2. Stem Cell/Wnt Autophagy
  3. Gli Autophagy
  4. GANT 61

GANT 61  (Synonyms: NSC 136476)

Cat. No.: HY-13901 Purity: ≥98.0%
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GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.

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

GANT 61 Chemical Structure

GANT 61 Chemical Structure

CAS No. : 500579-04-4

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 106 In-stock
50 mg USD 396 In-stock
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Customer Review

Based on 65 publication(s) in Google Scholar

GANT 61 Related Antibodies

Top Publications Citing Use of Products

54 Publications Citing Use of MCE GANT 61

WB
IF
Proliferation Assay

    GANT 61 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Apr 28;420:195-207.  [Abstract]

    Shh-Light 2 cells are transfected with Gli1 or Gli2 plasmids and the expression of proteins are analyzed by Western blot. Positive control JQ1, CBC and CBD inhibit Gli1 and Gli2 overexpression induced Gli luciferase activity, GDC-0499 and GANT61 have no effects.

    GANT 61 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 26;9:674.  [Abstract]

    Cyclopamine and GANT61 decrease the level of Gli1 as evidenced by western blot.

    GANT 61 purchased from MedChemExpress. Usage Cited in: Cancer Med. 2018 Nov;7(11):5704-5715.  [Abstract]

    The Hh signaling pathway is involved in DHA induced inhibition of cell proliferation. A and B, CCK8 assay of SKOV3 and SKOV3-IP cells is conducted following treatment with purmorphamine, DHA or a combination of DHA and purmorphamine for 48 h. C and D, SKOV3 and SKOV3‐IP cells are treated with GANT61, DHA, or a combination of DHA and GATN61 for 48 h, while controls are treated with DMSO. CCK8 assay is used to analyze cell viability of SKOV3 and SKOV3-IP cells.

    GANT 61 purchased from MedChemExpress. Usage Cited in: Chinese Pharmacological Bulletin. 2018, 34(9): 1235-1242.

    Expression of Gli1/2 (A) and DNA damage proteins (B) at OGD 6 h detected by Western blot.

    GANT 61 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Jan 28;385:128-136.  [Abstract]

    GANT61 or SHH siRNA treatment alone moderately increases LC3-II, and LC3-II increased in cells co-treated with R51211 and GANT61 or SHH siRNA.

    GANT 61 purchased from MedChemExpress. Usage Cited in: ACS Appl Mater Interfaces. 2017 Dec 13;9(49):42544-42555.  [Abstract]

    ATG101 cross-talk with the hedgehog pathway modulates hypoxia-induced HPAEC cell proliferation and apoptosis. Effects of ssATG101-TNP on the hedgehog pathway. HPAECs are pretreated with ssATG101-TNP and GANT61; then, they are under hypoxia for 24 h.

    GANT 61 purchased from MedChemExpress. Usage Cited in: Life Sci. 2017 Dec 15;191:82-89.  [Abstract]

    ORS cells are exposed to 3% oxygen for 48 h in presence or absence of Shh pathway inhibitor cyclopamine (5 μM) or GANT61 (10 μM). Immunofluorescence assay using anti-PCNA antibody is performed to detect the proliferative ORS cells (red). Cell nuclei are counterstained with DAPI (blue).

    GANT 61 purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2017 May;108(5):918-930.  [Abstract]

    Effects of E2 and GANT61 on the protein expression levels of GLI1 and GLI2 in MCF-7 cells. The expression levels are measured with a western blotting as described in the Materials and Methods.

    GANT 61 purchased from MedChemExpress. Usage Cited in: Breast Cancer. 2017 Sep;24(5):683-693.  [Abstract]

    Effects of GANT61 (0-20μM) on the expression levels of survivin in MDA-MB-231 cells. The cells are treated with the indicated concentrations of GANT61 for two days. The expression levels are tested using western blotting. The deduced molecular weight of surviving is approximately 16 kDa.

    GANT 61 purchased from MedChemExpress. Usage Cited in: Birla Institute of Technology, University of Colorado. 2016 Aug.

    Western blot analyses of whole cell lysates (WCLs) collected from MCF7-Ctrl cells cultured in MCF7-Ctrl and Six1 CM for 48 hrs treated with GANT61 or vehicle.

