2. PROTAC Membrane Transporter/Ion Channel Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease PI3K/Akt/mTOR
  3. PROTACs P-glycoprotein Apoptosis Reactive Oxygen Species (ROS) Akt Bcl-2 Family Na+/K+ ATPase PI3K
  4. 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/110β Ligand (HY-75124); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W002042)).

For research use only. We do not sell to patients.

PROTAC PI3K/110β degrader-2 Chemical Structure

PROTAC PI3K/110β degrader-2 Chemical Structure

CAS No. : 3070438-79-5

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PROTAC PI3K/110β degrader-2 Related Antibodies

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Description

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/110β Ligand (HY-75124); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W002042))[1].

IC50 & Target

Bcl-2

 

Bax

 

PI3K

 

Akt

 

In Vitro

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.

PROTAC PI3K/110β degrader-2 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MCF-7/ADM and A549/DDP cells
Concentration: 6.25, 12.5 and 25 μM
Incubation Time: 24 h
Result: Significantly increased the proportion of cell apoptosis and the level of Caspase3, Cyt-3 and Caspase12.

Western Blot Analysis[1]

Cell Line: MCF-7/ADM and A549/DDP cells
Concentration: 25 μM
Incubation Time: 24 h
Result: Increased the protein level of P-PERK, ATF4, CHOP,.PTEN and BAX and decreased the protein level of P-AKT and Bcl-2.

Western Blot Analysis[1]

Cell Line: MCF-7/ADM and A549/DDP cells
Concentration: 0.25, 2.5 and 25 μM
Incubation Time: 24 h
Result: Significantly reduced the level of P-Glycoprotein.
In Vivo

PROTAC PI3K/110β degrader-2 (Compoud J-6) (50 mg/kg; i.p.; once every other day; 7 times) effectively inhibits the growth of tumor by degrading 110β protein in the MCF-7/ADM injected female BALB/c mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c mice (5-6 weeks) bearing MCF-7/ADM xenograft tumor[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection (i.p.); once every other day for 7 times
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.
Molecular Weight

948.18

Formula

C51H65N9O7S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC PI3K/110β degrader-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC PI3K/110β degrader-23070438-79-5PROTACsP-glycoproteinApoptosisReactive Oxygen Species (ROS)AktBcl-2 FamilyNa+/K+ ATPasePI3KP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243PKBProtein kinase BSodium potassium pumpPhosphoinositide 3-kinasePI3K/110βPROTACROScancerapoptosisBcl-2ERSInhibitorinhibitorinhibit

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