1. Induced Disease Models Products Apoptosis
  2. Reproductive System Disease Models Bcl-2 Family
  3. Gossypol

Gossypol binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.

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

CAS No. : 303-45-7

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Gossypol:

Top Publications Citing Use of Products

    Gossypol purchased from MedChemExpress. Usage Cited in: Food Chem Toxicol. 2025 Jan:195:115122.

    Representative images of cumulus expansion in Gossypol (0, 10, 20, 40 μM) -exposed oocytes after 44 h culture in vitro maturation.

    Gossypol purchased from MedChemExpress. Usage Cited in: Food Chem Toxicol. 2025 Jan:195:115122.

    (A) Illustrative images of ROS staining of Gossypol (0, 10, 20, 40 μM)-exposed oocytes. (B) Fluorescence intensity of ROS in control and gossypol treatment groups.

    Gossypol purchased from MedChemExpress. Usage Cited in: Food Chem Toxicol. 2025 Jan:195:115122.

    Expression of oxidative stress-related genes (CAT, GSH-Px, SOD1, and SOD2) in control and Gossypol (0, 10, 20, 40 μM) treatment groups in porcine oocytes.

    Gossypol purchased from MedChemExpress. Usage Cited in: Food Chem Toxicol. 2025 Jan:195:115122.

    Illustrative images of mitochondrial membrane potential (MMP) in Gossypol (0, 10, 20, 40 μM) -exposed oocytes.

    Gossypol purchased from MedChemExpress. Usage Cited in: Food Chem Toxicol. 2025 Jan:195:115122.

    Expression of PINK1/Parkin-mediated mitophagy related proteins (PINK1, Parkin and P62) of Gossypol (20 μM)-exposed oocytes treated with melatonin. Statistical analysis of the expressions of PINK1/Parkin-mediated mitophagy related proteins in control, gossypol treatment and gossypol-melatonin co-treatment groups.

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    Description

    Gossypol binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.

    IC50 & Target[1]

    Bcl-xL

    0.5-0.6 μM (Ki)

    Bcl-2

    0.2-0.3 mM (Ki)

