2. MAPK/ERK Pathway Apoptosis Metabolic Enzyme/Protease Membrane Transporter/Ion Channel Neuronal Signaling NF-κB Immunology/Inflammation
  3. p38 MAPK Caspase Cytochrome P450 Calcium Channel Reactive Oxygen Species (ROS) Apoptosis Mitochondrial Metabolism GLUT
  4. PeS-9

PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors.

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

PeS-9 Chemical Structure

PeS-9 Chemical Structure

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PeS-9 Related Antibodies

Top Publications Citing Use of Products

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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GLUT1 GLUT2 GLUT3 GLUT4

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Description

PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors[1].
In Vitro

PeS-9 (48 h) shows cytotoxicity in cancer cells with IC50s of 0.49 μM (DU145), and 0.58 μM (LNCaP), while has low cytotoxicity for noncancer cells with IC50s of 3.41 μM (PNT2), 3.53 μM (MRC-9), 11.7 μM (HUVEC) and 7.51 μM (HEK)[1].

PeS-9 (0-2.5 μM, 4-48 h) downregulates the AR signaling pathway, produces ROS, and damages DNA in 22Rv1 cells[1].

PeS-9 (48 h) synergizes with antiandrogen Enzalutamide (HY-70002) and PARP inhibitor Olaparib (HY-10162) with CI ＜ 0.75 in 22Rv1 cells[1].

PeS-9 (0-1 μM, 1 h) activates the MAPK signaling pathways by increasing the level of stress kinases p-p38, p-JNK, and p-ERK in 22Rv1 cells, which can be antagonized by the tested MAPK inhibitor[1].

PeS-9 (0-2.5 μM, 1-48 h) induces apoptosis in 22Rv1 cells through mitochondrial targeting and cytotoxic ROS induction[1].

PeS-9 (0-2.5 μM, 1-48 h) causes increased cytosolic Ca2+ levels, expansion of the endoplasmic reticulum (ER), altered mitochondrial membrane permeability, and DNA damage, as quantified by an elevated sub-G1 cell population[1].

PeS-9 (0.5-4 μM, 24 h) inhibits the uptake of glucose in 22Rv1 cells, and this effect can be inhibited by GLUT-1 inhibitor Phloretin (HY-N0142)[1].

PeS-9 (0.1-10 μM, every 5 days over 20 days) reduces the survival fractions of tumoroids upon dose-dependently[1].

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

PeS-9 Related Antibodies

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 1, 2 μM
Incubation Time: 48 h
Result: Downregulated AR-FL, AR-V7, PSA, IGF-1 proteins dose-dependently.

Real Time qPCR[1]

Cell Line: 22Rv1 cells
Concentration: 0, 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Inhibited the transcription of TMPRSS2, FKBP5 and PSA genes dose-dependently.

Immunofluorescence[1]

Cell Line: 22Rv1 cells
Concentration: 1.25, 2.5 μM
Incubation Time: 4, 24 h,48h
Result: Induced DNA double-strand breaks (DSBs), as demonstrated by γH2AX/53BP1 foci formation Triggered primary DNA damage within 4 hours of treatment, reached peak damage levels at 24 hours, and showed signs of DNA repair activation by 48 hours.

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 0.5-4 μM
Incubation Time: 48 h
Result: Increased Bax/Bcl-2 ratio (0.5, 1, 2, 4, 8 μM).
Downregulated of antiapoptotic surviving-survivin (1, 2, μM).
Released cytotoxic mitochondrial proteins such as apoptosis-inducing factor (AIF) and cytochrome C to cellular cytoplasm (2, 4 μM).
Increased the level of caspase-9, caspase-3 and PRAP (2, 4 μM).
In Vivo

PeS-9 (27.9 mg/kg, i.p., daily for 15 days) exerts in vivo antitumor and antimetastatic activity with minor side effects in immunocompromised NOD/SCID gamma (NSG) mice bearing subcutaneously xenotransplanted human prostate cancer 22Rv1 cells[1].

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

Animal Model: NOD/SCID gamma (NSG) 8-12 weeks mice bearing subcutaneously xenotransplanted human prostate cancer 22Rv1 cells[1].
Dosage: 27.9 mg/kg
Administration: Daily i.p. administration for 15 days
Result: Reduced 40.0% tumor volume compared with the control group (1069.5 mm3 vs. 646.6 mm).
Reduced 4.4-fold lung micrometastases.
Showed no significant difference on the weights of the body, heart, lungs, liver, and kidney.
Enlarged spleen that indicate an immunostimulatory effect of the treatment.
Showed no significant difference on the white and red blood cells, platelets, hemoglobin content, and hematocrit.
Revealed no signs of tissue damage, inflammation or granuloma.
Molecular Weight

580.56

Formula

C26H28O13S
SMILES

COC1=C(CSC[C@H]2O[C@H]([C@@H]([C@H]([C@@H]2OC(C)=O)OC(C)=O)OC(C)=O)OC(C)=O)C(C3=C(C=CC=C3O)C1=O)=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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PeS-9 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:

PeS-9PeS9PeS 9p38 MAPKCaspaseCytochrome P450Calcium ChannelReactive Oxygen Species (ROS)ApoptosisMitochondrial MetabolismGLUTCYPsCa2+ channelsCa channelsGlucose transporterMAPK22Rv1 cellscancerInhibitorinhibitorinhibit

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