
|
MK-4827 tosylate hydrate
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-B2209
-
|
Vitamin B12a
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hydroxocobalamin (Vitamin B12a) is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia .
|
-
- HY-108631
-
|
|
PARP
|
Inflammation/Immunology
|
|
EB-47 dihydrochloride, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM. EB-47 mimics the substrate NAD +?and extends from the nicotinamide to the adenosine subsite .
|
-
- HY-15046
-
|
|
PARP
|
Cardiovascular Disease
Inflammation/Immunology
|
|
EB-47, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM. EB-47 mimics the substrate NAD + and extends from the nicotinamide to the adenosine subsite .
|
-
- 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-14406A
-
|
|
Neurokinin Receptor
|
Neurological Disease
Cancer
|
|
L-733060 hydrochloride is a potent tachykinin NK1 receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent .
|
-
- HY-B1657
-
|
|
Others
|
Neurological Disease
|
|
Fosphenytoin is a phosphate ester proagent developed as an alternative to intravenous phenytoin for acute intervention of seizures. Fosphenytoin has advantages including more convenient and rapid intravenous administration, availability for intramuscular injection, and low potential for adverse local reactions at injection sites .
|
-
- HY-14753
-
|
|
Cannabinoid Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
Rosonabant is a selective antagonist for cannabinoid receptor (CB1 receptor), which reduces body weight and improves improves the risk of obesity-related cardiovascular metabolic diseases. Rosonabant exhibits adverse side effect, such as nausea and mental disorder .
|
-
- HY-B0903R
-
