Reagenzien und Instrumente für die Immunologie Zellbiologie und Molekularbiologie

CHIR-99021 HCl [1797989-42-4]

Drucken

Katalog-Nummer NB-64-12366-500mg

Size : 500mg

Contact local distributor :

Telefonnummer : +1 850 650 7790

Weitere Informationen anfordern

Contact local distributor :

Telefonnummer : +1 850 650 7790

Remove All

CHIR-99021 HCl

(Synonyms: Laduviglusib HCl, CT99021 HCl) Copy Product Info

Synonyms: Laduviglusib HCl, CT99021 HCl

Catalog No. T2310L Copy Product Info

Purity: 98.14%

CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α/β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt/β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].

Cas No. 1797989-42-4

For research use only—not for human use. No sales to individuals. Use as intended only.

Select Batch

Purity:98.14%

Appearance:Oil

Color:Red

Product Introduction

Bioactivity

Description	CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α/β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt/β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].
In vitro	Laduviglusib monohydrochloride is a potent inhibitor of human GSK-3β, demonstrating a K_i value of 9.8 nM. As a small organic molecule, it competitively inhibits GSK3α and GSK3β by binding to their ATP-binding sites. Kinase assay results reveal that Laduviglusib monohydrochloride specifically targets GSK3β (IC 50 =~5 nM) and GSK3α (IC 50 =~10 nM) with minimal impact on other kinases. Studies show that at concentrations of 2.5 μM to 10 μM, Laduviglusib monohydrochloride significantly reduces the viability of ES-D3 cells in a dose-dependent manner, with an IC 50 of 4.9 μM, indicating a substantial reduction in cell viability at these concentrations.
In vivo	In ZDF rats, administering a single oral dose of Laduviglusib monohydrochloride, either 16 mg/kg or 48 mg/kg, swiftly lowers plasma glucose levels, achieving a peak reduction of approximately 150 mg/dl within 3-4 hours post-dose [1]. Additionally, a one-time administration of Laduviglusib (2 mg/kg) monohydrochloride, 4 hours prior to exposure, markedly enhances survival rates following 14.5 Gy abdominal irradiation (ABI). This treatment significantly inhibits crypt cell apoptosis and the buildup of p-H2AX + cells, while fostering crypt regeneration and increasing villus height. Furthermore, Laduviglusib monohydrochloride enhances the survival of Lgr5 + cells by preventing apoptosis and effectively halts the early reduction of Olfm4, Lgr5, and CD44 markers, observable as soon as 4 hours post-treatment [5].
Synonyms	Laduviglusib HCl, CT99021 HCl

Chemical Properties

Molecular Weight	501.8
Formula	C₂₂H₁₉Cl₃N₈
Cas No.	1797989-42-4
Smiles	Cl.N#CC1=CN=C(C=C1)NCCNC=2N=CC(C3=NC=C(N3)C)=C(N2)C=4C=CC(Cl)=CC4Cl
Relative Density.	no data available

Storage & Solubility Information

Storage

Keep away from direct sunlight,Store under nitrogen Pure form: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 60 mg/mL (119.57 mM), Sonication is recommended.

H2O: 6.4 mg/mL (12.75 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (4.98 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9928 mL	9.9641 mL	19.9283 mL	99.6413 mL
5 mM	0.3986 mL	1.9928 mL	3.9857 mL	19.9283 mL
10 mM	0.1993 mL	0.9964 mL	1.9928 mL	9.9641 mL

DMSO

	1mg	5mg	10mg	50mg
20 mM	0.0996 mL	0.4982 mL	0.9964 mL	4.9821 mL
50 mM	0.0399 mL	0.1993 mL	0.3986 mL	1.9928 mL
100 mM	0.0199 mL	0.0996 mL	0.1993 mL	0.9964 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

GSK-3α/βGSK3CHIR-99021 HCl

Related Tags: CHIR-99021 HCl chemical structure | CHIR-99021 HCl in vivo | CHIR-99021 HCl in vitro | CHIR-99021 HCl formula | CHIR-99021 HCl molecular weight