PROTAC PI3K/110β degrader-2
PROTAC PI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. PROTAC PI3K/110β degrader-2 can significantly degrade 110β protein and inhibit the expression of P-glycoprotein. PROTAC PI3K/110β degrader-2 can increase the level of reactive oxygen species (ROS). PROTAC PI3K/110β degrader-2 exerts anti-tumor effects by activating the endoplasmic reticulum stress (ERS)-mediated mitochondrial apoptosis pathway and inhibiting the AKT/Bcl-2 signaling pathway. PROTAC PI3K/110β degrader-2 can be used for research on cancer.
(Pink: PI3K and p110β ligand (HY-75124); Blue: VHL ligand (HY-125845); Black: linker (HY-W002042)).
For research use only. We do not sell to patients.
- CAS No.: 3070438-79-5
- Formula: C51H65N9O7S
- Molecular Weight:948.18
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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
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Biological Activity
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PI3K |
Bax |
Bcl-2 |
Akt |
PROTAC PI3K/110β degrader-2 (Compoud J-6) (24 h) has significant anti-tumor activity in A549 (IC50 = 58.2 μM), A549/DDP (IC50 = 39.23 μM), MCF-7 (IC50 = 53.99 μM) and MCF-7/ADM (IC50 = 38.73 μM) cells[1].
PROTAC PI3K/110β degrader-2 (0-50 μM, 0-48 h) can selectively degrade 110β protein in MCF-7/ADM and A549/DDP cells in a time and concentration-dependent manner[1].
PROTAC PI3K/110β degrader-2 (0-25 μM, 24 h) significantly increases ROS levels, reduces mitochondrial membrane potential, and activates ERS mediated apoptosis in MCF-7/ADM and A549/DDP cells[1].
PROTAC PI3K/110β degrader-2 (0-25 μM, 24 h) inhibits Na+/K+-ATPase activity and reduces P-Glycoprotein expression in MCF-7/ADM and A549/DDP cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7/ADM and A549/DDP cells
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Concentration:6.25, 12.5 and 25 μM
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Incubation Time:24 h
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Result:Significantly increased the proportion of cell apoptosis and the level of Caspase3, Cyt-3 and Caspase12.
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Cell Line:MCF-7/ADM and A549/DDP cells
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Concentration:25 μM
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Incubation Time:24 h
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Result:Increased the protein level of P-PERK, ATF4, CHOP,.PTEN and BAX and decreased the protein level of P-AKT and Bcl-2.
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Cell Line:MCF-7/ADM and A549/DDP cells
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Concentration:0.25, 2.5 and 25 μM
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Incubation Time:24 h
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Result:Significantly reduced the level of P-Glycoprotein.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice (5-6 weeks) bearing MCF-7/ADM xenograft tumor[1]
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Dosage:50 mg/kg
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Administration:Intraperitoneal injection (i.p.); once every other day for 7 times
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Result:Significantly reduced tumor volume.
Effectively downregulated the level of 110β in tumor tissue.
Significantly increased the level of ATF6, CHOP, GRP78, Caspase-12 and BAX inhibited caspase-8, P-AKT, Bcl-2 and P-Glycoprotein.
Did not significantly affect weight and did not cause organ damage.
Chemical Information
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CAS No. 3070438-79-5
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Molecular Weight 948.18
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Formula C51H65N9O7S
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SMILES
O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@H](C(C)(C)C)NC(CCCCCCNC(C4=CC=CC=C4NC(C)C5=CC(C)=CN6C5=NC(N7CCOCC7)=CC6=O)=O)=O)=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 PI3K/110β degrader-2 Related Classifications
HY-174469 Related Classifications
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