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Art. -Nr.: HY-156244

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PROTAC GDI2 Degrader-1

PROTAC GDI2 Degrader-1 is a GDI2 PROTAC degrader with a DC₅₀ value of 1.48 μM and a K_d 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).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₅₉H₈₁N₇O₉
Molecular Weight:1032.32

Speicherung:

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

Data Sheet (270 KB)

PROTAC GDI2 Degrader-1 Chemical Structure

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Preis

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Amount: USD 0.00

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PROTAC GDI2 Degrader-1 is a GDI2 PROTAC degrader with a DC₅₀ value of 1.48 μM and a K_d 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^[1]. (Pink: GDI2 ligand (HY-156242); Blue: cIAP1 ligand (HY-175690); Black: linker).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

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 D_max 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.

Western Blot Analysis^[1]

Cell Line:

AsPC-1 pancreatic cancer cells
Concentration:

0.63, 1.25, 2.5, 5, 10 μM (dose-response); 5 μM (time-course)
Incubation Time:

24 h (dose-response); 0, 3, 6, 9, 12, 24 h (time-course)
Result:

Induced dose-dependent degradation of GDI2 with a DC₅₀ of 1.48 μM and a maximum degradation (D_max) of 84.2% at 10 μM after 24 h.
Achieved > 70% depletion of GDI2 after 9 h of treatment with 5 μM.

Western Blot Analysis^[1]

Cell Line:

PC-3 prostate cancer cells
Concentration:

2 μM
Incubation Time:

24 h
Result:

Reduced GDI2 protein levels to 61% of DMSO control levels after 24 h.

In Vivo

PROTAC GDI2 Degrader-1 (Compound 21) (15 mg/kg; i.p.; every 3 days; 18 days) significantly suppresses AsPC-1 pancreatic tumor growth in nude mice via GDI2 depletion and induction of paraptosis, with no observed systemic toxicity^[1].
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.

Animal Model:

BALB/c athymic nude mice (male, 6-8 weeks old, subcutaneous inoculation of 5 × 10⁶ AsPC-1 cells)^[1]
Dosage:

15 mg/kg
Administration:

i.p.; every 3 days; 18 days
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).

Animal Model:

BALB/c athymic nude mice (male, 6-8 weeks old, subcutaneous inoculation of ~3 mm³ human PDAC tumor fragments)^[1]
Dosage:

15 mg/kg
Administration:

i.p.; every 3 days; 18 days
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

Molecular Weight 1032.32
Formel C₅₉H₈₁N₇O₉
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 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)

Verweise

[1]. Yong Sun, et al. Targeting GDP-Dissociation Inhibitor Beta (GDI2) with a Benzo[a]quinolizidine Library to Induce Paraptosis for Cancer Therapy. JACS Au 2023, September 26, 2023

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

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MOQ

Minimum order quantity

100 mg

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