PROTAC IKKβ degrader-1
PROTAC IKKβ degrader-1 is a IKKβ PROTAC degrader (DC50 = 7.15 μM). PROTAC IKKβ degrader-1 induces apoptosis (Apoptosis) in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 induces G1 phase cell cycle arrest in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 exhibits antiproliferative activity against a variety of cells. PROTAC IKKβ degrader-1 is applicable for research related to cancers such as triple-negative breast cancer, colon cancer, liver cancer, pancreatic cancer.
(Pink: IKKβ ligand (HY-N0141); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W015659)).
For research use only. We do not sell to patients.
- Formula: C37H46N4O9
- Molecular Weight:690.78
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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
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Cereblon |
IKK-β 7.15 μM (DC50) |
PROTAC IKKβ degrader-1 (Compound 8) potently inhibits the proliferation of MDA-MB-231, HCT116, HepG, Panc-1, and MCF-7 cells, with IC50 values of 1.55, 2.52, 3.83, 3.67, and 4.12 μM, respectively[1].
PROTAC IKKβ degrader-1 (0-10 μM; 0-24 h) efficiently induces IKKβ protein degradation in MDA-MB-231 cells via the ubiquitin-proteasome system, with a DC50 of 7.15 μM, and the degradation rate reaches 91.24% after treatment with 10 μM for 24 h[1].
PROTAC IKKβ degrader-1 (2-5 μM; 48 h) potently induces apoptotic cell death in MDA-MB-231 cells. After 48 h of treatment, the total apoptotic rate reaches 46.43% at 2 μM and 61.37% at 5 μM[1].
PROTAC IKKβ degrader-1 (2-5 μM) induces G1-phase cell cycle arrest in MDA-MB-231 cells, with 69.64% of cells in G1 phase at the concentration of 2 μM and 71.15% at 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:MDA-MB-231
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Concentration:2 μM, 5 μM
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Incubation Time:48 h
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Result:Induced dose-dependent increases in early and late apoptotic cell populations.
At 2 μM, total apoptotic rate was 46.43% (15.82% early + 30.61% late).
At 5 μM, total apoptotic rate was 61.37% (23.33% early + 38.04% late).
Chemical Information
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Molecular Weight 690.78
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Formula C37H46N4O9
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SMILES
O=C1N(C2CCC(NC2=O)=O)C(C3=C(NCCCCCCCCNC(OC/C4=C/CC[C@@](C)(O5)[C@H]5[C@@H](OC(C6=C)=O)[C@H]6CC4)=O)C=CC=C31)=O
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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 IKKβ degrader-1 Related Classifications
HY-181660 Related Classifications
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