2. Epigenetics TGF-beta/Smad
  3. PKC
  4. TAS-301

TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.

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

TAS-301 Chemical Structure

TAS-301 Chemical Structure

CAS No. : 193620-69-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
5 mg USD 50 In-stock
10 mg USD 80 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

TAS-301 Related Antibodies

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.

IC50 & Target[1]

PKC

 

In Vitro

TAS-301 (1-10 μM) concentration-dependently inhibits PKC activation and Ca2+ influx, induced by PDGF, with 62.7% inhibition on PKC activation at 10 μM, and reduces PMA-induced AP-1, with 38% and 67.6% inhibition at 3 and 10 μM, respectively[1]. TAS-301 (0.3-3 μM) dose-dependently reduces the migration of cells induced by growth factors (PDGF-BB, IGF-1,HB-EGF). TAS-301 (1-10 μM) also decreases bFGF-induced BrdU incorporation, especially at 3 and 10 μM[2].

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

TAS-301 Related Antibodies
In Vivo

TAS-301 (3-100 mg/kg, p.o.) dose-dependently reduces the neointimal thickening and I/M ratio and decreases the level of intimal cells in rats 14 days after balloon injury[2].

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

357.40

Formula

C23H19NO3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NC2=C(C=CC=C2)/C1=C(C3=CC=C(OC)C=C3)/C4=CC=C(OC)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 38 mg/mL (106.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7980 mL 13.9899 mL 27.9799 mL
5 mM 0.5596 mL 2.7980 mL 5.5960 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Cell Assay
[2]

Cell proliferation is determined by the incorporation of BrdU by quiescent cells. SMCs are seeded at 1 × 104cells/well in 96-well plates in DMEM containing 10% FBS. Two days after the seeding, their growth is arrested for 3 days in a serum-free DMEM containing 5 μg/mL insulin, 5 μg/mL transferrin and 5 ng/mL sodium selenium (ITS). Then, the DMEM/ITS is removed, and serum-free DMEM containing 0.1% BSA with or without TAS-301 or tranilast is added to the quiescent cells 2 hr before treatment with the growth factor (i.e., bFGF 0.1 ng/mL). At 24 hr after stimulation, BrdU (10 μM) is added to the cells; 24 hr later, the cells are fixed. An ELISA is used to detect and to quantify the incorporated BrdU (n = 6). The drugs are present during the entire experiment[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Rats[2]
On the 14th day after the balloon injury, the rats are anesthetized with ether so as to avoid any stress to the animals and then perfused transcardially with saline, followed by 10% buffered formalin. Next, the left carotid artery (length from aortic arch to bifurcation) is removed, postfixed and embedded in paraffin. Then, 3-μm-thick artery sections (six sections for each artery) are cut and stained with hematoxylin and eosin. The cross-sectional areas of the intima and the media on photographs are measured by use of a digital analyzer. The average of the ratio of the intimal area to the medial area in each artery is determined. Experimental groups are as follows: Vehicle (n = 9), TAS-301 (3, 10, 30 and 100 mg/kg,n = 9) and tranilast (100 and 300 mg/kg,n = 9). The data on two rats (one in TAS-301 100 mg/kg group and one in tranilast 100 mg/kg group) is omitted from the evaluation because of death due to faulty oral administration[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7980 mL 13.9899 mL 27.9799 mL 69.9496 mL
5 mM 0.5596 mL 2.7980 mL 5.5960 mL 13.9899 mL
10 mM 0.2798 mL 1.3990 mL 2.7980 mL 6.9950 mL
15 mM 0.1865 mL 0.9327 mL 1.8653 mL 4.6633 mL
20 mM 0.1399 mL 0.6995 mL 1.3990 mL 3.4975 mL
25 mM 0.1119 mL 0.5596 mL 1.1192 mL 2.7980 mL
30 mM 0.0933 mL 0.4663 mL 0.9327 mL 2.3317 mL
40 mM 0.0699 mL 0.3497 mL 0.6995 mL 1.7487 mL
50 mM 0.0560 mL 0.2798 mL 0.5596 mL 1.3990 mL
60 mM 0.0466 mL 0.2332 mL 0.4663 mL 1.1658 mL
80 mM 0.0350 mL 0.1749 mL 0.3497 mL 0.8744 mL
100 mM 0.0280 mL 0.1399 mL 0.2798 mL 0.6995 mL
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TAS-301 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:

TAS-301193620-69-8TAS301TAS 301PKCProtein kinase CInhibitorinhibitorinhibit

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