2. PI3K/Akt/mTOR
    Stem Cell/Wnt
    Autophagy
  3. GSK-3
    Wnt
    β-catenin
    Autophagy
  4. Laduviglusib monohydrochloride

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

Cat. No.: HY-10182A Purity: 99.93%
COA Handling Instructions

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

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

Laduviglusib monohydrochloride Chemical Structure

Laduviglusib monohydrochloride Chemical Structure

CAS No. : 1797989-42-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 97 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 97 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 88 In-stock
Estimated Time of Arrival: December 31
10 mg USD 121 In-stock
Estimated Time of Arrival: December 31
50 mg USD 308 In-stock
Estimated Time of Arrival: December 31
100 mg USD 605 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 117 publication(s) in Google Scholar

Other Forms of Laduviglusib monohydrochloride:

Top Publications Citing Use of Products

111 Publications Citing Use of MCE Laduviglusib monohydrochloride

WB
RT-PCR
IF

    Laduviglusib monohydrochloride purchased from MCE. 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 monohydrochloride purchased from MCE. 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 monohydrochloride purchased from MCE. 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 monohydrochloride purchased from MCE. 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 monohydrochloride purchased from MCE. 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 monohydrochloride purchased from MCE. 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

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

    IC50 & Target[1] [1] [1]

    GSK-3β

    6.7 nM (IC50)

    GSK-3α

    10 nM (IC50)

    cdc2

    8800 nM (IC50)

    In Vitro

    Laduviglusib monohydrochloride inhibits human GSK-3β with Ki values of 9.8 nM[1]. Laduviglusib monohydrochloride is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites. In vitro kinase assays reveal that Laduviglusib monohydrochloride specifically inhibits GSK3β (IC50=~5 nM) and GSK3α (IC50=~10 nM), with little effect on other kinases[4]. In the presence of Laduviglusib monohydrochloride 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 monohydrochloride with an IC50 of 4.9 μM[2].

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

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    501.80

    Appearance

    Solid

    Formula

    C22H19Cl3N8
    CAS No.
    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
    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 : 60 mg/mL (119.57 mM; Need ultrasonic)

    H2O : 7.14 mg/mL (14.23 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9928 mL 9.9641 mL 19.9283 mL
    5 mM 0.3986 mL 1.9928 mL 3.9857 mL
    10 mM 0.1993 mL 0.9964 mL 1.9928 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  PBS

      Solubility: 5 mg/mL (9.96 mM); Clear solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 3 mg/mL (5.98 mM); Clear solution

    • 3.

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

      Solubility: ≥ 3 mg/mL (5.98 mM); Clear solution

    • 4.

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

      Solubility: ≥ 3 mg/mL (5.98 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.93%

    COA (248 KB) HNMR (223 KB) LCMS (137 KB)

    Handling Instructions (2659 KB)
    References
    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
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    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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    Keywords:

    Laduviglusib monohydrochloride1797989-42-4CHIR-99021 monohydrochlorideCT99021 monohydrochlorideGSK-3Wntβ-cateninAutophagyGlycogen synthase kinase-3Glycogen synthase kinase 3Beta cateninInhibitorinhibitorinhibit

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