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| 产品名称 | Bax ↓ ↑ | Bcl-2 ↓ ↑ | Bcl-B ↓ ↑ | Bcl-w ↓ ↑ | Bcl-xL ↓ ↑ | Bfl-1 ↓ ↑ | Mcl-1 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| BTSA1 | ✔ | 99%+ | |||||||||||||||||
| HA14-1 |
+
Bcl-2, IC50: 9 μM |
98% | |||||||||||||||||
| Venetoclax |
++++
Bcl-2, Ki: <0.01 nM |
99% | |||||||||||||||||
| Navitoclax | 99%+ | ||||||||||||||||||
| Obatoclax Mesylate |
+++
Bcl-2, Ki: 0.22 μM |
99% | |||||||||||||||||
| ABT-737 |
+++
Bcl-2, EC50: 30.3 nM |
+
Bcl-B, EC50: 1.82 μM |
+++
Bcl-w, EC50: 197.8 nM |
+++
Bcl-xL, EC50: 78.7 nM |
99%+ | ||||||||||||||
| Gambogic Acid |
+
Bfl-1, IC50: 1.06 μM Bcl-2, IC50: 1.21 μM |
++
Bcl-B, IC50: 0.66 μM |
++++
Bcl-w, IC50: 0.02 μM |
+
Bcl-xL, IC50: 1.47 μM |
+
Bfl-1, IC50: 1.06 μM |
++
Mcl-1, IC50: 0.79 μM |
Caspase | 99% HPLC | |||||||||||
| BH3I-1 |
+
BH3-Bcl-xL interaction, Ki: 2.4 μM |
99% | |||||||||||||||||
| A-1331852 |
++++
Bcl-xL, Ki: <0.01 nM |
99%+ | |||||||||||||||||
| A-1210477 |
++++
MCL-1, IC50: 26.2 nM |
99%+ | |||||||||||||||||
| Maritoclax | ✔ | 97% | |||||||||||||||||
| TW-37 |
+++
Bcl-2, Ki: 0.29 μM |
+
Bcl-xL, Ki: 1.11 μM |
+++
Mcl-1, Ki: 0.26 μM |
98% | |||||||||||||||
| UMI-77 |
++
Mcl-1, Ki: 490 nM |
97% | |||||||||||||||||
| (R)-(-)-Gossypol acetic acid |
++
Bcl-2, Ki: 0.32 μM |
++
Bcl-xL, Ki: 0.48 μM |
+++
Mcl-1, Ki: 0.18 μM |
99% | |||||||||||||||
| Sabutoclax |
++
Bfl-1, IC50: 0.62 μM Bcl-2, IC50: 0.32 μM |
++
Bcl-xL, IC50: 0.31 μM |
++
Bfl-1, IC50: 0.62 μM |
+++
Mcl-1, IC50: 0.20 μM |
98% | ||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | Jaceosidin is a flavonoid isolated from Artemisia vestita that has been reported to possess anti-tumor and anti-proliferative activities in many cancer cells. Jaceosidin induced apoptosis in multiple human renal carcinoma cells (Caki, ACHN, A498, and 786-O), lung cancer cells (A549) and glioma cells (U251MG). Treatment with jaceosidin also caused loss of mitochondrial membrane potential (MMP) and Bax activation, which led to the release of cytochrome c into the cytosol[3]. Jaceosidin is a more potent inhibitor of cell growth than cisplatin in human endometrial cancer cells. In contrast, jaceosidin-induced cytotoxicity in normal endometrial cells was lower than that observed for cisplatin. Jaceosidin induced G2/M phase cell cycle arrest and modulated the levels of cyclin B and p-Cdc2 in Hec1A cells. Jaceosidin shows cytostatic activity to HES and HESC cells with IC50s of 52.68 and 55.10 μM, and is less cytotocxic on Hec1 A and KLE (IC50, 70.54, 147.14 μM, respectively), after treatment for 48 h[4]. Jaceosidin could improve ER (endoplasmic reticulum) stress and attenuate insulin resistance via SERCA2b (sarco-endoplasmic reticulum Ca2+-ATPase 2b) upregulation in mice skeletal muscles[5]. Mice were orally administrated with Jaceosidin (15, 30 and 60 mg/kg) after LPS challenge. 24 h after LPS (lipopolysaccharide) challenge, Jaceosidin could significantly decrease the lung wet-to-dry weight (W/D) ratio and the protein concentration in bronchoalveolar lavage fluid (BALF) [6]. |
