PROTAC GDI2 Degrader-1
PROTAC GDI2 Degrader-1 is a GDI2 PROTAC degrader with a DC50 value of 1.48 μM and a Kd value of 23.9 μM. PROTAC GDI2 Degrader-1 triggers paraptosis in tumor cells via endoplasmic reticulum expansion and fusion, endoplasmic reticulum stress, unfolded protein response, and cytoplasmic vacuolization. PROTAC GDI2 Degrader-1 exhibits significant in vivo anti-tumor activity in pancreatic cancer xenograft models. PROTAC GDI2 Degrader-1 can be used for research related to pancreatic cancer.
(Pink: GDI2 ligand (HY-156242); Blue: cIAP1 ligand (HY-175690); Black: linker).
For research use only. We do not sell to patients.
- Formula: C59H81N7O9
- Molecular Weight:1032.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
PROTAC GDI2 Degrader-1 (Compound 21) (0.63-10 μM; 24 h; 5 μM; 0-24 h) degrades GDI2 in AsPC-1 pancreatic cancer cells in a dose-dependent manner with a DC50 of 1.48 μM and a Dmax of 84.2%, and in a time-dependent manner with > 70% depletion observed by 9 h[1].
PROTAC GDI2 Degrader-1 (2 μM; 24 h) reduces GDI2 protein levels to 61% of control in PC-3 prostate cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AsPC-1 pancreatic cancer cells
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Concentration:0.63, 1.25, 2.5, 5, 10 μM (dose-response); 5 μM (time-course)
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Incubation Time:24 h (dose-response); 0, 3, 6, 9, 12, 24 h (time-course)
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Result:Induced dose-dependent degradation of GDI2 with a DC50 of 1.48 μM and a maximum degradation (Dmax) of 84.2% at 10 μM after 24 h.
Achieved > 70% depletion of GDI2 after 9 h of treatment with 5 μM.
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Cell Line:PC-3 prostate cancer cells
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Concentration:2 μM
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Incubation Time:24 h
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Result:Reduced GDI2 protein levels to 61% of DMSO control levels after 24 h.
PROTAC GDI2 Degrader-1 (15 mg/kg; i.p.; every 3 days; 18 days) significantly suppresses growth of patient-derived pancreatic adenocarcinoma tumors in nude mice via GDI2 depletion and induction of paraptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c athymic nude mice (male, 6-8 weeks old, subcutaneous inoculation of 5 × 106 AsPC-1 cells)[1]
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Dosage:15 mg/kg
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Administration:i.p.; every 3 days; 18 days
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Result:Significantly attenuated tumor growth compared to the vehicle group.
Achieved over 90% GDI2 depletion that was not restored 72 hours post final injection.
Elevated protein levels of ER stress/UPR markers GRP78, CHOP, and p-eIF2α in tumor tissues.
Induced extensive cytoplasmic vacuolization indicating paraptosis in tumor tissues.
Caused no significant body weight loss or histopathological injury to major organs (heart, lung, liver, spleen, kidney).
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Animal Model:BALB/c athymic nude mice (male, 6-8 weeks old, subcutaneous inoculation of ~3 mm3 human PDAC tumor fragments)[1]
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Dosage:15 mg/kg
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Administration:i.p.; every 3 days; 18 days
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Result:Significantly suppressed PDAC tumor growth to levels similar to the gemcitabine positive control group.
Achieved excellent GDI2 depletion in PDAC tumors.
Elevated protein levels of ER stress/UPR markers GRP78, CHOP, and p-eIF2α in tumor tissues.
Induced cytoplasmic vacuolization in tumor tissues.
Caused no significant systemic toxicity.
Chemical Information
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Molecular Weight 1032.32
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Formula C59H81N7O9
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SMILES
CC1=CC(C)=CC(COC2=CC3=C([C@](C[C@](O)(CC4=CN(CCOCCOCCOCCNC([C@@H](CC(C)C)NC([C@@H](O)[C@H](N)CC5=CC=CC=C5)=O)=O)N=N4)C[C@@H]6C)([H])N6CC3)C=C2OCC7=CC(C)=CC(C)=C7)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC GDI2 Degrader-1 Related Classifications
HY-156244 Related Classifications
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