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

PROTAC PI3Kδ degrader-1 是一种靶向赖氨酸的共价 PI3Kδ PROTAC 降解剂，DC50 为 3.98 nM。PROTAC PI3Kδ degrader-1 具有强效的抗增殖活性和 PI3Kδ 选择性抑制 (IC50：8 nM)。PROTAC PI3Kδ degrader-1 还能显著降解 p-AKT，诱导细胞周期停滞于 G1 期，并促进细胞凋亡 (apoptosis) 和自噬 (autophagy)。PROTAC PI3Kδ degrader-1 可有效抑制 SU-DHL-6 异种移植小鼠模型中的肿瘤生长。粉色：PI3Kδ ligand (HY-169983)；蓝色：VHL ligase ligand (HY-112078)；黑色：linker (HY-W013381)

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PROTAC PI3Kδ degrader-1

PROTAC PI3Kδ degrader-1 Chemical Structure

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PROTAC PI3Kδ degrader-1 相关抗体

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

PROTAC PI3Kδ degrader-1 (Compound B14) (0.001-10 μM，72 小时) 对 SU-DHL-6 和 Pfeiffer 细胞(GI50：分别为 0.17 和 0.35 μM)[1]。
PROTAC PI3Kδ degrader-1 (10 mM，0-48 小时) 具有优异的稳定性，孵育 48 小时后仍有 80% 的残留[1]。
PROTAC PI3Kδ degrader-1 (0.1-1 μM，6-24 小时) 以剂量和时间依赖性方式降解 SU-DHL-6 细胞中 p-AKT 和 p110δ (DC50：3.98 nM)[1]。
PROTAC PI3Kδ degrader-1 (1-100 nM，24 小时) 可增加 LC3II /LC3I 的比例，从而启动 SU-DHL-6 细胞中的自噬[1]。
PROTAC PI3Kδ degrader-1 (100 nM，6-24 小时) 以时间依赖性的方式降解 SU-DHL-6 细胞 p110δ，且降解作用持续时间延长[1]。
PROTAC PI3Kδ degrader-1 (0.1-1 μM，12 小时) 对 VHL 连接酶配体和 p110δ 及 p-AKT 具有更高的结合亲和力，且两种衍生物的抗增殖活性与其自身相比较弱 (GI50：0.17 vs 0.90 和 0.87 μM)[1]。
PROTAC PI3Kδ degrader-1 (100 nM，12 小时) 通过泛素-蛋白酶体途径降解 SU-DHL-6 细胞中的 p110δ，而这种作用可以被 MLN4924 (HY-70062) (泛素化抑制剂) 和 MG132 (HY-13259) (蛋白酶体抑制剂) 逆转[1]。
PROTAC PI3Kδ degrader-1 选择性抑制 SU-DHL-6 细胞中 PI3Kδ (IC50：8 nM)，对其他三种亚型的选择性高出 70 倍以上 (IC50 均 >589 nM)[1]。
PROTAC PI3Kδ degrader-1 (1-1000 nM，24 小时) 对 SU-DHL-6 细胞中的 p110δ 有较强的降解作用，但对 p110α 和 p110β 蛋白水平 (DC50 > 1000 nM) 的降解作用较弱，对 p110γ 无降解作用[1]。
PROTAC PI3Kδ degrader-1 (0.01-1 μM，24 小时) 以剂量依赖性方式增加 SU-DHL-6 细胞中 G1 期细胞的比例并显著诱导细胞死亡和损伤[1]。

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

PROTAC PI3Kδ degrader-1 相关抗体:

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.
体内研究
(In Vivo)

PROTAC PI3Kδ degrader-1 (Compound B14) (2-10 mg/kg，腹腔注射，每 2 天一次，共 21 天) 在 SU-DHL-6 异种移植小鼠模型中表现出显著的抗肿瘤功效，且无明显毒性[1]。

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.
分子量

1150.44

Formula

C63H79N11O8S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PROTAC PI3Kδ degrader-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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