    Cellular Effect
    Cell Line Type Value Description References
    4T1 IC50
    18.78 μM
    Compound: 1
    Cytotoxicity against mouse 4T1 cells after 72 hrs by MTT assay
    Cytotoxicity against mouse 4T1 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    4T1 IC50
    21.53 μM
    Compound: 2
    Cytotoxicity against mouse 4T1 cells after 72 hrs by MTT assay
    Cytotoxicity against mouse 4T1 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    A549 IC50
    1.32 μM
    Compound: 1
    Cytotoxicity against human A549 cells after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    A549 IC50
    33.08 μM
    Compound: 2
    Cytotoxicity against human A549 cells after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    B16-F10 IC50
    17.97 μM
    Compound: 2
    Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay
    Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    B16-F10 IC50
    5.54 μM
    Compound: 1
    Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay
    Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    B16-F10 IC50
    5.56 μg/mL
    Compound: (R)-Gossypol
    Antiproliferative activity against mouse B16/F10 cells after 48 hrs by MTT assay
    Antiproliferative activity against mouse B16/F10 cells after 48 hrs by MTT assay
    [PMID: 22739087]
    CT26 IC50
    13.59 μM
    Compound: 2
    Cytotoxicity against mouse CT26 cells after 72 hrs by MTT assay
    Cytotoxicity against mouse CT26 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    CT26 IC50
    2.21 μM
    Compound: 1
    Cytotoxicity against mouse CT26 cells after 72 hrs by MTT assay
    Cytotoxicity against mouse CT26 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    CT26 IC50
    23.2 μM
    Compound: (-)-Gossypol
    Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27994761]
    CT26 IC50
    46.78 μM
    Compound: (+/-)-Gossypol
    Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27994761]
    CT26 IC50
    61.9 μM
    Compound: (+)-Gossypol
    Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27994761]
    Cancer cell lines GI50
    2.85 μM
    Compound: (+/-)-Gossypol
    Cytotoxicity against human non-small cell lung cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human non-small cell lung cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 27994761]
    Cancer cell lines GI50
    2.97 μM
    Compound: (+/-)-Gossypol
    Cytotoxicity against human CNS cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human CNS cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 27994761]
    Cancer cell lines GI50
    3.16 μM
    Compound: (+/-)-Gossypol
    Cytotoxicity against human renal cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human renal cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 27994761]
    Cancer cell lines GI50
    3.19 μM
    Compound: (+/-)-Gossypol
    Cytotoxicity against human colon cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human colon cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 27994761]
    Cancer cell lines GI50
    3.5 μM
    Compound: (+/-)-Gossypol
    Cytotoxicity against human ovarian cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human ovarian cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 27994761]
    DU-145 IC50
    19.17 μM
    Compound: (+)-Gossypol
    Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27994761]
    DU-145 IC50
    7.93 μM
    Compound: (+/-)-Gossypol
    Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27994761]
    DU-145 IC50
    7.97 μM
    Compound: (-)-Gossypol
    Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27994761]
    HCT-116 IC50
    21.99 μM
    Compound: 2
    Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    HCT-116 IC50
    3.03 μM
    Compound: (+/-)-Gossypol
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27994761]
    HCT-116 IC50
    3.33 μM
    Compound: 1
    Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    HCT-116 IC50
    3.59 μM
    Compound: (-)-Gossypol
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27994761]
    HCT-116 IC50
    5.01 μM
    Compound: (+)-Gossypol
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27994761]
    HEK293 IC50
    11.04 μM
    Compound: AT-101
    Cytotoxicity against human HEK293 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human HEK293 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27353532]
    HL-60 IC50
    6.6 μM
    Compound: AT-101
    Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human HL60 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27353532]
    HT-29 IC50
    > 5 μg/mL
    Compound: 18
    Cytotoxicity against human HT29 cells by SRB assay
    Cytotoxicity against human HT29 cells by SRB assay
    [PMID: 18553924]
    HeLa IC50
    0.08 μg/mL
    Compound: 18
    Cytotoxicity against human HeLa cells by SRB assay
    Cytotoxicity against human HeLa cells by SRB assay
