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PARP1-IN-50 is a selective, orally active PARP-1 inhibitor with an IC50 of 64.98 nM. It inhibits PAR formation and induces DNA double-strand breaks, resulting in DNA damage. PARP1-IN-50 can cause G2/M phase arrest and apoptosis (apoptosis) in cancer cells, demonstrating significant antiproliferative activity against various cancer cell lines. This compound is useful in cancer research, including studies on breast cancer.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | PARP1-IN-50 is a selective, orally active PARP-1 inhibitor with an IC50 of 64.98 nM. It inhibits PAR formation and induces DNA double-strand breaks, resulting in DNA damage. PARP1-IN-50 can cause G2/M phase arrest and apoptosis (apoptosis) in cancer cells, demonstrating significant antiproliferative activity against various cancer cell lines. This compound is useful in cancer research, including studies on breast cancer. |
| Targets&IC50 | PARP1:64.98 nM |
| In vitro | PARP1-IN-50 (Compound 13) demonstrates significant antiproliferative activity in HCC-1937, Capan-1, MCF-7, and PANC-1 cells, with IC50 values of 0.88, 0.56, 4.49, and 1.53 μM, respectively. In HCC-1937 cells, PARP1-IN-50 (1-10 μM, 48 h) induces G2/M phase arrest and decreases the expression levels of CDK1 and cyclin B. Additionally, PARP1-IN-50 (1-10 μM, 4 h) inhibits H2O2-induced PAR formation in HCC-1937 cells. It also enhances PARP-1-DNA trapping and induces DNA double-strand breaks within 30 minutes at concentrations of 1-10 μM. Furthermore, treatment with PARP1-IN-50 (1-10 μM, 48 h) results in apoptosis in HCC-1937 cells. |
| In vivo | PARP1-IN-50 (Compound 13), administered orally at a dose of 25-50 mg/kg once daily for 21 days, significantly inhibits the growth of HCC-1937 xenograft tumors in BALB/c nude mice and demonstrates favorable safety characteristics. |
| Molecular Weight | 662.42 |
| Formula | C22H26Br2N6O4S2 |
| Cas No. | 2255341-36-5 |
| Smiles | S=C(N)NN=CC1=CC(Br)=C(OCCCCOC2=C(Br)C=C(C=NNC(=S)N)C=C2OC)C(OC)=C1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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