Date published: 2026-5-1

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CP 100356 hydrochloride (CAS 142716-85-6)

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Alternate Names:
4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-N-(3,4-dimethoxyphenethyl)-6,7-dimethoxyquinazolin-2-amine
Application:
CP 100356 hydrochloride is a high affinity Mdr-1 inhibitor
CAS Number:
142716-85-6
Purity:
≥98%
Molecular Weight:
597.1
Molecular Formula:
C31H36N4O6•HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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CP 100356 hydrochloride has been reported to be a high affinity multi-drug resistance protein (Mdr-1/P-gp) inhibitor. This compound binds to the active site of Mdr-1 and inhibits the efflux of active compounds, enhancing their effectiveness by allowing them to remain in the cytoplasm. It is selective for P-gp over multidrug resistance-associated protein 2 (MRP2) at 15 µM, as well as the cytochrome P450 (CYP) isoforms CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 (IC50s = >50 µM for all) and organic anion transporter 1B1 (OATP1B1; IC50 = ~66 µM), but does inhibit breast cancer resistance protein (BCRP; IC50 = 1.5 µM).


CP 100356 hydrochloride (CAS 142716-85-6) References

  1. Preclinical pharmacokinetics and metabolism of 6-(4-(2,5-difluorophenyl)oxazol-5-yl)-3-isopropyl-[1,2,4]-triazolo[4,3-a]pyridine, a novel and selective p38alpha inhibitor: identification of an active metabolite in preclinical species and human liver microsomes.  |  Kalgutkar, AS., et al. 2006. Biopharm Drug Dispos. 27: 371-86. PMID: 16944451
  2. Calcium and P-glycoprotein independent synergism between schweinfurthins and verapamil.  |  Sheehy, RM., et al. 2015. Cancer Biol Ther. 16: 1259-68. PMID: 26046259
  3. Fgd5 is a Rac1-specific Rho GEF that is selectively inhibited by aurintricarboxylic acid.  |  Park, S., et al. 2021. Small GTPases. 12: 147-160. PMID: 31601145
  4. Potent, Novel SARS-CoV-2 PLpro Inhibitors Block Viral Replication in Monkey and Human Cell Cultures.  |  Shen, Z., et al. 2021. bioRxiv.. PMID: 33594371
  5. Improved SARS-CoV-2 Mpro inhibitors based on feline antiviral drug GC376: Structural enhancements, increased solubility, and micellar studies.  |  Vuong, W., et al. 2021. Eur J Med Chem. 222: 113584. PMID: 34118724
  6. Rational Design of Hybrid SARS-CoV-2 Main Protease Inhibitors Guided by the Superimposed Cocrystal Structures with the Peptidomimetic Inhibitors GC-376, Telaprevir, and Boceprevir.  |  Xia, Z., et al. 2021. ACS Pharmacol Transl Sci. 4: 1408-1421. PMID: 34414360
  7. CP100356 Hydrochloride, a P-Glycoprotein Inhibitor, Inhibits Lassa Virus Entry: Implication of a Candidate Pan-Mammarenavirus Entry Inhibitor.  |  Takenaga, T., et al. 2021. Viruses. 13: PMID: 34578344
  8. Discovery of SARS-CoV-2 main protease covalent inhibitors from a DNA-encoded library selection.  |  Ge, R., et al. 2022. SLAS Discov. 27: 79-85. PMID: 35063690
  9. Covalent narlaprevir- and boceprevir-derived hybrid inhibitors of SARS-CoV-2 main protease: room-temperature X-ray and neutron crystallography, binding thermodynamics, and antiviral activity.  |  Kneller, D., et al. 2022. Res Sq.. PMID: 35169792
  10. Natural Compounds Inhibit SARS-CoV-2 nsp13 Unwinding and ATPase Enzyme Activities.  |  Corona, A., et al. 2022. ACS Pharmacol Transl Sci. 5: 226-239. PMID: 35434533
  11. Covalent narlaprevir- and boceprevir-derived hybrid inhibitors of SARS-CoV-2 main protease.  |  Kneller, DW., et al. 2022. Nat Commun. 13: 2268. PMID: 35477935
  12. Fluorescence-Based Activity Screening Assay Reveals Small Molecule Inhibitors of Vaccinia Virus mRNA Decapping Enzyme D9.  |  Bednarczyk, M., et al. 2022. ACS Chem Biol. 17: 1460-1471. PMID: 35576528
  13. Proscillaridin A Sensitizes Human Colon Cancer Cells to TRAIL-Induced Cell Death.  |  Semba, M., et al. 2022. Int J Mol Sci. 23: PMID: 35805980
  14. Efficacy of Licensed Monoclonal Antibodies and Antiviral Agents against the SARS-CoV-2 Omicron Sublineages BA.1 and BA.2.  |  Fiaschi, L., et al. 2022. Viruses. 14: PMID: 35891355

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

CP 100356 hydrochloride, 10 mg

sc-361154
10 mg
$377.00

CP 100356 hydrochloride, 50 mg

sc-361154A
50 mg
$1122.00