2. PROTAC Cell Cycle/DNA Damage Epigenetics
  3. PROTACs PARP
  4. PARP1 PROTAC 180055

PARP1 PROTAC 180055 (Compound 180055) is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PARP1 PROTAC 180055 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PARP1 PROTAC 180055 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells (Pink: PARP1 ligand (HY-10617A); Blue: E3 ligase VHL ligand (HY-125845); Black: linker (HY-W014787)).

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

PARP1 PROTAC 180055

PARP1 PROTAC 180055 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Customer Review

Based on 1 publication(s) in Google Scholar

PARP1 PROTAC 180055 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PARP1 PROTAC 180055

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PARP1 PROTAC 180055 (Compound 180055) is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PARP1 PROTAC 180055 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PARP1 PROTAC 180055 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells (Pink: PARP1 ligand (HY-10617A); Blue: E3 ligase VHL ligand (HY-125845); Black: linker (HY-W014787))[1].

IC50 & Target[1]

PARP1

 

In Vitro

PARP1 PROTAC 180055 (1-10 μM, 24-48 h) protects T47D and MOLT4 cells from gene toxicity-induced cell death[1].
PARP1 PROTAC 180055 (10 μM, 3-6 days) induces substantial cytotoxic effects in MOLT4 cells with BRCA1 mutation[1].

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

PARP1 PROTAC 180055 Related Antibodies

Cell Viability Assay[1]

Cell Line: Cardiomyocyte cell lines lacking BRCA1 mutations and MOLT4 cells
Concentration: 1, 5, 10 μM
Incubation Time: 144 h
Result: Showed minimal cytotoxicity in cardiomyocyte cell lines lacking BRCA1 mutations.
Induced substantial cytotoxic effects in MOLT4 cells with BRCA1 mutation.
In Vivo

PARP1 PROTAC 180055 (40 mg/kg, i.p., 16 days) shows an anti-tumor effect in BRCA1-mutated MOLT4 xenografts mice[1].

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

Animal Model: 5-week-old NSG mice (injected 8 × 106 MOLT4 cells or 4 × 106 A2780)[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection (i.p.), 16 days
Result: Exhibited a noticeable reduction in tumor size compared to the control group.
Effectively degraded PARP1 in tumors derived from MOLT4-xenografted mice.
Showed no significant alterations in neutrophil count, lymphocyte count or glutamic-pyruvic transaminase levels.
Molecular Weight

920.14

Formula

C51H62FN7O6S
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NCCC2=C(C3=CC=C(CN(C)C(CCCCCCCCC(N[C@H](C(N4C[C@H](O)C[C@H]4C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)C(C)(C)C)=O)=O)C=C3)NC7=CC(F)=CC1=C72
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (108.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0868 mL 5.4340 mL 10.8679 mL
5 mM 0.2174 mL 1.0868 mL 2.1736 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0868 mL 5.4340 mL 10.8679 mL 27.1698 mL
5 mM 0.2174 mL 1.0868 mL 2.1736 mL 5.4340 mL
10 mM 0.1087 mL 0.5434 mL 1.0868 mL 2.7170 mL
15 mM 0.0725 mL 0.3623 mL 0.7245 mL 1.8113 mL
20 mM 0.0543 mL 0.2717 mL 0.5434 mL 1.3585 mL
25 mM 0.0435 mL 0.2174 mL 0.4347 mL 1.0868 mL
30 mM 0.0362 mL 0.1811 mL 0.3623 mL 0.9057 mL
40 mM 0.0272 mL 0.1358 mL 0.2717 mL 0.6792 mL
50 mM 0.0217 mL 0.1087 mL 0.2174 mL 0.5434 mL
60 mM 0.0181 mL 0.0906 mL 0.1811 mL 0.4528 mL
80 mM 0.0136 mL 0.0679 mL 0.1358 mL 0.3396 mL
100 mM 0.0109 mL 0.0543 mL 0.1087 mL 0.2717 mL
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PARP1 PROTAC 180055 Related Classifications

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 PROTAC 180055PROTACsPARPpoly ADP ribose polymeraseMOLT4Anti-tumorT47DMDA-MB-231XenograftsOvarian and Breast cancer.Inhibitorinhibitorinhibit

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