    [PMID: 18553924]
    HeLa IC50
    17.8 μM
    Compound: (-)-Gossypol
    Anticancer activity against human HeLa cells after 48 hrs by MTT assay
    Anticancer activity against human HeLa cells after 48 hrs by MTT assay
    [PMID: 19447525]
    HeLa IC50
    31.3 μM
    Compound: (+)-Gossypol
    Anticancer activity against human HeLa cells after 48 hrs by MTT assay
    Anticancer activity against human HeLa cells after 48 hrs by MTT assay
    [PMID: 19447525]
    HepG2 IC50
    10.16 μg/mL
    Compound: (R)-Gossypol
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    [PMID: 22739087]
    K562 IC50
    4.55 μM
    Compound: (R)-Gossypol
    Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
    Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
    [PMID: 25818766]
    K562 IC50
    5.6 μM
    Compound: Gossypol
    Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
    Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
    [PMID: 27810438]
    K562 IC50
    5.91 μM
    Compound: Gossypol
    Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
    Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
    [PMID: 26620718]
    K562 IC50
    7.31 μM
    Compound: Gossypol
    Antiproliferative activity against human K562 cells by MTT assay
    Antiproliferative activity against human K562 cells by MTT assay
    [PMID: 26421995]
    K562 IC50
    8.28 μM
    Compound: (-)-(R)-Gossypol
    Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
    Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
    [PMID: 28233676]
    KB IC50
    0.04 μg/mL
    Compound: 18
    Cytotoxicity against human KB cells by SRB assay
    Cytotoxicity against human KB cells by SRB assay
    [PMID: 18553924]
    Leukemia cell GI50
    2.47 μM
    Compound: (+/-)-Gossypol
    Cytotoxicity against human leukemia cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human leukemia cells assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 27994761]
    MCF7 IC50
    12.58 μM
    Compound: 1
    Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    MCF7 IC50
    21.56 μM
    Compound: 2
    Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    MCF7 IC50
    54 μM
    Compound: (-)-Gossypol
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27994761]
    MCF7 IC50
    60.1 μM
    Compound: (+/-)-Gossypol
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27994761]
    MCF7 IC50
    75 μM
    Compound: (+)-Gossypol
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 27994761]
    MCF7S IC50
    13.2 μM
    Compound: Gossypol
    Inhibitory concentration in MCF-7 cells
    Inhibitory concentration in MCF-7 cells
    [PMID: 13678404]
    MDA-MB-231 IC50
    1.9 μM
    Compound: 1
    Growth inhibition of human MDA-MB-231 cells after 4 days by WST-based assay
    Growth inhibition of human MDA-MB-231 cells after 4 days by WST-based assay
    [PMID: 17552510]
    MDA-MB-231 IC50
    3.7 μM
    Compound: 2, R-(-)-gossypol
    Growth inhibition of human MDA-MB-231 2LMP cells after 4 days by WST-8 based assay
    Growth inhibition of human MDA-MB-231 2LMP cells after 4 days by WST-8 based assay
    [PMID: 18237106]
    MDA-MB-231 IC50
    4.8 μM
    Compound: Gossypol
    Antiproliferative activity against human MDA-MB-231 cells by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells by MTT assay
    [PMID: 26421995]
    MDA-MB-231 IC50
    8.54 μM
    Compound: (-)-(R)-Gossypol
    Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
    [PMID: 28233676]
    MDA-MB-231 IC50
    9.21 μM
    Compound: (R)-Gossypol
    Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
    [PMID: 25818766]
    MDA-MB-231 IC50
    9.23 μM
    Compound: Gossypol
    Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
    [PMID: 27810438]
    MDA-MB-231 IC50
    9.42 μM
    Compound: Gossypol
    Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
    [PMID: 26620718]
    MDA-MB-435 IC50
    11.78 μM
    Compound: 1
    Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    MDA-MB-435 IC50
    33.25 μM
    Compound: 2
    Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    MDCK CC50
    3.53 μM
    Compound: (+)-Gossypol
    Cytotoxicity against MDCK cells by MTT assay
    Cytotoxicity against MDCK cells by MTT assay
    [PMID: 23538114]
    MDCK CC50
    3.53 μM
    Compound: Gossypol
    Cytotoxicity against MDCK cells by MTT assay
    Cytotoxicity against MDCK cells by MTT assay
    [PMID: 22226654]
    MDCK CC50
    35.35 μM
    Compound: (-)-Gossypol
    Cytotoxicity against MDCK cells by MTT assay
    Cytotoxicity against MDCK cells by MTT assay
    [PMID: 23538114]
    MDCK IC50
    1.87 μM
    Compound: (+)-Gossypol
    Antiviral activity against Influenza A virus (A/Vietnam/1194/2004(H5N1)) infected in MDCK cells by plaque reduction assay
    Antiviral activity against Influenza A virus (A/Vietnam/1194/2004(H5N1)) infected in MDCK cells by plaque reduction assay
