製品番号: HY-100035

PT-262

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Based on 1 Customer Validation

PT-262 is a potent ROCK inhibitor with an IC₅₀ value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.21%
CAS 番号: 86811-36-1
分子式: C₁₄H₁₃ClN₂O₂
分子量:276.72

保管条件:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

PT-262 構造式

CAS 番号: 86811-36-1

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

IC₅₀ & Target^[1]^[2]

ROCK

5 μM (IC₅₀)

ERK

CDK2

ROCK アイソフォーム固有の製品をすべて表示 :

ERK アイソフォーム固有の製品をすべて表示 :

CDK アイソフォーム固有の製品をすべて表示 :

体外実験

PT-262 (5-40 μM; 24 h) induces cytotoxicity and proliferation inhibition in human lung cancer cells^[1].
PT-262 (2-20 μM; 4-24 h) induces caspase-3 activation, mitochondrial dysfunction and apoptosis in lung cancer cells^[1].
PT-262 (10-20 μM; 24 h) induces the accumulation of G2/M phases in both the p53-wild type and p53-null lung cancer cells, and inhibits the phosphorylation of CDC2 proteins^[1].
PT-262 (0-10 μM; 24 h) represses ERK phosphorylation in lung cancer cells^[1].
PT-262 (2 μM; 24 h) induces the cytoskeleton alteration and cell elongation in lung carcinoma A549 cells^[2].
PT-262 (2-10 μM; 6 h) significantly blocks the cell migration in a concentration-dependent manner^[2].

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

Cell Viability Assay^[1]

Cell Line:

A549 cells
Concentration:

5-40 μM
Incubation Time:

24 h
Result:

Reduced the cell viability via a concentration-dependent manner in A549 cells.
The IC₅₀ value toward human normal lung fibroblast was >20 μM.

Apoptosis Analysis^[1]

Cell Line:

A549 cells
Concentration:

2-20 μM
Incubation Time:

4-24 h
Result:

The apoptotic cells were increased after treatment at 10 μM for 8-24 h.
The active forms of caspase-3 (12 and 17 kD) were induced following treatment with 2-20 μM for 24 h.

Cell Cycle Analysis^[1]

Cell Line:

A549 and H1299 cells
Concentration:

10-20 μM
Incubation Time:

24 h
Result:

Significantly decreased the G1 fractions while increased the G2/M fractions in both A549 and H1299 cells with 10 μM for 24 h.
Decreased the protein levels of cyclin B1 and phospho-CDC2 at Thr14, Tyr15, and Thr161 via a concentration-dependent manner in A549 cells.

Western Blot Analysis^[1]

Cell Line:

A549 cells
Concentration:

0-10 μM
Incubation Time:

24 h
Result:

Significantly inhibited the phosphorylation of ERK.

化学情報

CAS 番号 86811-36-1
性状 Solid
分子量 276.72
分子式 C₁₄H₁₃ClN₂O₂
Color Brown to reddish brown
SMILES

O=C(C(N1CCCCC1)=C2Cl)C3=C(N=CC=C3)C2=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (361.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.6138 mL

18.0688 mL

36.1376 mL

5 mM

0.7228 mL

3.6138 mL

7.2275 mL

10 mM

0.3614 mL

1.8069 mL

3.6138 mL

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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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

Stock Solution Working Solution

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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (9.03 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Tzu-Sheng Hsu, et al. 7-Chloro-6-piperidin-1-yl-quinoline-5,8-dione (PT-262), a novel synthetic compound induces lung carcinoma cell death associated with inhibiting ERK and CDC2 phosphorylation via a p53-independent pathway. Cancer Chemother Pharmacol. 2008 Oct;62(5):799-808. [Content Brief]

[2]. Chih-Chien Tsai, et al. 7-Chloro-6-piperidin-1-yl-quinoline-5,8-dione (PT-262), a novel ROCK inhibitor blocks cytoskeleton function and cell migration. Biochem Pharmacol. 2011 Apr 1;81(7):856-65. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.6138 mL	18.0688 mL	36.1376 mL	90.3440 mL
	5 mM	0.7228 mL	3.6138 mL	7.2275 mL	18.0688 mL
	10 mM	0.3614 mL	1.8069 mL	3.6138 mL	9.0344 mL
	15 mM	0.2409 mL	1.2046 mL	2.4092 mL	6.0229 mL
	20 mM	0.1807 mL	0.9034 mL	1.8069 mL	4.5172 mL
	25 mM	0.1446 mL	0.7228 mL	1.4455 mL	3.6138 mL
	30 mM	0.1205 mL	0.6023 mL	1.2046 mL	3.0115 mL
	40 mM	0.0903 mL	0.4517 mL	0.9034 mL	2.2586 mL
	50 mM	0.0723 mL	0.3614 mL	0.7228 mL	1.8069 mL
	60 mM	0.0602 mL	0.3011 mL	0.6023 mL	1.5057 mL
	80 mM	0.0452 mL	0.2259 mL	0.4517 mL	1.1293 mL
	100 mM	0.0361 mL	0.1807 mL	0.3614 mL	0.9034 mL

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PT-262

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Bioactive Compound Library Max

Bioactive Compound Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

ROCK アイソフォーム固有の製品をすべて表示

ERK アイソフォーム固有の製品をすべて表示

CDK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

PT-262 関連分類

HY-100035 関連分類