Antibodies
Apogossypolone (ApoG2)
- 貨號 Cat. No.
- S7200
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
Apogossypolone (ApoG2)
Catalog No.S7200
Apogossypolone (ApoG2) is a pan Bcl-2 inhibitor for Bcl-2, Bcl-XL and Mcl-1 with Ki of 35 nM, 660 nM and 25 nM, respectively.
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Biological Activity
| Description | Apogossypolone (ApoG2) is a pan Bcl-2 inhibitor for Bcl-2, Bcl-XL and Mcl-1 with Ki of 35 nM, 660 nM and 25 nM, respectively. | |||||
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| Targets | Bcl-2 | Bcl-XL | Mcl-1 | |||
| IC50 | 35 nM (Ki) [1] | 660 nM (Ki) [1] | 25 nM (Ki) [1] | |||
| In vitro | Apogossypolone (ApoG2) is a semi-synthesized derivative of Gossypol. ApoG2 is a pan Bcl-2 inhibitor for Bcl-2, Bcl-XL and Mcl-1 with Ki of 35 nM, 660 nM and 25 nM, respectively. ApoG2 blocks the formation of heterodimers between Bcl-XL and Bim. ApoG2 effectively inhibits growth of DLCL2 cells at least partly by inducing apoptosis, with IC50 of 350 nM for a treatment of 72 h.[1] ApoG2 inhibits the growth of WSU-FSCCL, with IC50 of 109 nM, and decreases cell number of fresh lymphoma cells. ApoG2 activates caspases-9, -3, and -8, and the cleavage of PARP and AIF.[2] ApoG2 selectively inhibits the proliferation of 3 nasopharyngeal carcinoma (NPC) cell lines (C666-1, CNE-1 and CNE-2) that highly expresses Bcl-2 proteins, with IC50 values of 1.7, 2.055, 4.915 μM.[3]ApoG2 inhibits proliferation of breast cancer cell line MCF-7 by inducing cell apoptosis and autophagy, with 89.20% inhibition for ApoG2 at 40 μM at 72 h.[4] ApoG2 induces ER stress-dependent apoptosis in gastric cancer cells, with IC50 of 18.7 μM at 72 h.[5] | |||||
| In vivo | ApoG2 treatment at 600 mg/kg results in significant growth inhibition of WSU-DLCL2 xenografts.[1] In the WSU-FSCCL-SCID xenograft model, ApoG2 shows a significant antilymphoma effect, with %ILS of 84% in the intravenous and 63% in intraperitoneal treated mice.[2] ApoG2 effectively suppresses tumor growth of NPC xenografts in nude mice.[3] ApoG2 has anticancer effect in subcutaneous gastric cancer cell xenografts in mice.[5] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| Fluorescence polarization-based binding assay | 5-carboxyfluorecein is coupled to the N-terminus of a peptide, GQVGRQLAIIGDDINR, derived from the BH3 domain of Bak (Flu-BakBH3), which is able to bind to Bcl-2, Bcl-XL and Mcl-1 with high-affinity. Recombinant human Bcl-2, Bcl-XL and Mcl-1 proteins are prepared. The binding of Flu-BakBH3 to Bcl-2, Bcl-XL and Mcl-1 proteins is measured on a LS-50 luminescence spectrometer equipped with polarizers using a dual path length quartz cell (500 ml). The fluorophore is excited with vertical polarized light at 480 nm (excitation slit width 15 nm), and the polarization value of the emitted light is observed through vertical and horizontal polarizers at 530 nm (emission slit width 15 nm). The binding affinity of each compound for Bcl-2, Bcl-XL and Mcl-1 proteins is assessed by determining the ability of different concentrations of the compound to inhibit Flu-BakBH3 binding. |
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Cell Assay: [1]
| Cell lines | WSU-DLCL2 |
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| Concentrations | ~1000 nM |
| Incubation Time | 72 h |
| Method | WSU-DLCL2 cells are plated in 24-well culture plates at a density of 2 × 105 viable cells per ml per well. Triplicate wells are treated with 0–1000 nM of ApoG2. Plates are incubated at 37°C in a humidified incubator with 5% CO2. All cultures are monitored throughout the experiment by cell counting every 24 h for four days using 0.4% Trypan Blue stain and a hemacytometer. |
Animal Study: [1]
| Animal Models | SCID mice bearing tumor xenografts |
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| Dosages | 120 mg/kg |
| Administration | oral or i.v. |
References
Chemical Information
Download Apogossypolone (ApoG2) SDF
| Molecular Weight (MW) | 490.5 |
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| Formula | C28H26O8 |
| CAS No. | 886578-07-0 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | mg/mL (<1 mM) |
|---|---|---|---|
| Water | mg/mL (<1 mM) | ||
| Ethanol | mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
