1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. PARP Apoptosis Caspase
  3. YCH3971

YCH3971 is a PARP1 inhibitor with a PARP1 IC50 of 7.52 nM and a PARP1 EC50 of 67.75 nM. YCH3971 inhibits the proliferation of BRCA-deficient tumor cells. YCH3971 induces DNA damage, G2/M phase arrest, and caspase-mediated Apoptosis in triple-negative breast cancer cells. YCH3971 can be used for the research of BRCA-deficient tumors.

For research use only. We do not sell to patients.

YCH3971

YCH3971 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

YCH3971 is a PARP1 inhibitor with a PARP1 IC50 of 7.52 nM and a PARP1 EC50 of 67.75 nM. YCH3971 inhibits the proliferation of BRCA-deficient tumor cells. YCH3971 induces DNA damage, G2/M phase arrest, and caspase-mediated Apoptosis in triple-negative breast cancer cells. YCH3971 can be used for the research of BRCA-deficient tumors[1].

IC50 & Target

PARP-1

7.52 nM (IC50)

PARP-1

67.75 nM (EC50)

In Vitro

YCH3971 (0.01-10000 nM, 7 days) potently inhibits the proliferation of BRCA1-deficient MDA-MB-436 cells, with an IC50 of 2.10 nM[1].
YCH3971 (0.01-10000 nM, 7 days) inhibits the proliferation of BRCA2-deficient V-C8 cells with an IC50 of 69.61 nM, while it exhibits only extremely weak activity against BRCA2-proficient V79 cells[1].
YCH3971 (0.01-10000 nM, 7 days) inhibits the proliferation of BRCA1-mutant UWB1.289 ovarian cancer cells with an IC50 of 112.86 nM, whereas it shows almost no activity against UWB1.289 + BRCA1 cells with restored BRCA1 expression[1].
YCH3971 (0.01-1 μM; 48 h) induces dose-dependent DNA damage in MDA-MB-436 cells[1].
YCH3971 (0.01-1 μM; 3 days) induces dose-dependent G2/M phase arrest in MDA-MB-436 cells[1].
YCH3971 (0.01-1 μM; 4 days) induces dose-dependent caspase-mediated apoptosis in MDA-MB-436 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Immunofluorescence[1]

Cell Line: MDA-MB-436 cells
Concentration: 0, 0.01, 0.1, 1 μM
Incubation Time: 48 h
Result: Induced dose-dependent DNA damage.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 0, 0.01, 0.1, 1 μM
Incubation Time: 3 days
Result: Led to a dose-dependent accumulation of cells in the G2/M phase.
At concentrations ≥0.1 μM, caused a statistically significant increase in G2/M phase cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 0, 0.01, 0.1, 1 μM
Incubation Time: 4 days
Result: Led to a dose-dependent increase in Annexin V+/PI+ apoptotic cells.
At 1 μM, induced a slightly higher level of apoptosis.
Confirmed dose-dependent cleavage of caspases-3, -7, and -8 via western blotting.
At 1 μM, induced slightly stronger caspase activation.

Western Blot Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 0, 0.01, 0.1, 1 μM
Incubation Time: 48 h
Result: Activated DNA damage response markers, including phosphorylated CHK1 (p-CHK1), phosphorylated RPA32 (p-RPA32), and γH2AX.
Parmacokinetics
Species Dose Route AUC0-last T1/2 CL Vss_obs Cmax Tmax Bioavailability
Rat[1] 1 mg/kg i.v. 837 ng·h/mL 12.6 h 19.8 mL/min/kg 1727 L/kg / / /
Rat[1] 3 mg/kg p.o. 30.8 2.59 h / / 16.9 ng/mL 0.83 h 1.22 %
Molecular Weight

387.48

Formula

C23H25N5O

SMILES

CC1=C(N2CCN(CC3=CN4C(C=C(C5CC5)C(N4)=O)=C3)CC2)C=CC(C#N)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
YCH3971
Cat. No.:
HY-181664
Quantity:
MCE Japan Authorized Agent: