2. PROTAC PI3K/Akt/mTOR Apoptosis Autophagy
  3. PROTACs PI3K Akt Apoptosis Autophagy
  4. PROTAC PI3Kδ degrader-1

PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model. Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)

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PROTAC PI3Kδ degrader-1 Chemical Structure

PROTAC PI3Kδ degrader-1 Chemical Structure

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PROTAC PI3Kδ degrader-1 Related Antibodies

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Akt Akt1 Akt2 Akt3

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Description

PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model[1]. Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)

IC50 & Target

PI3Kδ

3.98 nM (DC50)

PI3Kδ

8 nM (IC50)

PI3Kα

589 nM (IC50)

PI3Kβ

>10000 nM (IC50)

PI3Kγ

605 nM (IC50)

In Vitro

PROTAC PI3Kδ degrader-1 (Compound B14) (0.001-10 μM, 72 h) has a potent antiproliferation activity against SU-DHL-6 and Pfeiffer cells (GI50: 0.17 and 0.35 μM, respectively)[1].
PROTAC PI3Kδ degrader-1 (10 mM, 0-48 h) has excellent stability with 80% remains After 48 h incubation[1].
PROTAC PI3Kδ degrader-1 (0.1-1 μM, 6-24 h) dose- and time-dependently degrades p-AKT and p110δ (DC50: 3.98 nM) in SU-DHL-6 cells[1].
PROTAC PI3Kδ (1-100 nM, 24 h) degrader-1 increases the ratio of LC3II /LC3I, booting up the autophagy in SU-DHL-6 cells[1].
PROTAC PI3Kδ degrader-1 (0.1-1 μM, 12 h) has a superior binding affinity to VHL ligase ligand, p110δ and p-AKT, and its two derivatives has a weaker antiproliferative activity compared to itself (GI50: 0.17 vs 0.90 and 0.87 μM)[1].
PROTAC PI3Kδ degrader-1 (100 nM, 12 h) degrades p110δ with a ubiquitin-proteasome pathways in SU-DHL-6 cells, and this effect is reversed by MLN4924 (HY-70062) (ubiquitination inhibitor) and MG132 (HY-13259) (proteasome inhibitor)[1].
PROTAC PI3Kδ degrader-1 selectively inhibits PI3Kδ (IC50: 8 nM), with > 70-fold selectivity for the other three isoforms (IC50s : >589 nM, respectively) in SU-DHL-6 cells[1].
PROTAC PI3Kδ degrader-1 (1-1000 nM, 24 h) has a strong degradation effect in p110δ but weak effect in p110α and p110β protein levels (DC50 > 1000 nM) and no degradation in p110γ in SU-DHL-6 cells[1].
PROTAC PI3Kδ degrader-1 (0.01-1 μM, 24 h) dose-dependently increases the proportion of cells in G1 phase and significantly induces cell death and damage in SU-DHL-6 cells[1].

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

PROTAC PI3Kδ degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: SU-DHL-6 cells
Concentration: 0.1, 1, 3, 10, 30, 100, 1000 nM
Incubation Time: 24 h
Result: Effectively degraded the protein levels of p110δ and p-AKT at 100 and 1000 nM.
Induced the degradation of p110δ in a concentration-dependent manner, and the levels of p-AKT were lowered correspondingly.
Increased the ratio of LC3II /LC3I, booting up the autophagy.
exhibited much effective p110δ degradation activity with 58% and 65% degradation of p110δ at 100 and 1 000 nM.

Cell Cycle Analysis[1]

Cell Line: SU-DHL-6 cells
Concentration: 0.01, 0.1, 1 μM
Incubation Time: 24 h
Result: Dose-dependently increased the proportion of cells in G1 phase.
Potently induced the cell cycle arrest at 0.1 μM compared that at 10 μM of Idelalisib (HY-13026).

Apoptosis Analysis[1]

Cell Line: SU-DHL-6 cells
Concentration: 0.01, 0.1, 1 μM
Incubation Time: 24 h
Result: Induced a significant amount of cell death and damage.
Induced much higher cell apoptotic percentages than that of Idelalisib with the same dose.
In Vivo

PROTAC PI3Kδ degrader-1 (Compound B14) (2-10 mg/kg, i.p., every 2 days for 21  days) demonstrates significant antitumor efficacy without obvious toxicity in SU-DHL-6 xenograft mice model[1].

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

Animal Model: Male Balb/c nude mice (4-6 weeks old) were injected subcutaneously with SU-DHL-6 cells (1× 107 cells/mouse)[1].
Dosage: 2, 10 mg/kg
Administration: i.p., every 2 days for 21  days and then measured tumor size and body weight.
Result: Exhibited remarkable antitumor efficacy with tumor growth inhibition of 59.1 and 73.3% at 2 and 10 mg/kg doses, respectively.
Induced no substantial toxic effects without significant body weight changes and death up to 10 mg/kg.
Significantly reduced p110δ protein levels, and dose-dependently decreased the expression of p-AKT.
Had a significant antiproliferative activity with reduction of Ki67 level.
Caused no obvious organ damage with normal morphology in the tissues of heart, liver, spleen, and kidneys.
Molecular Weight

1150.44

Formula

C63H79N11O8S
SMILES

O=C([C@@H](NC(CCCCCCCCCN1CCC(C(N2CC[C@H](NC3=NC=NC4=CC=C(C5=CN=C(C(C(OC6=CC=CC=C6)=O)=C5)OC)N=C43)C2)=O)CC1)=O)C(C)(C)C)N7[C@@H](C[C@H](C7)O)C(N[C@H](C8=CC=C(C=C8)C9=C(N=CS9)C)C)=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 PI3Kδ degrader-1 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 PI3Kδ degrader-1PROTACsPI3KAktApoptosisAutophagyPhosphoinositide 3-kinasePKBProtein kinase BPROTACDegradationPI3KδAntiproliferationAntitumorSU-DHL-6 cellsSU-DHL-6 xenograft mice modelInhibitorinhibitorinhibit

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