    GANT 61 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Nov 3;6(34):36700-12.  [Abstract]

    BE2-M17 NB cells are incubated with GANT-61 (0–40 μM) for 3 days. The cell viability is monitored using an MTS assay. The expression levels of N-myc and INSM1 in the cells treated with 20 μM of GANT-61 is determined by Western blot analysis. Actin is used as a loading control.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.

    IC50 & Target

    Gli1/2[1]
    Cellular Effect
    Cell Line Type Value Description References
    HeLa IC50
    6.83 μM
    Compound: GANT61
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
    		[PMID: 29624387]
    IMR-32 GI50
    5.82 μM
    Compound: 32, GANT-61
    Cytotoxicity against human IMR32 cells after 72 hrs by fluorometric microculture cytotoxicity assay
    Cytotoxicity against human IMR32 cells after 72 hrs by fluorometric microculture cytotoxicity assay
    		10.1039/C3MD00334E
    NIH3T3 EC50
    5 μM
    Compound: 4; GANT-61
    Inhibition of Hh signaling pathway in Shh-LIGHT2 incorporated mouse NIH 3T3 cells assessed as downregulation of Gli1 gene expression by luciferase reporter gene assay
    Inhibition of Hh signaling pathway in Shh-LIGHT2 incorporated mouse NIH 3T3 cells assessed as downregulation of Gli1 gene expression by luciferase reporter gene assay
    		[PMID: 26976215]
    Shh Light II IC50
    5 μM
    Compound: 128, GANT61
    Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay
    Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay
    		[PMID: 19309080]
    SH-SY5Y GI50
    5.82 μM
    Compound: 32, GANT-61
    Cytotoxicity against human SH-SY5Y cells after 72 hrs by fluorometric microculture cytotoxicity assay
    Cytotoxicity against human SH-SY5Y cells after 72 hrs by fluorometric microculture cytotoxicity assay
    		10.1039/C3MD00334E
    SK-N-AS GI50
    5.82 μM
    Compound: 32, GANT-61
    Cytotoxicity against human SK-N-AS cells after 72 hrs by fluorometric microculture cytotoxicity assay
    Cytotoxicity against human SK-N-AS cells after 72 hrs by fluorometric microculture cytotoxicity assay
    		10.1039/C3MD00334E
    SK-N-DZ GI50
    5.82 μM
    Compound: 32, GANT-61
    Cytotoxicity against human SK-N-DZ cells after 72 hrs by fluorometric microculture cytotoxicity assay
    Cytotoxicity against human SK-N-DZ cells after 72 hrs by fluorometric microculture cytotoxicity assay
    		10.1039/C3MD00334E
    SK-N-FI GI50
    5.82 μM
    Compound: 32, GANT-61
    Cytotoxicity against human SK-N-FI cells after 72 hrs by fluorometric microculture cytotoxicity assay
    Cytotoxicity against human SK-N-FI cells after 72 hrs by fluorometric microculture cytotoxicity assay
    		10.1039/C3MD00334E
    SK-N-SH GI50
    5.82 μM
    Compound: 32, GANT-61
    Cytotoxicity against human SK-N-SH cells after 72 hrs by fluorometric microculture cytotoxicity assay
    Cytotoxicity against human SK-N-SH cells after 72 hrs by fluorometric microculture cytotoxicity assay
    		10.1039/C3MD00334E
    In Vitro

    GANT61 (20 μM) induces greater cell death than targeting Smo (cyclopamine). GANT61 (0, 5, 10, 20 μM) inhibits clonogenic survival of human colon carcinoma cell lines. GANT61 (20 μM, 0-72 hr) down-regulates Gli1 and Gli2 expression in HT29 cells. GANT61 (0, 10 μM or 20 μM) differentially regulates genes involved in the balance between cell death and cell survival[1].
    GANT-61 inhibits cell viability and induces apoptosis in pancreatic CSCs. GANT-61 inhibits expression of downstream targets of Shh pathway, decreases Gli-DNA interaction, Gli transcriptional activity and Gli nuclear translocation in pancreatic CSCs. GANT-61 differentially regulates genes involved in cell survival, cell death and pluripotency. GANT-61 inhibits motility, invasion and migration of CSCs[2].
    GANT61 sensitivity positively correlates to GLI1 and negatively to MYCN expression in the neuroblastoma cell lines tested. GANT61 downregulates GLI1, c-MYC, MYCN and Cyclin D1 expression and induces apoptosis of neuroblastoma cells[3].

