2. PROTAC PI3K/Akt/mTOR
  3. PROTACs PI3K Akt
  4. HL-8

HL-8 is a PI3Kα PROTAC degrader. HL-8 promotes the ubiquitination and degradation of PI3Kα. HL-8 reduces pAKT levels. HL-8 has anticancer activity against colon and cervical cancer (Pink: PI3Kα ligand (HY-143277); Blue: E3 ligase VHL ligand (HY-138678); Black: linker (HY-W002042)).

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HL-8

HL-8 構造式

CAS 番号 : 2766352-64-9

容量 価格（税別） 在庫状況 数量
1 mg $676 在庫あり
5 mg $1420 在庫あり
10 mg $2340 在庫あり
25 mg $4680 在庫あり
50 mg   お問い合わせ  
100 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

HL-8 関連抗体

Top Publications Citing Use of Products

PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

PI3K アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Akt アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Akt Akt1 Akt2 Akt3

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

HL-8 is a PI3Kα PROTAC degrader. HL-8 promotes the ubiquitination and degradation of PI3Kα. HL-8 reduces pAKT levels. HL-8 has anticancer activity against colon and cervical cancer (Pink: PI3Kα ligand (HY-143277); Blue: E3 ligase VHL ligand (HY-138678); Black: linker (HY-W002042))[1].

体外実験

HL-8 (1 nM) inhibits PI3Kα kinase by 49.75%[1].
HL-8 (10 μM; 72 h) inhibits the proliferation of HT-29, HCT-116, and Hela cells by 72.18%, 50.30%, and 96.33%, respectively[1].
HL-8 (10 μM; 2-24 h) significantly degrades PI3Kα and reduces phosphorylated AKT levels in Hela cells[1].

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

HL-8 関連抗体
分子量

1144.27

分子式

C57H59F2N11O9S2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

COC1=NC=C(C=C1NS(=O)(C2=C(C=C(C=C2)F)F)=O)C3=CN4C(C5=NN=C(O5)C6=C(C=CC=C6)C(NCCCCCCC(N[C@@H](C(C)(C)C)C(N7C[C@H](C[C@@H]7C(NCC8=CC=C(C=C8)C9=C(N=CS9)C)=O)O)=O)=O)=O)=CN=C4C=C3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (87.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8739 mL 4.3696 mL 8.7392 mL
5 mM 0.1748 mL 0.8739 mL 1.7478 mL
10 mM 0.0874 mL 0.4370 mL 0.8739 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.8739 mL 4.3696 mL 8.7392 mL 21.8480 mL
5 mM 0.1748 mL 0.8739 mL 1.7478 mL 4.3696 mL
10 mM 0.0874 mL 0.4370 mL 0.8739 mL 2.1848 mL
15 mM 0.0583 mL 0.2913 mL 0.5826 mL 1.4565 mL
20 mM 0.0437 mL 0.2185 mL 0.4370 mL 1.0924 mL
25 mM 0.0350 mL 0.1748 mL 0.3496 mL 0.8739 mL
30 mM 0.0291 mL 0.1457 mL 0.2913 mL 0.7283 mL
40 mM 0.0218 mL 0.1092 mL 0.2185 mL 0.5462 mL
50 mM 0.0175 mL 0.0874 mL 0.1748 mL 0.4370 mL
60 mM 0.0146 mL 0.0728 mL 0.1457 mL 0.3641 mL
80 mM 0.0109 mL 0.0546 mL 0.1092 mL 0.2731 mL
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HL-8 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

HL-82766352-64-9HL8HL 8PROTACsPI3KAktPhosphoinositide 3-kinasePKBProtein kinase BPI3K kinasecancer diseasesInhibitorinhibitorinhibit

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製品名:
HL-8
製品番号:
HY-143275
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