2. Cell Cycle/DNA Damage Epigenetics Apoptosis Cytoskeleton
  3. Topoisomerase HDAC Apoptosis Kinesin RAD51
  4. SeSA-HCPT

SeSA-HCPT is an orally active dual-target inhibitor integrating Topo I and HDAC inhibition. SeSA-HCPT induces potent DNA damage, apoptosis, S-phase arrest in prostate cancer cells. SeSA-HCPT inhibits cancer cells proliferation and migration. SeSA-HCPT impairs homologous recombination by suppressing KIF4A-RAD51 signaling. SeSA-HCPT markedly inhibits CRPC tumor growth with minimal systemic toxicity.

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SeSA-HCPT

SeSA-HCPT Chemical Structure

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SeSA-HCPT Related Antibodies

Top Publications Citing Use of Products

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Topoisomerase Topo I Topo II DNA gyrase

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

View All Kinesin Isoform Specific Products:

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Kinesin-5/Eg5/KSP Kinesin-6 Kinesin-7/CENP-E Kinesin-12 Kinesin-14 Kinesin-13

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Description

SeSA-HCPT is an orally active dual-target inhibitor integrating Topo I and HDAC inhibition. SeSA-HCPT induces potent DNA damage, apoptosis, S-phase arrest in prostate cancer cells. SeSA-HCPT inhibits cancer cells proliferation and migration. SeSA-HCPT impairs homologous recombination by suppressing KIF4A-RAD51 signaling. SeSA-HCPT markedly inhibits CRPC tumor growth with minimal systemic toxicity[1].

IC50 & Target[1]

Topoisomerase I

 

KIF4A

 

In Vitro

SeSA-HCPT (48 h) exerts superior selective cytotoxicity against AR-positive (LNCaP) and AR-negative (PC3, DU145) human prostate cancer cells with IC50 values of 0.182, 0.198 and 0.175 μM, with minimal toxicity to normal human keratinocyte HaCaT cells (IC50 =5.17 μM)[1].
SeSA-HCPT (200 nM; 24-48 h) induces significantly higher apoptosis in PC3, DU145, and LNCaP human prostate cancer cells[1].
SeSA-HCPT (0.175-5.17 μM; 24 h) induces S-phase cell cycle arrest in PC3, DU145, and LNCaP human prostate cancer cells, with no effect on normal human keratinocyte HaCaT cells, and upregulates Cyclin E expression in PC3 and DU145 cells[1].
SeSA-HCPT (3-10 μM) inhibits Topo1-mediated DNA relaxation, and exhibits binding affinity for the Topo1-DNA complex than HCPT, enhancing its ability to block Topo1 catalytic function[1].
SeSA-HCPT (1.25-5 nM) inhibits HDAC activity in PC3 and DU145 human prostate cancer cells[1].
SeSA-HCPT (1.25-5 nM) induces dose-dependent DNA damage in PC3 and DU145 human prostate cancer cells, as measured by increased γ-H2AX levels[1].
SeSA-HCPT (5 nM; 24-48 h) significantly inhibits proliferation and migration of PC3 and DU145 human prostate cancer cells[1].
SeSA-HCPT (0-50 nM; 24 h) impairs homologous recombination-mediated DNA repair in PC3 and DU145 human prostate cancer cells by downregulating KIF4A and reducing Rad51 recruitment to DNA damage sites, while inducing a DNA damage response, and induces a dose-dependent decrease in KIF4A levels from 0 to 50 nM[1].

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

SeSA-HCPT Related Antibodies

Apoptosis Analysis[1]

Cell Line: PC3, DU145, LNCaP cells
Concentration: 200 nM (Annexin V/PI staining); 200 nM (Western blot)
Incubation Time: 48 h (Annexin V/PI staining); 24 h (Western blot)
Result: Induced significantly higher levels of apoptosis.
Increased levels of cleaved caspase-3 and p21 in all three cell lines.

Cell Cycle Analysis[1]

Cell Line: PC3, DU145, LNCaP, HaCaT cells
Concentration: 0.175, 0.182, 0.198, 5.17 μM
Incubation Time: 24 h
Result: Induced significant S-phase arrest in PC3, DU145, and LNCaP cells.
Upregulated Cyclin E expression in PC3 and DU145 cells, with no significant changes in Cyclin A2 or Cyclin B levels.
Did not alter cell cycle distribution in HaCaT cells.

Western Blot Analysis[1]

Cell Line: PC3, DU145 cells
Concentration: 1, 5, 10, 30, 50 nM
Incubation Time: 24 h
Result: Increased γ-H2AX and phosphorylated ATM
(pS1981-ATM) levels at 5 nM.
Reduced KIF4A levels from 1 to 50 nM.
In Vivo

SeSA-HCPT (20 mg/kg; i.g.; sigle dose) potently inhibits castration-resistant prostate cancer xenograft growth, reduces tumor cell proliferation, induces DNA damage, and exhibits minimal systemic toxicity[1].

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

Animal Model: BALB/c nude (male, 5-week-old, subcutaneous xenograft of PC3 cells)[1]
Dosage: 20 mg/kg
Administration: I.g.; sigle dose
Result: Reduced tumor weight and growth significantly.
Reduced Ki67-positive cells pronouncedly.
Increased γ-H2AX-positive cells significantly .
Showed no significant body weight difference compared with controls.
Caused no significant alterations in hepatic (ALT, AST, ALP) or renal (BUN, creatinine) parameters.
Molecular Weight

1519.37

Formula

C76H76N6O18Se2
SMILES

O=C(NC1=CC(COC(CCC(OC2=C(C=C(CN3C4=CC5=C(COC(C5(CC)O)=O)C3=O)C4=N6)C6=CC=C2)=O)=O)=CC=C1)CCCCCC[Se][Se]CCCCCCC(NC7=CC(COC(CCC(OC8=C9C=C%10CN%11C(C%12=C(C=C%11C%10=NC9=CC=C8)C(O)(C(OC%12)=O)CC)=O)=O)=O)=CC=C7)=O
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
References
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SeSA-HCPT Related Classifications

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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:

SeSA-HCPTTopoisomeraseHDACApoptosisKinesinRAD51Histone deacetylasestopoisomerase IHaCaT cellsKIF4Anormal human keratinocytescastration-resistant prostate cancerprostate cancer cellsPC3DU145LNCaPInhibitorinhibitorinhibit

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