2. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton MAPK/ERK Pathway Apoptosis
  3. ROCK ERK CDK Apoptosis
  4. PT-262

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.

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

PT-262 Chemical Structure

PT-262 Chemical Structure

CAS No. : 86811-36-1

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5 mg USD 120 In-stock
10 mg USD 190 In-stock
25 mg USD 380 In-stock
50 mg USD 620 In-stock
100 mg USD 980 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PT-262 Related Antibodies

Top Publications Citing Use of Products

View All ROCK Isoform Specific Products:

View All Isoforms
ROCK ROCK1 ROCK2

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • Biological Activity

  • Purity & Documentation

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Description

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[1][2].

IC50 & Target[1][2]

ROCK

5 μM (IC50)

ERK

 

CDK2

 

In Vitro

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.

PT-262 Related Antibodies

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.
Molecular Weight

276.72

Formula

C14H13ClN2O2
CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

O=C(C(N1CCCCC1)=C2Cl)C3=C(N=CC=C3)C2=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6138 mL 18.0688 mL 36.1376 mL
5 mM 0.7228 mL 3.6138 mL 7.2275 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 (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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

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    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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

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(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).

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

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.
Purity & Documentation
References

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 (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.

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 Related Classifications

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:

PT-26286811-36-1PT262PT 262ROCKERKCDKApoptosisRho-associated protein kinaseRho-associated kinaseRho-kinaseROKExtracellular signal regulated kinasesCyclin dependent kinasemitochondrial membrane potentialcaspase-3p-ERKp-CDC2p53-independent cytoskeletonmigrationG2/MG1Inhibitorinhibitorinhibit

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