PROTAC PARP1 degrader free base

PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand.

For research use only. Not for human or veterinary use.

Target PROTACs PARP Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

PROTAC PARP1 degrader structure

CAS No.: 2369022-68-2

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
5 mg	USD 1,680.00	BP-00330-5mg	In stock	Get quote
10 mg	USD 2,580.00	BP-00330-10mg	In stock	Get quote
25 mg	Inquire	BP-00330-25mg	In stock	Inquire

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Description

PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.

Biological activity

PROTAC PARP1 degrader (10 μM; 24-48 h) potently inhibits the viability of MDA-MB-231 cells, with an IC50 of 8.45 μM at 24 h and 6.12 μM at 48 h. Its potency in this cell line is 5-fold higher than that of the PARP1 inhibitors niraparib, olaparib and veliparib. PROTAC PARP1 degrader (100 μM; 48 h) shows high selectivity toward MDA-MB-231 cells; even after treatment at 100 μM for 48 h, it exhibits only extremely low or no cytotoxicity, with no PARP1 degradation, in MCF10A, BEAS-2B, HeLa and HepG2 cells

Specifications

MW (average): 1145.0950
Formula: C₅₈H₆₃Cl₂N₁₁O₁₀
CAS No.: 2369022-68-2
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃, protect from light; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : 100 mg/mL

Documents

References

[1]. Zhao Q, et al. Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule. Chem Commun (Camb). 2019 Jan 2;55(3):369-372.

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