2. Apoptosis Autophagy Anti-infection Protein Tyrosine Kinase/RTK
  3. Bcl-2 Family Apoptosis Autophagy Fungal ROS Kinase
  4. Apogossypolone

Apogossypolone (ApoG2) is an orally active Bcl-2 family proteins inhibitor with Ki values of 35, 25 and 660 nM for Bcl-2, Mcl-1 and Bcl-XL, respectively. Apogossypolone shows antitumor activities, induces cell apoptosis and autophagy. Apogossypolone also has antifungal activity.

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Apogossypolone

Apogossypolone Chemical Structure

CAS No. : 886578-07-0

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Based on 1 publication(s) in Google Scholar

Apogossypolone Related Antibodies

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

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Description

Apogossypolone (ApoG2) is an orally active Bcl-2 family proteins inhibitor with Ki values of 35, 25 and 660 nM for Bcl-2, Mcl-1 and Bcl-XL, respectively. Apogossypolone shows antitumor activities, induces cell apoptosis[1] and autophagy[2]. Apogossypolone also has antifungal activity[3].

IC50 & Target

Mcl-1

25 nM (Ki)

Bcl-2

35 nM (Ki)

Bcl-xL

660 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
NCI-H1299 EC50
2.76 μM
Compound: 6a
Cytotoxicity against human H1299 cells expressing high level of Mcl-1 after 72 hrs by ATP-LITE assay
Cytotoxicity against human H1299 cells expressing high level of Mcl-1 after 72 hrs by ATP-LITE assay
[PMID: 21033669]
NCI-H460 EC50
0.4 μM
Compound: 6a
Cytotoxicity against human H460 cells expressing high level of Bcl-2 after 72 hrs by ATP-LITE assay
Cytotoxicity against human H460 cells expressing high level of Bcl-2 after 72 hrs by ATP-LITE assay
[PMID: 21033669]
PC-3 EC50
1.46 μM
Compound: 6a
Cytotoxicity against human PC3 cells expressing high level of Bcl-xL after 72 hrs by ATP-LITE assay
Cytotoxicity against human PC3 cells expressing high level of Bcl-xL after 72 hrs by ATP-LITE assay
[PMID: 21033669]
RS4-11 EC50
7.4 μM
Compound: 6a
Induction of apoptosis in human RS4:11 cells expressing high level of Bcl-2 and Bcl-xL after 24 hrs by annexin V-FITC and propidium iodide staining
Induction of apoptosis in human RS4:11 cells expressing high level of Bcl-2 and Bcl-xL after 24 hrs by annexin V-FITC and propidium iodide staining
[PMID: 21033669]
RS4-11 EC50
7.47 μM
Compound: 6a
Cytotoxicity against human RS4:11 cells expressing high level of Bcl-2 and Bcl-xL after 72 hrs by annexin V-FITC and propidium iodide staining
Cytotoxicity against human RS4:11 cells expressing high level of Bcl-2 and Bcl-xL after 72 hrs by annexin V-FITC and propidium iodide staining
[PMID: 21033669]
In Vitro

Apogossypolone (ApoG2) shows improved stability under stressed conditions[1].
Apogossypolone (0-1 μM, 72 or 96 h) inhibits WSU-DLCL2 cells growth in a dose-dependent manner[1].
Apogossypolone (0-5 μM, 24 or 48 h) interferes with the formation of heterodimers between anti-apoptotic and pro-apoptotic Bcl-2 family members, and leads to cleavage of caspase-3, caspase-9 and PARP[1].
Apogossypolone (0-8 μM, 0-72 h) induces apoptotic WSU-DLCL2 cell death in a time- and dose-dependent manner[1].
Apogossypolone (0-10 μM, 0-24 h) induces autophagy and promotes ROS generation in HCC cells[2].

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

Apogossypolone Related Antibodies

Cell Proliferation Assay[1]

Cell Line: WSU-DLCL2
Concentration: 250, 350, 500 and 1000 nM
Incubation Time: 96 h for cell counting, 72 h for MTT
Result: Inhibited growth in a dose-dependent manner. The 50% growth inhibition concentration (IC50) was approximately 350 nM.

Western Blot Analysis[1]

Cell Line: WSU-DLCL2
Concentration: 0.35, 0.5, 1 and 5 µM
Incubation Time: 24 or 48 h
Result: Blocked the formation of heterodimers between Bcl-XL and Bim in a concentration-dependent manner. Resulted in the activation of cleavages of caspase-3, caspase-9 and PARP.

Apoptosis Analysis[1]

Cell Line: WSU-DLCL2
Concentration: 0, 1, 2, 4 and 8 µM
Incubation Time: 24, 48 and 72 h
Result: Induced cell apoptosis in a time- and dose-dependent manner.

Cell Autophagy Assay[2]

Cell Line: HepG2 and Hep3B
Concentration: 1.25, 2.5, 5 and 10 µM
Incubation Time: 6, 12, 18 and 24 h
Result: Induced LC3 (Light chain 3)-II conversion in a dose- and time-dependent manner.
In Vivo

Apogossypolone (ApoG2) (120 mg/kg; i.v. or p.o.; once a day for 5 days) effectively inhibits growth of diffuse large cell lymphoma cells without toxicity[1].

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

Animal Model: Four-week-old female ICR-SCID mice, each mouse received 107 WSU-DLCL2 cells (in serum-free RPMI 1640) subcutaneously (sc) in each flank area[1]
Dosage: 120 mg/kg
Administration: Intravenous or administration per day for five days
Result: Inhibited the growth of WSU-DLCL2 and significantly decreased the tumor weight.
Animal Model: Non-tumor-bearing SCID mice[1]
Dosage: 160 mg/kg
Administration: Intravenous or administration per day for five days
Result: Was well tolerated in mice up to 800 mg/kg. Displayed no gross signs of toxicity.
Molecular Weight

490.50

Formula

C28H26O8
CAS No.
Appearance

Solid

Color

Orange to reddish brown

SMILES

O=C1C(C(C2=O)=C(C)C(C3=C2C=C(O)C(O)=C3C(C)C)=O)=C(C)C(C4=C1C=C(O)C(O)=C4C(C)C)=O
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
Purity & Documentation

Purity: 98.58%

SDS (393 KB)

COA (251 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
References
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Apogossypolone Related Classifications

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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.

Keywords:

Apogossypolone886578-07-0ApoG2ApoG 2ApoG-2Bcl-2 FamilyApoptosisAutophagyFungalROS KinaseantitumorWSU-DLCL2lymphomacaspase-3caspase-9Mcl-1Bcl-XLBcl-2no toxicityantifungalHCCInhibitorinhibitorinhibit

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