1. Epigenetics
    TGF-beta/Smad
    Apoptosis
  2. PKC
    Apoptosis
  3. PKCβ inhibitor 1

PKCβ inhibitor 1 

Cat. No.: HY-13335 Purity: 98.21%
Handling Instructions

PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).

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

PKCβ inhibitor 1 Chemical Structure

PKCβ inhibitor 1 Chemical Structure

CAS No. : 257879-35-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 724 In-stock
Estimated Time of Arrival: December 31
500 μg USD 155 In-stock
Estimated Time of Arrival: December 31
1 mg USD 275 In-stock
Estimated Time of Arrival: December 31
5 mg USD 800 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε)[1][2].

IC50 & Target[1]

human PKCβ1

21 nM (IC50)

human PKCβ2

5 nM (IC50)

PKCα

331 nM (IC50)

In Vitro

PKCβ inhibitor 1 (0-30 μM; 48 hours) suppresses tumor cell proliferation in a time- and dose-dependent manner[2].
PKCβ inhibitor 1 (14 μM; 2-48 hours) induces apoptosis in 2F7 cells[2].
PKCβ inhibitor 1 (15 μM; 2-48 hours) inhibits cell cycle progression in 2F7 and BCBL-1 cells[2].
PKCβ (15 or 14 μM, respectively; 2-48 hours) inhibitor 1 reduces the expression of phospho-PKCβ in BCBL-1 and 2F7 cells[2].
PKCβ inhibitor 1(0-48 hours) suppresses GSK3β, mTOR, and S6 phosphorylation[2].

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

Cell Proliferation Assay[2]

Cell Line: 2F7, BCBL-1 cells
Concentration: 0, 5, 10, 20, and 30 μM
Incubation Time: 48 hours
Result: A dose-dependent reduction in viability of the 2F7 and BCBL-1 cells starting at 5 μM and increasing with elevated inhibitor concentration.

Apoptosis Analysis[2]

Cell Line: 2F7 cells
Concentration: 14 μM
Incubation Time: 2-48 hours
Result: Apoptotic induction in 2.1% of the 2F7 cells above background after 2 hours of treatment, increasing through 48 hours of treatment.

Cell Cycle Analysis[2]

Cell Line: BCBL-1 Cells
Concentration: 15 μM (the IC50)
Incubation Time: 2-48 hours
Result: Inhibits cell cycle progression in 2F7 and BCBL-1 cells.

Western Blot Analysis[2]

Cell Line: BCBL-1 and 2F7 cell lines
Concentration: 15 or 14 μM (at the IC50 respectively)
Incubation Time: 2-48 hours
Result: The expression of phospho-PKCβ in BCBL-1 and 2F7 cells reduced.
Molecular Weight

411.46

Formula

C₂₄H₂₁N₅O₂

CAS No.

257879-35-9

SMILES

O=C(C(C1=CN(CCCN2C=CN=C2)C3=C1C=CC=C3)=C4NC5=CC=CC=C5)NC4=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (607.59 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4304 mL 12.1518 mL 24.3037 mL
5 mM 0.4861 mL 2.4304 mL 4.8607 mL
10 mM 0.2430 mL 1.2152 mL 2.4304 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 6.25 mg/mL (15.19 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 6.25 mg/mL (15.19 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

PKCβ inhibitor 1PKCβ inhibitor1PKCβ inhibitor-1PKCApoptosisProtein kinase CATP-competitiveselectivetumor2F7BCBL-1cellproliferationGSK3βmTORS6phosphorylationInhibitorinhibitorinhibit

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PKCβ inhibitor 1
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HY-13335
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