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> Laduviglusib [252917-06-9]

Laduviglusib [252917-06-9]

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Katalog-Nummer HY-10182-5mg

Size : 5mg

Marke : MedChemExpress

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Beschreibung

Laduviglusib (CHIR-99021) is a potent, selective and orally active GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy[1][2][3].

IC50 & Target[1]

GSK-3β

6.7 nM (IC50)

GSK-3α

10 nM (IC50)

cdc2

8800 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
CHO EC50
0.13 μM
Compound: 1
Inhibition of GSK3 in CHO cells expressing insulin receptor assessed as activation of glycogen synthase measured after 30 mins in presence of glucose-6-phosphate by filter paper assay
Inhibition of GSK3 in CHO cells expressing insulin receptor assessed as activation of glycogen synthase measured after 30 mins in presence of glucose-6-phosphate by filter paper assay
[PMID: 31926786]
HepG2 EC50
1.5 μM
Compound: 1, CHIR-99021
Inhibition of GSK3-beta in human HepG2 cells assessed as incorporation of [3H]glucose into glycogen after 3 hrs by liquid scintillation counting
Inhibition of GSK3-beta in human HepG2 cells assessed as incorporation of [3H]glucose into glycogen after 3 hrs by liquid scintillation counting
[PMID: 22261023]
In Vitro

Laduviglusib (1-10 μM, 3 days) reduces the viability of the ES-D3 cells with an IC50 of 4.9 μM[2].
Laduviglusib (5 μM, 48 h) activates the canonical Wnt-pathway in ES-D3 cells and ES-CCE cells[2].
Laduviglusib (3 μM, 4 days) inhibits ES cell differentiation into neural cells[3].
Laduviglusib (1 μM, 2 weeks) inhibits adipogenesis by blocking induction of C/EBPα and PPARγ in 3T3-L1 preadipocytes[4].
Laduviglusib (2.5 μM, 24 h) protects Lgr5+ cells against radiation-induced apoptosis[5].

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

Laduviglusib Related Antibodies

Cell Viability Assay[2]

Cell Line: ES-D3 cells
Concentration: 1-10 μM
Incubation Time: 3 days
Result: Reduced the viability of the ES-D3 cells by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM
In Vivo

Laduviglusib (30 mg/kg, p.o ) rapidly lowers plasma glucose[1].
Laduviglusib (2 mg/kg, i.p.) protects mice against radiation-induced lethal GI injury[5].

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

Animal Model: ZDF rats[1]
Dosage: 30 mg/kg
Administration: Oral administration
Result: Lowered plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration.
Animal Model: WT C57BL/6 mice[5]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Blocked crypt apoptosis and increased Lgr5+ cell survival.
Molekulargewicht

465.34

Formel

C22H18Cl2N8
CAS. Nr.
Appearance

Solid

Color

Off-white to light brown

SMILES

N#CC1=CC=C(N=C1)NCCNC2=NC=C(C(C3=CC=C(Cl)C=C3Cl)=N2)C4=NC=C(N4)C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 16.67 mg/mL (35.82 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 2.1490 mL 10.7448 mL 21.4897 mL
5 mM 0.4298 mL 2.1490 mL 4.2979 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  0.5% CMC-Na/saline water

    Solubility: 5 mg/mL (10.74 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  20% SBE-β-CD in Saline adjusted to pH 4-4.5 with 1 N Acetic

    Solubility: 5 mg/mL (10.74 mM); Clear solution; Need ultrasonic
Reinheit & Dokumentation
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