製品番号: HY-139156

SK-575

5 Cited Publications

カスタマーレビュー

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).

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.86%
CAS 番号: 2523016-96-6
分子式: C₄₇H₅₃FN₈O₈
分子量:876.97

保管条件:

-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 構造式

CAS 番号: 2523016-96-6

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (5)
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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)

PROTACs アイソフォーム固有の製品をすべて表示 :

PARP アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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.

体内実験

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

化学情報

CAS 番号 2523016-96-6
性状 Solid
分子量 876.97
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-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

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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.

溶剤 & 溶解度

体外:

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

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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

MedChemExpress（MCE）の使用を引用している文献 SK-575

PROTACs アイソフォーム固有の製品をすべて表示

PARP アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (5)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

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

MedChemExpress（MCE）の使用を引用している文献 SK-575

PROTACs アイソフォーム固有の製品をすべて表示

PARP アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (5)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

SK-575 関連分類

HY-139156 関連分類