2. Cell Cycle/DNA Damage Epigenetics Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. PARP Apoptosis Reactive Oxygen Species (ROS) DNA/RNA Synthesis STING
  4. PARP1-IN-44

PARP1-IN-44, an Olaparib (HY-10162) derivative, is an orally active PARP1 inhibitor (IC50 = 0.6 nM), and also inhibits PARP2 (IC50 = 1.0 nM) and PARP7 (IC50 = 7.5 nM). PARP1-IN-44 has selective antiproliferative activity against BRCA-deficient cancer cells with minimal toxicity to normal cells. PARP1-IN-44 induces G2/M phase arrest, promotes apoptosis, elevates ROS levels, disrupts mitochondrial membrane potential. PARP1-IN-44 suppresses PARylation while increasing γH2AX accumulation. PARP1-IN-44 activates the cGAS-STING pathway, upregulating IFN-β and CXCL10 expression. PARP1-IN-44 enhancing CD8+ T cell infiltration in a CT26 tumor mouse model, demonstrating robust in vivo antitumor efficacy.

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PARP1-IN-44

PARP1-IN-44 Chemical Structure

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PARP1-IN-44 Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

PARP1-IN-44, an Olaparib (HY-10162) derivative, is an orally active PARP1 inhibitor (IC50 = 0.6 nM), and also inhibits PARP2 (IC50 = 1.0 nM) and PARP7 (IC50 = 7.5 nM). PARP1-IN-44 has selective antiproliferative activity against BRCA-deficient cancer cells with minimal toxicity to normal cells. PARP1-IN-44 induces G2/M phase arrest, promotes apoptosis, elevates ROS levels, disrupts mitochondrial membrane potential. PARP1-IN-44 suppresses PARylation while increasing γH2AX accumulation. PARP1-IN-44 activates the cGAS-STING pathway, upregulating IFN-β and CXCL10 expression. PARP1-IN-44 enhancing CD8+ T cell infiltration in a CT26 tumor mouse model, demonstrating robust in vivo antitumor efficacy[1].

IC50 & Target[1]

PARP1

0.6 nM (IC50)

PARP2

1 nM (IC50)

PARP7

7.5 nM (IC50)

PARP3

12.5 nM (IC50)

PARP5A

20.5 nM (IC50)

PARP5B

38.1 nM (IC50)

In Vitro

PARP1-IN-44 (Compound B3) (3.63-100 μM, 5 days) has anti-proliferative activity against a panel of tumor cells, with IC50s of 9.70 μM HCT-15), 5.80 μM (HCC1937), 18.06 μM (HepG2), 16.48 μM (MCF7), and 9.88 μM (Capan-1), 12.48μM (CT26), and displays an excellent safety profile, with IC50 values greater than 100 μM against the non-cancerous NCM460 and GES-1 cell lines[1].
PARP1-IN-44 (2.5-10 μM, 48 h) induces apoptosis and cell cycle arrest in HCC1937 cells[1].
PARP1-IN-44 (2.5-10 μM, 24 h) inhibits PARP1 mediated H2O2-induced DNA damage repair in HCC1937 cells[1].
PARP1-IN-44 (2.5-10 μM, 24 h) induces ROS accumulation (detected with the DCFH-DA probe (HY-D0940)) and mitochondrial depolarization (assessed by JC-1 (HY-15534) staining) in HCC1937 cells[1].
PARP1-IN-44 (0.25-2 μM, 72 h) restores the innate immune response in CT26 cells[1].

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

PARP1-IN-44 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HCC1937 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 48 h
Result: Induced apoptosis in a concentration dependent manner, with apoptosis rates of 37.14 % and 62.64 % at concentrations of 5 μM and 10 μM.

Immunofluorescence[1]

Cell Line: H2O22 (600 μM, 30 min)-induced HCC1937 cells
Concentration: 1 μM
Incubation Time: 72 h
Result: Decreased fluorescence intensity of PAR (green) compared to the H2O2-induced group.
Increased γH2AX (green) fluorescence intensity in a concentration dependent manner.

RT-PCR[1]

Cell Line: CT26 cells
Concentration: 0.25, 0.5, 1 and 2 μM
Incubation Time: 72 h
Result: Increased in the expression of immune-related genes (IFN-β and CXCL10).
In Vivo

PARP1-IN-44 (30 and 50 mg/kg, p.o., once daily, 14 days) shows antitumor efficacy in BALB/c mice bearing CT26 tumors[1].

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

Animal Model: Six-week-old female BALB/c mice subcutaneously inoculated with CT26 cells in the axillary region[1].
Dosage: 30 mg/kg and 50 mg/kg
Administration: Oral gavage, once daily for 14 days
Result: Significantly reduced both tumor volume and weight, with the 30 mg/kg dose group exhibiting comparable tumor inhibition efficacy to RBN-2397 (HY-136174) (30 mg/kg, p.o.).
Demonstrated remarkable antitumor effects with approximately 5-fold reduction in average tumor volume and approximately 943 mg decrease in tumor weight at 50 mg/kg dose group compared to the control group.
Had no significant differences in body weight changes.
Displayed pronounced morphological changes (H&E staining): chromatin condensation, nuclear fragmentation, nuclear envelope rupture, increased and enlarged cytoplasmic vacuolation, loose cellular arrangement, and reduced intercellular connections.
Promoted the infiltration of CD8+ T cells in the tumor microenvironment.
Molecular Weight

536.55

Formula

C27H22F2N4O4S
SMILES

O=C(NC1(C2)CC2(NS(=O)(C3=CC=C(F)C=C3)=O)C1)C4=CC(CC5=NNC(C6=C5C=CC=C6)=O)=CC=C4F
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
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PARP1-IN-44 Related Classifications

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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.

Keywords:

PARP1-IN-44PARPApoptosisReactive Oxygen Species (ROS)DNA/RNA SynthesisSTINGpoly ADP ribose polymerase Stimulator of Interferon GenesTMEM173MITAERISMPYSBCPPARP1PARP7antitumorCT26HCC1937DNA damagemitochondrial membrane potentialInhibitorinhibitorinhibit

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