Laduviglusib (Synonyms: CHIR-99021; CT99021)

Name: Laduviglusib
Brand: MedChemExpress
SKU: HY-10182
Rating: 5.0 (174 reviews)

Cat. No.: HY-10182 Purity: 99.71%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

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

Laduviglusib Chemical Structure

CAS No. : 252917-06-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 79	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 79	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 108	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 324	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 516	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 880	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Customer Review

Based on 174 publication(s) in Google Scholar

Other Forms of Laduviglusib:

168 Publications Citing Use of MCE Laduviglusib

RT-PCR

: Laduviglusib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2020 Apr 2;524(2):280-287. [Abstract]; Western blot analysis of Tcf7l1 protein levels in mESCs pre-treated with the indicative different small molecules for 1 h and then treated with CHIR for 24 h.

: Laduviglusib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2020 Apr 2;524(2):280-287. [Abstract]; Western blot analysis of Tcf7l1 protein levels in mESCs pre-treated with D4476 or DMAT and then treated with CHIR or PD03 for 24 h.

: Laduviglusib purchased from MedChemExpress. Usage Cited in: Chemosphere. 2018 Oct 23;216:372-378. [Abstract]; AhR mediates EOM-inhibited cardiac differentiation by downregulating β-catenin expression in P19 cells. mRNA expression changes of β-catenin by Q-PCR. The concentrations of CH (CH223191, AhR antagonist) and CHIR (CHIR99021, Wnt activator) are 0.25 and 0.5 μM respectively.

: Laduviglusib purchased from MedChemExpress. Usage Cited in: Chemosphere. 2018 Oct 23;216:372-378. [Abstract]; AhR mediates EOM-inhibited cardiac differentiation by downregulating β-catenin expression in P19 cells. Percentage of cTnT positive cells at differentiation day 14. The concentrations of CH (CH223191, AhR antagonist) and CHIR (CHIR99021, Wnt activator) are 0.25 and 0.5 μM respectively.

: Laduviglusib purchased from MedChemExpress. Usage Cited in: Chemosphere. 2018 Oct 23;216:372-378. [Abstract]; AhR mediates EOM-inhibited cardiac differentiation by downregulating β-catenin expression in P19 cells. Percentage of cTnT positive cells at differentiation day 14. The concentrations of CH (CH223191, AhR antagonist) and CHIR (CHIR99021, Wnt activator) are 0.25 and 0.5 μM respectively.

: Laduviglusib purchased from MedChemExpress. Usage Cited in: Toxicology. 2016 May 20;355-356:31-38. [Abstract]; Western analysis of β-catenin protein level in zebrafish embryos exposed to EOM in the presence or absence of CH/CHIR (n = 3). Different letters indicate significant differences. Moreover, both CH and CHIR attenuate the EOM-induced changes in the protein level of b-catenin and in EROD activity.

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GSK-3 GSK-3α GSK-3β

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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.

Molecular Weight

465.34

Formula

C₂₂H₁₈Cl₂N₈

CAS No.

252917-06-9

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

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
10 mM	0.2149 mL	1.0745 mL	2.1490 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.76%

Select Batch:

Data Sheet (279 KB) SDS (480 KB)

COA (248 KB) HNMR (194 KB) LCMS (343 KB) Elemental Analysis Report (105 KB)

Handling Instructions (2659 KB)

References

[1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95. [Content Brief]

[2]. Naujok O, et al. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors.BMC Res Notes. 2014 Apr 29;7:273. [Content Brief]

[3]. Ye S, et al. Pleiotropy of glycogen synthase kinase-3 inhibition by CHIR99021 promotes self-renewal of embryonic stem cells from refractory mouse strains. PLoS One. 2012;7(4):e35892. [Content Brief]

[4]. Bennett CN, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998-1004. [Content Brief]

[5]. Wang X, et al. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10;5:8566. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1490 mL	10.7448 mL	21.4897 mL	53.7242 mL
	5 mM	0.4298 mL	2.1490 mL	4.2979 mL	10.7448 mL
	10 mM	0.2149 mL	1.0745 mL	2.1490 mL	5.3724 mL
	15 mM	0.1433 mL	0.7163 mL	1.4326 mL	3.5816 mL
	20 mM	0.1074 mL	0.5372 mL	1.0745 mL	2.6862 mL
	25 mM	0.0860 mL	0.4298 mL	0.8596 mL	2.1490 mL
	30 mM	0.0716 mL	0.3582 mL	0.7163 mL	1.7908 mL

Laduviglusib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Laduviglusib (Synonyms: CHIR-99021; CT99021)

Customer Review

Other Forms of Laduviglusib:

168 Publications Citing Use of MCE Laduviglusib

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•Related Small Molecules:

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View All GSK-3 Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

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Complete Stock Solution Preparation Table

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Laduviglusib (Synonyms: CHIR-99021; CT99021)

Customer Review

Other Forms of Laduviglusib:

Laduviglusib Related Antibodies

168 Publications Citing Use of MCE Laduviglusib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All GSK-3 Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Laduviglusib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Laduviglusib Related Classifications

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Your Recently Viewed Products:

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