Referencia número: HY-139156

SK-575

5 Cited Publications

Revisión del cliente

Based on 5 publication(s) in Google Scholar

SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC₅₀ of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations.
(Pink: PARP1 ligand (HY-75706); Blue: Cereblon ligand (HY-41547); Black: linker).

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.86%
No. CAS: 2523016-96-6
Fòrmula: C₄₇H₅₃FN₈O₈
Peso molecular:876.97

Almacenamiento:

-20°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

SK-575 Chemical Structure

No. CAS: 2523016-96-6

Tamaño

Precio

Stock

Cantidad

Amount: USD 0.00

* Seleccione Cantidad antes de agregar artículos.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC₅₀ of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations^[1]. (Pink: PARP1 ligand (HY-75706); Blue: Cereblon ligand (HY-41547); Black: linker).

IC₅₀ & Target

PARP1

2.30 nM (IC₅₀)

Ver todos los productos específicos de isoformas PROTACs :

Ver todos los productos específicos de isoformas PARP :

Cellular Effect

Cell Line	Type	Value	Description	References
CAPAN-1	IC₅₀	0.056 μM Compound: 18; SK-575	Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 13 days by by CCK-8 assay Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 13 days by by CCK-8 assay	[PMID: 32924477]
MDA-MB-436	IC₅₀	0.019 μM Compound: 18; SK-575	Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 7 days by CCK-8 assay Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 7 days by CCK-8 assay	[PMID: 32924477]

In Vitro

SK-575 inhibits cell growth in MDA-MB-436 and Capan-1 cells, with IC₅₀ values of 19 ± 6 nM and 56 ± 12 nM, respectively^[1].
SK-575 (0-1 μM, 24 h) shows good PARP1 degradation activity in cancer cell lines (MDA-MB-436, Capan-1, and SW620 cells)^[1].
SK-575 (0-10 μM, 24 h) effectively induces the formation of γH2AX in MDA-MB-436 and Capan-1 cells in a dose dependent manner^[1].

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

Western Blot AnalysisM^[1]

Cell Line:

MDA-MB-436, Capan-1, and SW620 cells
Concentration:

10000, 1000, 300, 100, 30, 10, 3, 1, 0.3, 0.1, 0.03, and 0.01 nM
Incubation Time:

24 h
Result:

Showed good PARP1 degradation activity in these cancer cell lines (MDA-MB-436, Capan-1, and SW620 cells), with DC₅₀ values of 1.26, 6.72 and 0.509 nM, respectively. Effectively induced the formation of γH2AX in MDA-MB-436 and Capan-1 cells in a dose dependent manner.

In Vivo

SK-575 (mice bearing BRCA2-mutated Capan-1 xenografts, 25 and 50 mg/kg, IP, once daily for 5 days) significantly inhibits the tumor growth in vivo as a single-agent in HR-deficient xenograft models^[1].
SK-575 (25 mg/kg, IP, once) achieves sufficient exposure in plasma for over 24 h and effectively induces PARP1 degradation in the SW620 xenograft tumor tissue with the effect persisting for >24 h^[1].

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

Animal Model:

Male BALB/c nude mice (bearing xenograft Capan-1 tumors)^[1]
Dosage:

25 mg/kg, 50 mg/kg
Administration:

IP, once daily for 5 consecutive days
Result:

Inhibited tumor growth. SK-575 at these doses (25 and 50 mg/kg) were well tolerated, with no mice lethality or significant weight loss observed during the treatment time.

Animal Model:

Female ICR mice (20-23 g, 6-7 week-old, n=3 per group)^[1]
Dosage:

25 mg/kg
Administration:

Intraperitoneally, a single dose (Pharmacokinetic Analysis)
Result:

Pharmacokinetic Parameters of SK-575 in female ICR mice^[1].

Parameters mean

T_max (h) 0.25

C_max (ng/mL) 1843

AUC_all (ng/mL∗h) 5316

AUC_inf (ng/mL∗h) 5363

t_1/2 (ng/mL) 3.08

Chemical Information

No. CAS 2523016-96-6
Appearance Solid
Peso molecular 876.97
Fòrmula C₄₇H₅₃FN₈O₈
Color Light yellow to yellow
SMILES

O=C(NCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCCCCCCCCC(N4CCN(C(C5=CC(CC6=NNC(C7=C6C=CC=C7)=O)=CC=C5F)=O)CC4)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

-20°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Publications (5)

All Bio/Physico-chemical AssayIPWBIFCell Migration/Invasion Assay

Sort by:

Journal Impact Factor

Nat Chem Biol

High-throughput ligand diversification to discover chemical inducers of proximity. [Abstract]

2026 Feb 16. PMID: 41699285

SK-575 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2026 Feb 16. [Abstract]