    [PMID: 23538114]
    MDCK IC50
    2.14 μM
    Compound: Gossypol, (-)/(+)-Gossypol
    Antiviral activity against H5N1 subtype infected in MDCK cells
    Antiviral activity against H5N1 subtype infected in MDCK cells
    [PMID: 23538114]
    MDCK IC50
    3.82 μM
    Compound: (-)-Gossypol
    Antiviral activity against Influenza A virus (A/Vietnam/1194/2004(H5N1)) infected in MDCK cells by plaque reduction assay
    Antiviral activity against Influenza A virus (A/Vietnam/1194/2004(H5N1)) infected in MDCK cells by plaque reduction assay
    [PMID: 23538114]
    Melanoma cell GI50
    3.22 μM
    Compound: (+/-)-Gossypol
    Cytotoxicity against human melanoma cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human melanoma cells assessed as cell growth inhibition after 48 hrs by SRB assay
    [PMID: 27994761]
    NCI-H1299 EC50
    6 μM
    Compound: 1, Gossypol
    Cytotoxicity against human H1299 cells assessed as cell viability after 72 hrs by ATP-LITE assay
    Cytotoxicity against human H1299 cells assessed as cell viability after 72 hrs by ATP-LITE assay
    [PMID: 19555126]
    NCI-H460 EC50
    3 μM
    Compound: 1, Gossypol
    Cytotoxicity against human H460 cells assessed as cell viability after 72 hrs by ATP-LITE assay
    Cytotoxicity against human H460 cells assessed as cell viability after 72 hrs by ATP-LITE assay
    [PMID: 19555126]
    PC-3 EC50
    17.8 μM
    Compound: (+)-1
    Cytotoxicity against human PC3 cells after 3 days by ATP-LITE assay
    Cytotoxicity against human PC3 cells after 3 days by ATP-LITE assay
    [PMID: 20443627]
    PC-3 EC50
    3.3 μM
    Compound: (-)-1
    Cytotoxicity against human PC3 cells after 3 days by ATP-LITE assay
    Cytotoxicity against human PC3 cells after 3 days by ATP-LITE assay
    [PMID: 20443627]
    PC-3 IC50
    2.5 μM
    Compound: 2, R-(-)-gossypol
    Growth inhibition of human PC3 cells after 4 days by WST-8 based assay
    Growth inhibition of human PC3 cells after 4 days by WST-8 based assay
    [PMID: 18237106]
    PC-3 IC50
    22.36 μM
    Compound: 2
    Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
    Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    PC-3 IC50
    5.61 μM
    Compound: Gossypol
    Antiproliferative activity against human PC3 cells by MTT assay
    Antiproliferative activity against human PC3 cells by MTT assay
    [PMID: 26421995]
    PC-3 IC50
    5.78 μM
    Compound: Gossypol
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    [PMID: 26620718]
    PC-3 IC50
    6.26 μM
    Compound: (R)-Gossypol
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    [PMID: 25818766]
    PC-3 IC50
    6.71 μg/mL
    Compound: (R)-Gossypol
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    [PMID: 22739087]
    PC-3 IC50
    7.54 μM
    Compound: Gossypol
    Antiproliferative activity against human PC3 cells measured after 48 hrs by MTT assay
    Antiproliferative activity against human PC3 cells measured after 48 hrs by MTT assay
    [PMID: 27810438]
    PC-3 IC50
    8.58 μM
    Compound: (-)-(R)-Gossypol
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    [PMID: 28233676]
    PC-3 IC50
    9.14 μM
    Compound: 1
    Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
    Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    SW-620 IC50
    12.58 μM
    Compound: 1
    Cytotoxicity against human SW620 cells after 72 hrs by MTT assay
    Cytotoxicity against human SW620 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    SW-620 IC50
    21.56 μM
    Compound: 2
    Cytotoxicity against human SW620 cells after 72 hrs by MTT assay
    Cytotoxicity against human SW620 cells after 72 hrs by MTT assay
    [PMID: 20684596]
    TZM CC50
    18.12 μM
    Compound: (+)-Gossypol
    Cytotoxicity against human TZM-bl cells after 72 hrs by MTT assay
    Cytotoxicity against human TZM-bl cells after 72 hrs by MTT assay
    [PMID: 29162455]
    TZM CC50
    5.22 μM
    Compound: (-)-Gossypol
    Cytotoxicity against human TZM-bl cells after 72 hrs by MTT assay
    Cytotoxicity against human TZM-bl cells after 72 hrs by MTT assay
    [PMID: 29162455]
    TZM CC50
    9.76 μM
    Compound: Gossypol
    Cytotoxicity in human TZM-bl cells by MTT assay
    Cytotoxicity in human TZM-bl cells by MTT assay
    [PMID: 22226654]
    U-87MG ATCC IC50
    30.2 μM
    Compound: (-)-Gossypol
    Anticancer activity against human U87 cells after 48 hrs by MTT assay
    Anticancer activity against human U87 cells after 48 hrs by MTT assay
    [PMID: 19447525]
    U-87MG ATCC IC50
    59.6 μM
    Compound: (+)-Gossypol
    Anticancer activity against human U87 cells after 48 hrs by MTT assay
    Anticancer activity against human U87 cells after 48 hrs by MTT assay
    [PMID: 19447525]
    ZR-75-1 IC50
    8.4 μM
    Compound: Gossypol
    Inhibitory concentration in ZR-75-1 cells
    Inhibitory concentration in ZR-75-1 cells
    [PMID: 13678404]
    In Vitro

