1. Epigenetics
    TGF-beta/Smad
  2. PKC
  3. LXS196

LXS196 

Cat. No.: HY-101569 Purity: 99.25%
Handling Instructions

LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. It can be used for the treatment of uveal melanoma.

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

LXS196 Chemical Structure

LXS196 Chemical Structure

CAS No. : 1874276-76-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 161 In-stock
Estimated Time of Arrival: December 31
2 mg USD 80 In-stock
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5 mg USD 155 In-stock
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10 mg USD 235 In-stock
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25 mg USD 409 In-stock
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50 mg USD 610 In-stock
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100 mg USD 920 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. It can be used for the treatment of uveal melanoma[1][2].

IC50 & Target[2]

PKCα

1.9 nM (IC50)

PKCθ

0.4 nM (IC50)

GSK3β

3.1 μM (IC50)

In Vitro

Upon oral administration, protein kinase C inhibitor LXS196 binds to and inhibits PKC, which prevents the activation of PKC-mediated signaling pathways. This may lead to the induction of cell cycle arrest and apoptosis in susceptible tumor cells. PKC, a serine/threonine protein kinase overexpressed in certain types of cancer cells, is involved in tumor cell differentiation, proliferation, invasion and survival[1].

In Vivo

LXS196 (compound 9) (15, 30, 75, 150 mg/kg, P.O., mice) shows improved efficacy (regression) in a 92.1 GNAQ uveal melanoma xenograft model in a dose-dependently manner[2].

Animal Model: Mice implanted with 92.1 GNAQ mutant uveal melanoma cells[2].
Dosage: 15, 30, 75, 150 mg/kg
Administration: P.O. (bid) for 35 days
Result: Dose-dependently suppressed the tumor growth.
Clinical Trial
Molecular Weight

472.47

Formula

C₂₂H₂₃F₃N₈O

CAS No.

1874276-76-2

SMILES

NC1=C(C(NC2=C(N3CCC(C)(N)CC3)C=CC=N2)=O)N=C(C4=NC=CC=C4C(F)(F)F)C=N1

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 : ≥ 100 mg/mL (211.65 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1165 mL 10.5827 mL 21.1654 mL
5 mM 0.4233 mL 2.1165 mL 4.2331 mL
10 mM 0.2117 mL 1.0583 mL 2.1165 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: ≥ 2.5 mg/mL (5.29 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.29 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.29 mM); Clear solution

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

LXS196LXS 196LXS-196PKCProtein kinase CInhibitorinhibitorinhibit

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LXS196
Cat. No.:
HY-101569
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