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CAPAN-1

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-155993
    YCH1899

    		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].
    YCH1899
  • HY-101570
    Nedisertib
    20+ Cited Publications

    Peposertib; M3814

    		 DNA-PK BCRP Cancer
    Nedisertib (Peposertib) is an orally active selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of less than 3 nM. Nedisertib also acts as a modulator of ABCG2, capable of reversing ABCG2-mediated multidrug resistance (MDR), thus providing new strategies for combination therapy. By inhibiting DNA double-strand break repair, Nedisertib can enhance the efficacy of chemotherapy and radiotherapy. Nedisertib exhibits antitumor activity [1] .
    Nedisertib
  • HY-155766
    PARP1-IN-14

    		PARP Apoptosis Cancer
    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 [1].
    PARP1-IN-14
  • HY-163817
    PARP1/2-IN-3

    		PARP Cancer
    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 [1].
    PARP1/2-IN-3
  • HY-14687
    (rac)-Talazoparib

    (rac)-BMN-673; (rac)-LT-673

    		 PARP Cancer
    (rac)-Talazoparib ((rac)-BMN-673) (Compound 47) is the orally active inhibitor for PARP1/2 with Ki of 1.2 nM and 0.87 nM. (rac)-Talazoparib inhibits cellular PARylation with an EC50 of 2.51 nM. (rac)-Talazoparib causes the accumulation of DNA damage, inhibits proliferation of BRCA1/2-mutated MX-1 cell and Capan-1 cell with IC50 of 0.3 nM and 5 nM. (rac)-Talazoparib exhibits antitumor efficacy in mouse models [1].
    (rac)-Talazoparib
  • HY-161934
    PARP1-IN-27

    		PARP Reactive Oxygen Species (ROS) Apoptosis Cancer
    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 [1].
    PARP1-IN-27
  • HY-147101
    SK-575-NEG

    		PARP Cancer
    SK-575-NEG (compound 28), a methylation counterpart of SK-575, is synthesized by methylation of the amino group of piperidine-2,6-dione in SK-575 as an control compound. SK-575-NEG is strongly bound to PARP1, with an IC50 of 2.64 nM. SK-575-NEG was completely ineffective in inducing PARP1 degradation in MDA-MB-436 and Capan-1 cells at concentrations up to 1 μM [1].
    SK-575-NEG
  • HY-163715
    Antitumor agent-165

    		FAK Cancer
    Antitumor agent-165 (Compound 10l) is a potent focal adhesion kinase (FAK) inhibitor. Antitumor agent-165 exhibits effective antiproliferative activity against CAPAN-1, PANC-1, PATU-T, SUIT-2, BxPC-3, PDAC-3 and PANC-1 GR with IC50s in the range of 1.04-3.44 μM [1].
    Antitumor agent-165
  • HY-168721
    Tubulin inhibitor 48

    		Microtubule/Tubulin Cancer
    Tubulin inhibitor 48 (compound 16) is an anti-cancer agent targeting tubulin. Tubulin inhibitor 48 has an IC50 of 0.1 and 0.07 μM for LN-229 and Capan-1 cell, respectively [1].
    Tubulin inhibitor 48
  • HY-150765
    PARP1-IN-12

    		PARP Apoptosis Cancer
    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 [1].
    PARP1-IN-12
  • HY-139156
    SK-575

    		PROTACs PARP Cancer
    SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations [1].
    SK-575
  • HY-10617AR
    Rucaparib (Standard)

    AG014699 (Standard); PF-01367338 (Standard)

    		 Reference Standards PARP Cancer
    Rucaparib (Standard) is the analytical standard of Rucaparib. This product is intended for research and analytical applications. 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] .
    Rucaparib (Standard)
  • HY-115552
    Simmiparib

    		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].
    Simmiparib
  • HY-10617R
    Rucaparib phosphate (Standard)

    AG-014699 phosphate (Standard); PF-01367338 phosphate (Standard)

    		 Reference Standards PARP Cancer
    Rucaparib (phosphate) (Standard) is the analytical standard of Rucaparib (phosphate). This product is intended for research and analytical applications. 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] .
    Rucaparib phosphate (Standard)
  • HY-108436
    Deltazinone 1

    		Phosphodiesterase (PDE) Cancer
    Deltazinone 1, a pyrazolopyridazinone, is a highly selective PDEδ inhibitor with a KD of 8 nM. Deltazinone 1 inhibits the PDEδ-Ras interaction. Deltazinone 1 shows a dose-dependent inhibitory response on proliferation in oncogenic KRas-dependent cell lines [1] .
    Deltazinone 1
  • HY-10617
    Rucaparib phosphate
    40+ Cited Publications

    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] .
    Rucaparib phosphate
  • HY-10617A
    Rucaparib
    Maximum Cited Publications
    44 Publications Verification

    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] .
    Rucaparib
  • HY-102003A
    Rucaparib camsylate

    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] .
    Rucaparib camsylate
  • HY-102003
    Rucaparib monocamsylate
    35+ Cited Publications

    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] .
    Rucaparib monocamsylate
  • HY-151372
    Protein kinase D inhibitor 1

    		PKD Cancer
    Protein kinase D inhibitor 1 (compound 17m) is a pan-PKD inhibitor, with IC50 values ranging from 17 to 35 nM. Protein kinase D inhibitor 1 inhibits PKD-dependent cortactin phosphorylation [1].
    Protein kinase D inhibitor 1
  • HY-159480
    AD1058

    		Src ATM/ATR Apoptosis mTOR AMPK Cancer
    AD1058 is an orally active, selective, and BBB-permeable inhibitor of ATR (IC50: 1.6 nM). AD1058 exhibits anticancer activity by inhibiting tumor cell proliferation, inducing cell cycle arrest, and promoting apoptosis. AD1058 is suitable for research on advanced malignancies and brain metastases [1].
    AD1058

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