1. Stem Cell/Wnt
    Autophagy
  2. Gli
    Autophagy

GANT 61 (Synonyms: NSC 136476)

Cat. No.: HY-13901 Purity: 99.87%
Handling Instructions

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 (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
50 mg USD 360 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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    GANT 61 purchased from MCE. Usage Cited in: Oncotarget. 2015 Nov 3;6(34):36700-12.

    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.

    GANT 61 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 28;420:195-207.

    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 MCE. Usage Cited in: Cancer Sci. 2017 May;108(5):918-930.

    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 MCE. Usage Cited in: ACS Appl Mater Interfaces. 2017 Dec 13;9(49):42544-42555.

    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 MCE. Usage Cited in: Life Sci. 2017 Dec 15;191:82-89.

    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 MCE. Usage Cited in: Cancer Lett. 2017 Jan 28;385:128-136.

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

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

    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 MCE. Usage Cited in: Front Pharmacol. 2018 Jun 26;9:674.

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

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

    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 MCE. 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 MCE. Usage Cited in: University of Colorado. 8.19.2016.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    Gli1/2[1]

    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].

    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].

    Solvent & Solubility
    In Vitro: 

    DMSO : 17.6 mg/mL (40.97 mM; Need ultrasonic and warming)

    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
    10 mM 0.2328 mL 1.1639 mL 2.3277 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      GANT 61 is resuspended in 4:1 corn oil: 100% Ethanol mixture[4].

    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
    Molecular Weight

    429.60

    Formula

    C₂₇H₃₅N₅

    CAS No.

    500579-04-4

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.87%

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    Product Name:
    GANT 61
    Cat. No.:
    HY-13901
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    Cat. No.: HY-13901