    Gossypol, a natural product isolated from cottonseeds and roots that has been studied as an anticancer agent. The racemic form of Gossypol [(±)-Gossypol] is tested in several clinical trials and is well tolerated. The racemic form Gossypol ((±)-Gossypol) binds to Bcl-xL protein with a Ki of 0.5 to 0.6 μM. (±)-Gossypol also potently binds to Bcl-2 protein with a Ki value of 0.2-0.3 mM. The natural racemic Gossypol has two enantiomers, namely the (-)-Gossypol and (+)-Gossypol enantiomers. The racemic form and each of the enantiomers of Gossypol are tested against UM-SCC-6 and UM-SCC-14A in 6-day MTT assays. (-)-Gossypol exhibits greater growth inhibition relative to (±)-Gossypol than (+)-Gossypol in both cell lines tested (P<0.001). An intermediate growth inhibitory effect is observed with (±)-Gossypol but this effect is only observed at the higher dose of Gossypol (10 μM, P<0.0001)[1].

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

    In Vivo

    Note:
    Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

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

    Clinical Trial
    Molecular Weight

    518.55

    Formula

    C30H30O8

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=CC1=C(O)C(O)=C(C(C)C)C2=CC(C)=C(C3=C(C)C=C4C(C(C)C)=C(O)C(O)=C(C=O)C4=C3O)C(O)=C12

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 33.33 mg/mL (64.28 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 1.9285 mL 9.6423 mL 19.2845 mL
    5 mM 0.3857 mL 1.9285 mL 3.8569 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

      Solubility: ≥ 2.08 mg/mL (4.01 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.
    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    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: 99.67%

    References
    Cell Assay
    [1]

    Two representative UM-SCC cell lines, UM-SCC-6 and UM-SCC-14A, are continuously exposed to 0 (vehicle control), 5 or 10 μM (±)-Gossypol, (-)-Gossypol or (+)-Gossypol in a 6-day MTT cell survival assay[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, 6 months; -20°C, 1 month (protect from light). 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 1 mM 1.9285 mL 9.6423 mL 19.2845 mL 48.2114 mL
    5 mM 0.3857 mL 1.9285 mL 3.8569 mL 9.6423 mL
    10 mM 0.1928 mL 0.9642 mL 1.9285 mL 4.8211 mL
    15 mM 0.1286 mL 0.6428 mL 1.2856 mL 3.2141 mL
    20 mM 0.0964 mL 0.4821 mL 0.9642 mL 2.4106 mL
    25 mM 0.0771 mL 0.3857 mL 0.7714 mL 1.9285 mL
    30 mM 0.0643 mL 0.3214 mL 0.6428 mL 1.6070 mL
    40 mM 0.0482 mL 0.2411 mL 0.4821 mL 1.2053 mL
    50 mM 0.0386 mL 0.1928 mL 0.3857 mL 0.9642 mL
    60 mM 0.0321 mL 0.1607 mL 0.3214 mL 0.8035 mL
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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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