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Cat. No.: HY-168725

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PROTAC KSP degrader 1

PROTAC KSP degrader 1 is a KSP PROTAC degrader with a DC₅₀ of 114.8 nM. PROTAC KSP degrader 1 induces ubiquitination and degradation of KSP protein. PROTAC KSP degrader 1 induces G2/M phase arrest of the cell cycle. PROTAC KSP degrader 1 triggers Apoptosis. PROTAC KSP degrader 1 exhibits anticancer activity against colon cancer. PROTAC KSP degrader 1 can be used for the research of colon cancer, lung cancer and breast cancer.
(Pink: KSP ligand (HY-168727); Blue: Cereblon ligand (HY-103596); Black: linker (HY-168726)).

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

CAS No.: 3099825-86-9
Formula: C₄₈H₅₁N₅O₈S
Molecular Weight:858.01

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

PROTAC KSP degrader 1 Chemical Structure

CAS No.: 3099825-86-9

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC KSP degrader 1 is a KSP PROTAC degrader with a DC₅₀ of 114.8 nM. PROTAC KSP degrader 1 induces ubiquitination and degradation of KSP protein. PROTAC KSP degrader 1 induces G2/M phase arrest of the cell cycle. PROTAC KSP degrader 1 triggers Apoptosis. PROTAC KSP degrader 1 exhibits anticancer activity against colon cancer. PROTAC KSP degrader 1 can be used for the research of colon cancer, lung cancer and breast cancer^[1]. (Pink: KSP ligand (HY-168727); Blue: Cereblon ligand (HY-103596); Black: linker (HY-168726)).

IC₅₀ & Target

^[1]

KSP

114.8 nM (DC₅₀)

Cereblon

All PROTACs Isoforms :

All Kinesin Isoforms :

In Vitro

OthersAnti-cancerCell Cycle RegulationApoptosis

Others

PROTAC KSP degrader 1 (Compound 21) (30 min) inhibits basal KSP ATPase activity in cell-free biochemical assays, with an IC₅₀ of 290.20 nM^[1].

Anti-cancer

PROTAC KSP degrader 1 (50-1000 nM; 48 h) dose-dependently degrades KSP in HCT-116 cells, with a DC₅₀ of 114.8 nM and a D_max of 90%. It also time-dependently degrades KSP within 48 h, and this degradation is mediated by the ubiquitin-proteasome system^[1].
PROTAC KSP degrader 1 (72 h) potently inhibits the proliferation of HCT-116 cells with an IC₅₀ value of 10.2 nM; it also exhibits moderate antiproliferative activity against A549, MCF-7 and MDA-MB-231 cells, with corresponding IC₅₀ values of 160.5 nM, 423.9 nM and 35.4 nM^[1].

Cell Cycle Regulation

Anti-cancer

PROTAC KSP degrader 1 (10-100 nM; 24 h) induces G₂/M phase cell cycle arrest in HCT-116 cells in a dose-dependent manner in vitro. After treatment with 10 nM and 100 nM for 24 h, the proportions of cells in the G₂/M phase reach 14.79% and 75.05%, respectively^[1].

Apoptosis

Anti-cancer

PROTAC KSP degrader 1 (10-100 nM; 48 h) induces apoptosis in HCT-116 cells in a dose-dependent manner. After treatment with 10 nM and 100 nM for 48 h, the proportions of apoptotic cells are 28.47% and 55.90%, respectively^[1].

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

Western Blot Analysis^[1]

Cell Line:

human colon carcinoma HCT-116 cells
Concentration:

50-1000 nM; 200 nM; 200 nM (following 2 h pre-incubation with 1 μM MG132 or 1 μM MLN4924)
Incubation Time:

48 h; 6-48 h; 24 h
Result:

Achieved 82.1% KSP degradation at 500 nM for 48 h.
Degraded KSP in a dose-dependent manner with a DC₅₀ of 114.8 nM and a Dmax of 90% after 48 h treatment.
Degraded KSP in a time-dependent manner, with substantial degradation observed within 6 h and sustained up to 48 h at 200 nM.
Had its KSP degradation blocked by pre-treatment with proteasome inhibitor MG132 or neddylation inhibitor MLN4924.

Cell Cycle Analysis^[1]

Cell Line:

human colon carcinoma HCT-116 cells
Concentration:

10-100 nM
Incubation Time:

24 h
Result:

Increased the percentage of HCT-116 cells in the G2/M phase from 4.05% (control) to 14.79% (10 nM) and 75.05% (100 nM).

Apoptosis Analysis^[1]

Cell Line:

human colon carcinoma HCT-116 cells
Concentration:

10-100 nM
Incubation Time:

48 h
Result:

Induced apoptosis in a dose-dependent manner, with apoptotic cell percentages of 28.47% (10 nM) and 55.90% (100 nM), compared to 4.38% in the control group.

In Vivo

Anti-cancer

PROTAC KSP degrader 1 (7.5-15 mg/kg; i.p.; once every 2 days; 14 days) demonstrates potent dose-dependent antitumor efficacy in HCT-116 xenograft mice, achieving 91-98% tumor volume reduction and 97-99% tumor weight reduction with no significant body weight loss^[1].

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

Animal Model:

BALB/c nu/nu (female, 6-8 weeks old, HCT-116 cells subcutaneous implantation)^[1]
Dosage:

7.5 mg/kg; 15 mg/kg
Administration:

i.p.; once every 2 days; 14 days
Result:

Reduced tumor volume by 91% and tumor weight by 97% compared to the control group.
Reduced tumor volume by 98% and tumor weight by 99% compared to the control group.
Showed no obvious body weight loss.

Related Protocols :

Chemical Information

CAS No. 3099825-86-9
Molecular Weight 858.01
Formula C₄₈H₅₁N₅O₈S
SMILES

O=C(NCCCCCCCCNC(COC1=C2C(C(N(C3CCC(NC3=O)=O)C2=O)=O)=CC=C1)=O)[C@@H](N)CSC4(C5=CC=C(OC)C=C5)C6=CC=CC=C6C=CC7=C4C=CC=C7
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 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)
Handling Instructions (2659 KB)

References

[1]. Zhao DG, et al. Discovery of novel KSP-targeting PROTACs with potent antitumor effects in vitro and in vivo. European journal of medicinal chemistry. 2025 Jan 15;282:117052. [Content Brief]

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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.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PROTAC KSP degrader 1

All PROTACs Isoforms

All Kinesin Isoforms