2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. PARP1-IN-34

PARP1-IN-34 (compound 30) is a selective PARP1 inhibitor with an IC50 of 0.32 nM. PARP1-IN-34 is a subnanomolar PARP1 inhibitor with >1000-fold selectivity against PARP2 with an IC50 of 326 nM. PARP1-IN-34 shows antitumor efficacy[1].

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PARP1-IN-34 Chemical Structure

PARP1-IN-34 Chemical Structure

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PARP1-IN-34 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-34 (compound 30) is a selective PARP1 inhibitor with an IC50 of 0.32 nM. PARP1-IN-34 is a subnanomolar PARP1 inhibitor with >1000-fold selectivity against PARP2 with an IC50 of 326 nM. PARP1-IN-34 shows antitumor efficacy[1].

IC50 & Target

PARP1

0.32 nM (IC50)

PARP2

326 nM (IC50)

In Vitro

PARP1-IN-34 shows the PARP1 trapping with EC50 of 34.7, 65.9, 102.7 nM at 60, 120, 180 min, respectively[1].
PARP1-IN-34 shows very weak PARP2 trapping with an EC50 of 9882 nM[1].
PARP1-IN-34 (180min) formed a tighter PARP1-DNA trapping than AZD9574 [1].
PARP1-IN-34 (10 nM, 72 h) stimulates DNA double-stands breaks in MDA-MB-436 cells. PARP1-IN-34 (10 nM, 72 h) could increase the levels of γH2AX in MDA-MB-436 cells and causes more significant DNA damage in cells than AZD9574[1].
PARP1-IN-34 displays neglectable antiproliferation activities in these BRCA WT cells (CAL-148, 22RV1, and PC3 cell) and 293T normal cells (IC50 > 10,000 nM), in contrast to IC50 = 2.6 nM in BRCA-mutated MDA-MB-436 cells, which indicates that its cellular activity is PARP1inhibition-dependent[1].
PARP1-IN-34 is a highly selective PARP1inhibitor over other PARPs, including PARP2, PARP3, PARP5A, PARP5B, PARP6, PARP7, PARP12, PARP14, and PARP15[1].

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

PARP1-IN-34 Related Antibodies

Western Blot Analysis

Cell Line: MDA-MB-436 cells
Concentration: 10 nM
Incubation Time: 72 h
Result: Increased the levels of γH2AX at 10 nM in MDA-MB-436 cells and causes more significant DNA damage in cells than AZD9574
In Vivo

PARP1-IN-34 (0.2-0.6 mg/kg, p.o., daily, 35 days) induces tumor shrinkage in a dose-dependent manner in the MDA-MB-436 mouse xenograft model[1].
PARP1-IN-34 (10 mg/kg, p.o., daily, 35 days) has synergy with Carboplatin(HY-17393) in the SUM149PT xenograft model[1].
PARP1-IN-34 (5, 25 mg/kg, p.o., daily, 14 days) has minimal impact on RET(reduction of the reticulocyte) [1].
Pharmacokinetics of PARP1-IN-34 in the Mouse, Rat, and Dog.

Therapeutic Index of PARP1-IN-34 Compared with Other PARP Inhibitors.
property mouse rat dog
plasma protein unbound fraction 0.012 0.067 0.022
t1/2 (h) 3.2 5.1 9.2
V ss(L/kg) 0.34 1.42 0.36
CLp(mL/min/kg) 2.0 4.9 0.58
AUC(0-t)(ng・h r/mL) po 45688 13622 15024
F(%) 132.4 93.1 67.3

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

Compound Olaparib AZD5305 AZD9574 PARP1-IN-34
Potency PARP1 IC50(nM)
PARP2 IC50(nM)
PARP 1/2 fold selectivity		 0.95
0.34
0.39
 0.46
10
22		 0.87
672
772
 0.32
326
1019
In vivo efficacy in MDA-MB-436 Dose of tumor regression ≥50%
AUC (ng/ml hr)
Unbound % in mice
Free - drug AUC (ng/ml hr)		 100 mg/kg
31426
29.3%
9208		 0.1 mg/kg
4043
2%
81		 2 mg/kg
9776
4%
391		 0.6 mg/kg
1039
1.2%
12.5
Hematox in rat Dose of RET > 50%↓
AUC (ng/ml hr)
Unbound % in rat
Free - drug AUC (ng/ml hr)		 <100 mg/kg
55803
26.6%
14844		 < 1 mg/kg
7505
2%
150.1		 >100 mg/kg
308365
9.7%
29911		 > 25 mg/kg
133541
6.7%
8947
Therapeutic index Fold of Free - drug AUC <1.61 < 1.71 >76.5 >715
Animal Model: Female Balb/c athymic nude mice (Vital River) (6-8 weeks) were subcutaneously implanted with 1 × 107 MDA-MB-436 cells in 0.2 mL Matrigel solution in the right flank[1] .
Dosage: 0.2, 0.6 mg/kg
Administration: p.o., daily, 35 days
Result: At 0.6 mg/kg QD induced tumor shrinkage by 65.7%, which was stronger than the efficacy of AZD9574 at 0.6 mg/kg QD (38.1% shrinkage) and that of AZD5305 at 0.03 mg/kg QD (24.4% shrinkage).
Induced minimal changes in animal body weight.
Animal Model: Female Balb/c athymic nude mice (Vital River) (6−8 weeks) were subcutaneously implanted with 1 × 107 SUM149PT cells in 0.2 mL Matrigel solution in the right flank.[1] .
Dosage: 10 mg/kg
Administration: p.o., daily, 35 days
Result: In combination with weekly 37.5 mg/kg carboplatin demonstrated great improvement of the antitumor effect compared to carboplatin monotherapy (94.7% TGI vs 69.7% TGI).
Induced no significant body weight loss during the study.
Animal Model: Female Balb/c athymic nude mice (Vital River) (6−8 weeks) were subcutaneously implanted with 1 × 107 SUM149PT cells in 0.2 mL Matrigel solution in the right flank.[1] .
Dosage: 5, 25 mg/kg
Administration: p.o., daily, 14days
Result: Had minimal impact on RET(reduction of the reticulocyte).
Induced no significant body weight loss during the study.
Molecular Weight

433.51

Formula

C23H27N7O2
SMILES

O=C(N1)[C@H](N2N=CC3=CC(CN4CCN(C(C=CC(C(NC)=O)=N5)=C5C)CC4)=CC1=C23)C
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-34 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-34PARPpoly ADP ribose polymerasecancerhematologicalDNA damageInhibitorinhibitorinhibit

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