1. Epigenetics
    TGF-beta/Smad
  2. PKC
  3. TPPB

TPPB 

Cat. No.: HY-12359 Purity: 99.81%
Handling Instructions

TPPB is a cell-permeable benzolactam-derived protein kinase C (PKC) activator with a Ki of 11.9 nM.

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

TPPB Chemical Structure

TPPB Chemical Structure

CAS No. : 497259-23-1

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 861 Get quote
1 mg USD 156 In-stock
Estimated Time of Arrival: December 31
5 mg USD 480 Get quote
10 mg USD 800 Get quote
25 mg USD 1700 Get quote
50 mg USD 2800 Get quote
100 mg USD 4300 Get quote
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

TPPB is a cell-permeable benzolactam-derived protein kinase C (PKC) activator with a Ki of 11.9 nM.

IC50 & Target[1]

PKC

11.9 nM (Ki)

In Vitro

By use of a cell line derived from an Alzheimer’s disease patient, significant enhancement of sAPPα secretion is achieved at 1 μM concentration for TPPB (Compound 5e)[1]. TPPB has a role against Aβ25-35-induced neurotoxicity in PC12 cells. TPPB at concentration of 1 μM could antagonize Aβ25-35 induced cell damage. TPPB could increase the phosphorylation of Akt, PKC, MARCKS and MAPK, which are inhibited by Aβ25-35 treatment. TPPB inhibits the activation of caspase-3 induced by Aβ25-35[2].

In Vivo

TPPB is evaluated for induction of hyperplasia after topical application to the shaved backs of outbred Sencar mice and shows a modest response at 300 μg[1].

Molecular Weight

501.54

Formula

C₂₇H₃₀F₃N₃O₃

CAS No.

497259-23-1

SMILES

O=C(NC1=CC=C(N(C)[[email protected]@H](C(C)C)C(N[[email protected]](CO)C2)=O)C2=C1)/C=C/C=C/C3=CC=C(C(F)(F)F)C=C3

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 : 135 mg/mL (269.17 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9939 mL 9.9693 mL 19.9386 mL
5 mM 0.3988 mL 1.9939 mL 3.9877 mL
10 mM 0.1994 mL 0.9969 mL 1.9939 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: ≥ 2.25 mg/mL (4.49 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.25 mg/mL (4.49 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

24 h after plating 2×104 pheochromocytoma PC12 cells in each well of a 96 well plate, cells are incubated with TPPB at a series of concentration (0.1, 0.5, 1, 5, 10, 20 μM). Twelve to 24 h later, the original media is replaced with media containing MTT at a final concentration of 0.5 g/L for 4 h. Cell viability is evaluated with MTT assays[2].

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

Animal Administration
[1]

Mice: Mice are 7 weeks old at the beginning of the treatments and are in the resting phase of the hair cycle. TPPB is applied once or else are applied twice weekly for a total of four applications. Two animals are treated at each dose of compound, and 72 h after the last application, the animals are euthanized. Two portions of treated skin are removed from each animal, fixed in neutral buffered formalin, and stained with hematoxylin and eosin for histological analysis[1].

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

References

Purity: 99.81%

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Keywords:

TPPBPKCProtein kinase CInhibitorinhibitorinhibit

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