Structure of PARP1/2 inhibitor scaffolds functionalized with the spirosuccinimide building block, PARP1 intracellular target engagement in MV4;11-PARP1-HiBiT cells after 4 h treatment (HiBiT luminescence signal normalized to DMSO, mean of 3 biological replicates ± S.E.M.), and HiBiT degradation assay in MV4;11-PARP1-HiBiT cells after 16 h treatment (HiBiT luminescence signal normalized to DMSO, mean of 4 biological replicates ± S.E.M.). Compounds are compared to SK-575 (2.5 μM, 4 h), a known PARP1 PROTAC degrader, or rucaparib and olaparib, which are known PARP1 ligands.
Nat Chem Biol

Stabilization of AFF1 by PARylation ensures transcriptional restart after DNA damage. [Abstract]

2025 Oct 8. PMID: 41062835

SK-575 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 Oct 8. [Abstract]

Blocking PARP1 with degrading it using PROTAC SK575 (500 nM, 6 h) abrogated AFF1 PARylation
J Control Release

A dual PROTAC nanocarrier amplifies DNA damage and STING activation for cancer immunotherapy. [Abstract]

2025 Oct 2;388(Pt 1):114290. PMID: 41045969

SK-575 purchased from MedChemExpress. Usage Cited in: J Control Release. 2025 Oct 2;388(Pt 1):114290. [Abstract]

SK-575 efficiently degraded PARP1 at a low concentration of 0.625 μM, accompanied by a significant upregulation of γH2AX, a well-established marker of DNA double-strand breaks.

SK-575 purchased from MedChemExpress. Usage Cited in: J Control Release. 2025 Oct 2;388(Pt 1):114290. [Abstract]

IC₅₀ values for different SK-575 to dBET1 ratios.

SK-575 purchased from MedChemExpress. Usage Cited in: J Control Release. 2025 Oct 2;388(Pt 1):114290. [Abstract]

The combination index (CI) in 4T1 cells treated with various ratios of SK-575 to dBET1.

SK-575 purchased from MedChemExpress. Usage Cited in: J Control Release. 2025 Oct 2;388(Pt 1):114290. [Abstract]

Immunofluorescence staining of γH2AX in 4T1 cells after treatment with various ratios of SK-575 (9.1 μg/mL) to dBET1; scale bar: 20 μm.

SK-575 purchased from MedChemExpress. Usage Cited in: J Control Release. 2025 Oct 2;388(Pt 1):114290. [Abstract]

Images of clone formation in 4T1 cells after treatment with SK-575 (9.1 μg/mL), dBET1, and SK-575 + dBET1.
bioRxiv

2026 Jan 13.
bioRxiv

2025 Jun 19.

Solvente y solubilidad

In Vitro:

DMSO : 80 mg/mL (91.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1403 mL

5.7014 mL

11.4029 mL

5 mM

0.2281 mL

1.1403 mL

2.2806 mL

10 mM

0.1140 mL

0.5701 mL

1.1403 mL

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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (274 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Cao C, et al. Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers. J Med Chem. 2020 Oct 8;63(19):11012-11033. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1403 mL	5.7014 mL	11.4029 mL	28.5072 mL
	5 mM	0.2281 mL	1.1403 mL	2.2806 mL	5.7014 mL
	10 mM	0.1140 mL	0.5701 mL	1.1403 mL	2.8507 mL
	15 mM	0.0760 mL	0.3801 mL	0.7602 mL	1.9005 mL
	20 mM	0.0570 mL	0.2851 mL	0.5701 mL	1.4254 mL
	25 mM	0.0456 mL	0.2281 mL	0.4561 mL	1.1403 mL
	30 mM	0.0380 mL	0.1900 mL	0.3801 mL	0.9502 mL
	40 mM	0.0285 mL	0.1425 mL	0.2851 mL	0.7127 mL
	50 mM	0.0228 mL	0.1140 mL	0.2281 mL	0.5701 mL
	60 mM	0.0190 mL	0.0950 mL	0.1900 mL	0.4751 mL
	80 mM	0.0143 mL	0.0713 mL	0.1425 mL	0.3563 mL

Keywords

SK-575

5 Cited Publications

100 mg Obtener un presupuesto

Subscribe to the

MedChemExpress

Newsletter

Nombre del producto:
Referencia número:
Cantidad:
MCE Japan Authorized Agent:

Nombre del producto:
No. CAS:
Species:
Pureza:
Cantidad:

SK-575

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Cancer Stem Cells Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) SK-575

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas PARP

Actividad biológica

Chemical Information

Publications (5)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Parameters	mean
T_max (h)	0.25
C_max (ng/mL)	1843
AUC_all (ng/mL∗h)	5316
AUC_inf (ng/mL∗h)	5363
t_1/2 (ng/mL)	3.08

SK-575

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Cancer Stem Cells Compound Library

PROTAC Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) SK-575

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas PARP

Actividad biológica

Chemical Information

Publications (5)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

SK-575 Related Classifications

HY-139156 Related Classifications