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

    GANT 61 Related Antibodies
    In Vivo

    GANT-61 (40 mg/kg, i.p., three days per week) inhibits CSC tumor growth in NOD/SCID IL2Rγ null mice[2].
    GANT61 (50 mg/kg, p.o.) enhances the effects of chemotherapeutic drugs used in the treatment of neuroblastoma in an additive or synergistic manner and reduces the growth of established neuroblastoma xenografts in nude mice[3].

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

    429.60

    Formula

    C27H35N5
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    CN(C)C1=CC=CC=C1CN2C(C3=CC=NC=C3)N(CC4=CC=CC=C4N(C)C)CCC2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    Ethanol : 66.67 mg/mL (155.19 mM; Need ultrasonic)

    DMSO : 25 mg/mL (58.19 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 2.3277 mL 11.6387 mL 23.2775 mL
    5 mM 0.4655 mL 2.3277 mL 4.6555 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (11.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 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% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: 5 mg/mL (11.64 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    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: ≥98.0%

    SDS (393 KB)

    COA (257 KB) HNMR (270 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Cells (1.5×104) are incubated with 0, 1, 5 and 10 μM of GANT-61 in 250 μL of culture medium in 96-well plate for 48 and 72 h. Cell viability is determined by the XTT assay. In brief, a freshly prepared XTT-PMS labeling mixture (50 μL) is added to the cell culture. The absorbance is measured at 450 nm with λ correction at 650 nm. The cell viability is expressed as ΔOD (OD450 − OD650). The apoptosis is determined by FACS analysis of propidium iodide (PI)-stained cells. In brief, cells are trypsinized, washed with PBS and resuspended in 200 μL PBS with 10 μL RNAase (10 mg/mL) and incubated at 37°C for 30 min. After incubation, 50 μL PI solution is added and cells are analyzed for apoptosis using a flow cytometry.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Humanized NOD/SCID/IL2Rgammanull mice are used for the assay. Before CSC’s injection, mice are humanized with tail vein injection of human normal CD34+ peripheral blood stem/progenitor cells. CD34+peripheral blood stem/progenitor cells (500 cells/mouse, 50-75 μL volume) are injected through tail vein. After 3 days, human pancreatic CSCs (1×103 cells mixed with Matrigel, Becton Dickinson, Bedford, MA, in 75 μL total volume, 50:50 ratio) are injected subcutaneously into the flanks of NOD/SCID IL2Rγnull mice (4–6 weeks old). After two weeks of CSC implantation, mice (10 mice per group) are treated with GANT-61(0 and 40 mg/kg body weight) ip three times per week for 6 weeks. At the end of the experiment, mice are euthanized, and tumors are isolated for biochemical analysis.

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

    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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / Ethanol 1 mM 2.3277 mL 11.6387 mL 23.2775 mL 58.1937 mL
    5 mM 0.4655 mL 2.3277 mL 4.6555 mL 11.6387 mL
    10 mM 0.2328 mL 1.1639 mL 2.3277 mL 5.8194 mL
    15 mM 0.1552 mL 0.7759 mL 1.5518 mL 3.8796 mL
    20 mM 0.1164 mL 0.5819 mL 1.1639 mL 2.9097 mL
    25 mM 0.0931 mL 0.4655 mL 0.9311 mL 2.3277 mL
    30 mM 0.0776 mL 0.3880 mL 0.7759 mL 1.9398 mL
    40 mM 0.0582 mL 0.2910 mL 0.5819 mL 1.4548 mL
    50 mM 0.0466 mL 0.2328 mL 0.4655 mL 1.1639 mL
    Ethanol 60 mM 0.0388 mL 0.1940 mL 0.3880 mL 0.9699 mL
    80 mM 0.0291 mL 0.1455 mL 0.2910 mL 0.7274 mL
    100 mM 0.0233 mL 0.1164 mL 0.2328 mL 0.5819 mL
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    GANT 61 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.

    Keywords:

    GANT 61500579-04-4NSC 136476GANT61GANT-61NSC136476NSC-136476GliAutophagyInhibitorinhibitorinhibit

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