PROTAC PDIA1 degrader 1
PROTAC PDIA1 degrader 1 is a PDIA1 PROTAC degrader with a DC50 of 29.71 μM. PROTAC PDIA1 degrader 1 induces proteasome-dependent PDIA1 degradation via recruiting E3 ligase, ubiquitination and proteasomal degradation processes. PROTAC PDIA1 degrader 1 exhibits anticancer activity against breast cancer and epidermoid carcinoma. PROTAC PDIA1 degrader 1 can be used for the research of breast cancer and epidermoid carcinoma.
(Pink: PDIA1 ligand (HY-100433); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W015088)).
For research use only. We do not sell to patients.
- CAS No.: 3024292-21-2
- Formula: C40H44N6O12S
- Molecular Weight:832.88
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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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Biological Activity
Description
IC50 & Target
[1]|
PDIA1 29.71 μM (DC50) |
Cereblon |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | DC50 |
29.71 μM
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Half-maximum degradation concentration of PDIA1 in human epidermoid carcinoma A431 cells measured via western blotting after 12 h incubation.
Half-maximum degradation concentration of PDIA1 in human epidermoid carcinoma A431 cells measured via western blotting after 12 h incubation.
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38917491 |
| MCF7 | DC50 |
>50 μM
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Half-maximum degradation concentration of PDIA1 in human breast cancer MCF-7 cells measured via western blotting after 12 h incubation.
Half-maximum degradation concentration of PDIA1 in human breast cancer MCF-7 cells measured via western blotting after 12 h incubation.
|
38917491 |
| MCF7 | IC50 |
18.4 μM
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Antiproliferative activity against human breast cancer MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
Antiproliferative activity against human breast cancer MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
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38917491 |
| A-431 | IC50 |
13.5 μM
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Antiproliferative activity against human epidermoid carcinoma A431 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
Antiproliferative activity against human epidermoid carcinoma A431 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
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38917491 |
In Vitro
PROTAC PDIA1 degrader 1 (Compound H4) (1-50 μM; 2-24 h) induces proteasome-dependent, time- and concentration-selective degradation of PDIA1 in A431 cells with a DC50 of 29.71 μM and in MCF-7 cells with a DC50 of >50 μM[1].
PROTAC PDIA1 degrader 1 (72 h) inhibits proliferation of MCF-7 cells with an IC50 of 18.4 μM and A431 cells with an IC50 of 13.5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human breast cancer MCF-7 cells, human epidermoid carcinoma A431 cells
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Concentration:1-50 μM (standard incubation); 50 μM (time-course); 20 μM (with pre-treatment of 200 μM pomalidomide or 2 μM MG-132)
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Incubation Time:12 h (standard incubation); 2-24 h (time-course); 12 h (with pre-treatment)
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Result:Induced potent, selective degradation of PDIA1 with minimal impact on PDIA3, PDIA4, and PDIA6.
Reached 62% PDIA1 degradation in A431 cells at 12 h and 64% at 24 h.
Exhibited a half-maximum degradation concentration (DC50) of 29.71 μM in A431 cells.
Showed a DC50 of >50 μM in MCF-7 cells.
Demonstrated time-dependent degradation, with <30% degradation observed within the first 8 h.
Abrogated PDIA1 degradation was observed when cells were pre-treated with pomalidomide or MG-132, confirming proteasome-dependent degradation and requirement for binding to both PDIA1 and the cereblon E3 ligase.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (5 weeks old)[1]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Maintained stable body weight with slight fluctuations at 50 mg/kg and 100 mg/kg doses.
Showed no significant tissue abnormalities in heart, liver, spleen, lung, and kidney at 100 mg/kg.
Kept serum levels of ALT, AST, ALP, BUN, and creatinine within normal ranges; increased BUN levels 2-fold but remained within normal limits.
Chemical Information
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CAS No. 3024292-21-2
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Molecular Weight 832.88
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Formula C40H44N6O12S
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SMILES
COC1=C(N(C(C#C)=O)C(C(NCC(NCCOCCOCCOCCNC2=C(C(N(C3C(NC(CC3)=O)=O)C4=O)=O)C4=CC=C2)=O)=O)C5=CC=CS5)C=CC(OC)=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 PDIA1 degrader 1 Related Classifications
HY-178118 Related Classifications
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