2. GPCR/G Protein Immunology/Inflammation Autophagy
  3. CXCR Autophagy
  4. UNBS5162

UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.

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

UNBS5162 Chemical Structure

UNBS5162 Chemical Structure

CAS No. : 956590-23-1

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10 mM * 1 mL in DMSO
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Based on 13 publication(s) in Google Scholar

UNBS5162 Related Antibodies

Top Publications Citing Use of Products

    UNBS5162 purchased from MedChemExpress. Usage Cited in: Thorac Cancer. 2018 Jan;9(1):105-111.  [Abstract]

    Apoptosis is induced by UNBS5162 treatment in human A549 non-small cell lung cancer (NSCLC) cells. Western blot analysis of apoptosis protein expression in human A549 NSCLC cells.

    UNBS5162 purchased from MedChemExpress. Usage Cited in: Exp Ther Med. 2018 Nov;16(5):3921-3928.  [Abstract]

    The effect of UNBS5162 on MDA-MB-231 cell apoptosis detected using western blot. Western blot assay is utilized to determine BCL-2, BAX and active caspase-3 protein expression levels in MDA MB 231 cells extracts.

    UNBS5162 purchased from MedChemExpress. Usage Cited in: Med Sci (Paris). 2018 Oct;34 Focus issue F1:99-104.  [Abstract]

    Western-blot analysis of proteins involved in the PI3K/Akt signaling pathway in HCT116 cells cultured in presence of UNBS5162 or DMSO (NC).

    UNBS5162 purchased from MedChemExpress. Usage Cited in: Med Sci (Paris). 2018 Oct;34 Focus issue F1:99-104.  [Abstract]

    The expression levels of Bcl-2, Bax and active caspase-3 proteins are measured using Western-blot analyses after incubation with UNBS5162 or DMSO for 24 h.

    UNBS5162 purchased from MedChemExpress. Usage Cited in: Onco Targets Ther. 2017 Nov 6;10:5303-5309.  [Abstract]

    UNBS5162 inhibits proliferation of human retinoblastoma cells through the Akt–mTOR pathway. Following Western blot, expression of Akt-pathway and key proliferation-related genes- those for p-Akt, p-mTOR, p70, and cyclin D1-is found to be downregulated significantly in the UNBS5162-treated group compared with the negative-control (NC) group in WERIRb1 cells.

    UNBS5162 purchased from MedChemExpress. Usage Cited in: Onco Targets Ther. 2017 Nov 6;10:5303-5309.  [Abstract]

    UNBS5162 inhibits proliferation of human retinoblastoma cells through the Akt–mTOR pathway. Following Western blot, expression of Akt-pathway and key proliferation-related genes- those for p-Akt, p-mTOR, p70, and cyclin D1-is found to be downregulated significantly in the UNBS5162-treated group compared with the negative-control (NC) group in Y79 cells.

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    Description

    UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.

    IC50 & Target[1]

    CXCL

     

    In Vitro

    UNBS5162 is a pan-antagonist of CXCL chemokine expression and exhibits weak antiproliferative activity against human cancer cell lines with mean IC50 of 17.9 µM. UNBS5162 markedly impairs PC-3 tumor cell growth kinetics, without inducing senescence, whereas the reverse feature is observed with respect to DU-145 cells[1]. UNBS5162 is cytotoxic to a range of human cancer cell lines including glioblastoma (Hs683 and U373MG), colorectal (HCT-15 and LoVo), non-small-cell lung (A549) and breast (MCF-7), with IC50s of 0.5-5 µM. UNBS5162 also markedly increases the levels of expression of LC3-I and LC3-II in human cancer cells. UNBS5162 displays no anti-topoisomerase II activity. Moreover, UNBS5162 induces cancer cell death through lysosomal membrane permeabilization (LMP) in PC3 prostate cancer cells but not in U373 glioblastoma cells, with this LMP process occurring as an UNBS5162-induced decrease in Hsp70 expression[2]. UNBS5162 inhibits the proliferation of esophageal cancer squamous cells via the PI3K/AKT signaling pathway. UNBS5162 downregulates the protein expression of proteins associated with the PI3K/AKT signaling pathway, including the levels of phosphorylated (p)-AKT, p-mechanistic target of rapamycin kinase, ribosomal protein S6 kinase β1 and cyclin D1[3].

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

    UNBS5162 Related Antibodies
    In Vivo

    UNBS5162 (20 mg/kg, i.v.) increases the therapeutic benefits of taxol in vivo in the orthotopic human PC-3 prostate cancer model[1].

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

    326.35

    Formula

    C17H18N4O3
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(N)NC1=CC2=CC=CC(C(N(CCN(C)C)C3=O)=O)=C2C3=C1
    Shipping

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

    DMSO : 21.5 mg/mL (65.88 mM; Need ultrasonic and warming; 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 3.0642 mL 15.3210 mL 30.6419 mL
    5 mM 0.6128 mL 3.0642 mL 6.1284 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    In Vivo Dissolution Calculator
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    Purity & Documentation
    References
    Animal Administration
    [1]

    Mice[1]
    Orthotopic xenografts are obtained by injecting 2.5 × 106 human PC-3 or DU-145 cells into the prostate of 6-week-old male nu/nu mice (n = 9 animals per treatment group). All grafts are performed under anesthesia [saline/Rompun/Imalgene; 5:1:1 by volume]. The end point in these orthotopic experiments is the survival period of the tumor-bearing mice after the administration of UNBS3157, UNBS5162, or reference anticancer agents (taxol, mitoxantrone, and amonafide). However, for ethical reasons, animals are killed when 20% of body weight have been lost compared to that determined at the time of tumor grafting. All animals are weighed three times a week. Autopsies and histologic diagnoses are performed on each mouse to confirm the presence of tumor development; 100% is achieved. In the case of UNBS5162 experiments in the PC-3 model, after the sacrifice of animals, tumors are removed from both drug-treated [10 mg/kg, intravenous (i.v.)] and vehicle-treated mice, fixed in buffered formalin, embedded in paraffin, and 5-µm-thick sections taken. These histologic slides are then stained with hematoxylin and eosin for blood vessel counts[1].

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.0642 mL 15.3210 mL 30.6419 mL 76.6049 mL
    5 mM 0.6128 mL 3.0642 mL 6.1284 mL 15.3210 mL
    10 mM 0.3064 mL 1.5321 mL 3.0642 mL 7.6605 mL
    15 mM 0.2043 mL 1.0214 mL 2.0428 mL 5.1070 mL
    20 mM 0.1532 mL 0.7660 mL 1.5321 mL 3.8302 mL
    25 mM 0.1226 mL 0.6128 mL 1.2257 mL 3.0642 mL
    30 mM 0.1021 mL 0.5107 mL 1.0214 mL 2.5535 mL
    40 mM 0.0766 mL 0.3830 mL 0.7660 mL 1.9151 mL
    50 mM 0.0613 mL 0.3064 mL 0.6128 mL 1.5321 mL
    60 mM 0.0511 mL 0.2553 mL 0.5107 mL 1.2767 mL
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    UNBS5162 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:

    UNBS5162956590-23-1UNBS 5162UNBS-5162CXCRAutophagyCXC chemokine receptorsC-X-C motif chemokine receptorsInhibitorinhibitorinhibit

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