Laduviglusib trihydrochloride (Synonyms: CHIR-99021 trihydrochloride; CT99021 trihydrochloride)

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

Cat. No.: HY-10182B Purity: 99.35%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

Laduviglusib trihydrochloride Chemical Structure

CAS No. : 1782235-14-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 133	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 133	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 106	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 172	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 647	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Based on 174 publication(s) in Google Scholar

Other Forms of Laduviglusib trihydrochloride:

168 Publications Citing Use of MCE Laduviglusib trihydrochloride

RT-PCR

: Laduviglusib trihydrochloride 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 trihydrochloride 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 trihydrochloride 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 trihydrochloride 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 trihydrochloride 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 trihydrochloride 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
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

GSK-3β

6.7 nM (IC₅₀)

GSK-3α

10 nM (IC₅₀)

cdc2

8800 nM (IC₅₀)

In Vitro

Laduviglusib trihydrochloride inhibits human GSK-3β with K_i values of 9.8 nM^[1]. Laduviglusib trihydrochloride is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that Laduviglusib trihydrochloride specifically inhibits GSK3β (IC₅₀=~5 nM) and GSK3α (IC₅₀=~10 nM), with little effect on other kinases^[4]. In the presence of Laduviglusib trihydrochloride the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM Laduviglusib trihydrochloride with an IC₅₀ of 4.9 μM^[2].

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

In Vivo

In ZDF rats, a single oral dose of Laduviglusib (16 mg/kg or 48 mg/kg) trihydrochloride rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration^[1]. Laduviglusib (2 mg/kg) trihydrochloride given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). Laduviglusib trihydrochloride treatment significantly blocks crypt apoptosis and accumulation of p-H2AX⁺ cells, and improves crypt regeneration and villus height. Laduviglusib trihydrochloride treatment increases Lgr5⁺ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h^[5].

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

Molecular Weight

574.72

Formula

C₂₂H₂₁Cl₅N₈

CAS No.

1782235-14-6

Appearance

Solid

Color

White to light yellow

SMILES

N#CC1=CC=C(NCCNC2=NC=C(C3=NC=C(C)N3)C(C4=CC=C(Cl)C=C4Cl)=N2)N=C1.[H]Cl.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 32 mg/mL (55.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 19 mg/mL (33.06 mM; Need ultrasonic and warming)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7400 mL	8.6999 mL	17.3998 mL
5 mM	0.3480 mL	1.7400 mL	3.4800 mL
10 mM	0.1740 mL	0.8700 mL	1.7400 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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 (3.62 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.62 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.62 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.35%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (250 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin 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]

Cell Assay ^[3]	The viability of the mouse ES cells is determined after exposure to different concentrations of GSK3 inhibitors for three days using the MTT assay. The decrease of MTT activity is a reliable metabolism-based test for quantifying cell viability; this decrease correlates with the loss of cell viability. 2,000 cells are seeded overnight on gelatine-coated 96-well plates in LIF-containing ES cell medium. On the next day the medium is changed to medium devoid of LIF and with reduced serum and supplemented with 0.1-1 μM BIO, or 1-10 μM SB-216763, CHIR-99021 or CHIR-98014. Basal medium without GSK3 inhibitors or DMSO is used as control. All tested conditions are analyzed in triplicates^[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]^[4]	Rats^[1] Primary hepatocytes from male Sprague Dawley rats that weighed <140 g are prepared and used 1-3 h after isolation. Aliquots of 1×10⁶cells in 1 mL of DMEM/F12 medium plus 0.2% BSA and CHIR-99021(orally at 16 or 48 mg/kg) or controls are incubated in 12-well plates on a low-speed shaker for 30 min at 37°C in a CO₂-enriched atmosphere, collected by centrifugation and lysed by freeze/thaw in buffer A plus 0.01% NP40; the GS assay is again performed. Mice^[4] Mice 6-10 weeks old are used. The PUMA^+/+ and PUMA^-/- littermates on C57BL/6 background (F10) and Lgr5-EGFP (Lgr5-EGFP-IRES-creERT2) mice are subjected to whole body irradiation (TBI), or abdominal irradiation (ABI). Mice are injected intraperitoneally (i.p.) with 2 mg/kg of CHIR99021 4 h before radiation or 1 mg/kg of SB415286 28 h and 4 h before radiation. Mice are sacrificed to collect small intestines for histology analysis and western blotting. All mice are injected i.p. with 100 mg/kg of BrdU before sacrifice. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin 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

H₂O / DMSO	1 mM	1.7400 mL	8.6999 mL	17.3998 mL	43.4994 mL
	5 mM	0.3480 mL	1.7400 mL	3.4800 mL	8.6999 mL
	10 mM	0.1740 mL	0.8700 mL	1.7400 mL	4.3499 mL
	15 mM	0.1160 mL	0.5800 mL	1.1600 mL	2.9000 mL
	20 mM	0.0870 mL	0.4350 mL	0.8700 mL	2.1750 mL
	25 mM	0.0696 mL	0.3480 mL	0.6960 mL	1.7400 mL
	30 mM	0.0580 mL	0.2900 mL	0.5800 mL	1.4500 mL
DMSO	40 mM	0.0435 mL	0.2175 mL	0.4350 mL	1.0875 mL
DMSO	50 mM	0.0348 mL	0.1740 mL	0.3480 mL	0.8700 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Laduviglusib trihydrochloride Related Classifications

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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.

Keywords:

Laduviglusib trihydrochloride1782235-14-6CHIR-99021 trihydrochloride CT99021 trihydrochlorideOrganoidGSK-3Wntβ-cateninAutophagyGlycogen synthase kinase-3Glycogen synthase kinase 3Beta cateninInhibitorinhibitorinhibit

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Laduviglusib trihydrochloride (Synonyms: CHIR-99021 trihydrochloride; CT99021 trihydrochloride)

Customer Review

Other Forms of Laduviglusib trihydrochloride:

Laduviglusib trihydrochloride Related Antibodies

168 Publications Citing Use of MCE Laduviglusib trihydrochloride

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All GSK-3 Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Laduviglusib trihydrochloride Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Laduviglusib trihydrochloride Related Classifications

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