| Concentration | Treated Time | Description | References | |
| 12 types of gastric cancer cells (including AGS, KATO-3, etc.) | 20, 40, 60, 80, 100 μM | 6, 12, 18, 24, 30 hours | JAC showed killing effects on various GC cells with IC50 values ranging from 38.65 to 90.46 μM | Redox Rep. 2024 Dec;29(1):2313366 |
| GES-1 normal gastric cells | 39 μM | 3, 6, 12, 24 hours | No increase in apoptosis observed | Redox Rep. 2024 Dec;29(1):2313366 |
| AGS gastric cancer cells | 39 μM | 3, 6, 12, 24 hours | Induced apoptosis in AGS cells via the mitochondrial pathway by upregulating Cyto-c, Bad, cle-caspase-3, and cle-PARP expressions and downregulating Bcl-2 expression | Redox Rep. 2024 Dec;29(1):2313366 |
| mouse articular chondrocytes | 10, 20, 40, 80 μmol/L | 12 hours | To evaluate the inhibitory effect of Jaceosidin on IL-1β-induced expression of MMP3, MMP13, ADAMTS4, and ADAMTS5. Results showed that Jaceosidin decreased the expression of these proteins in a concentration-dependent manner. | J Cell Mol Med. 2020 Jul;24(14):8126-8137 |
| H1975 cells | 0, 6, 12, 24 μM | 12, 24, 36 hours | Evaluate the inhibitory effect of Jaceosidin on the migration of H1975 cells, the results showed that Jaceosidin significantly inhibited the migration of H1975 cells. | Heliyon. 2023 May 11;9(5):e16158 |
| A549 cells | 0, 6, 12, 24 μM | 12, 24, 36 hours | Evaluate the inhibitory effect of Jaceosidin on the migration of A549 cells, the results showed that Jaceosidin significantly inhibited the migration of A549 cells. | Heliyon. 2023 May 11;9(5):e16158 |
| H1975 cells | 9.19 ±1.90 μM (IC50) | 72 hours | Evaluate the inhibitory effect of Jaceosidin on the proliferation of H1975 cells, the results showed that Jaceosidin significantly inhibited the proliferation of H1975 cells. | Heliyon. 2023 May 11;9(5):e16158 |
| A549 cells | 12.71 ±0.91 μM (IC50) | 72 hours | Evaluate the inhibitory effect of Jaceosidin on the proliferation of A549 cells, the results showed that Jaceosidin significantly inhibited the proliferation of A549 cells. | Heliyon. 2023 May 11;9(5):e16158 |
| oral squamous cell carcinoma YD-8 cells | 10-50 μM | 24 hours | JAC had a minor effect on the survival of YD-8 cells. | Am J Cancer Res. 2021 Oct 15;11(10):4919-4930 |
| Osteosarcoma MG63 cells | 10-50 μM | 24 hours | JAC had a minor effect on the survival of MG63 cells. | Am J Cancer Res. 2021 Oct 15;11(10):4919-4930 |
| human GBM T98G cells | 10-50 μM | 24 hours | JAC significantly reduced the survival of T98G cells, induced apoptotic cell death, altered morphological and molecular phenotypes, increased DNA fragmentation, activated cleavage of caspase-3 and PARP, and downregulated the expression of survivin and Bcl-2. | Am J Cancer Res. 2021 Oct 15;11(10):4919-4930 |
| HaCaT cells | 12.5–100 μM | 24 hours | Jaceosidin at concentrations of 12.5–100 μM did not affect the proliferation of HaCaT normal epithelial keratinocytes, indicating selective cytotoxicity towards cancer cells. | Evid Based Complement Alternat Med. 2018 May 13;2018:5765047 |
| Ca9.22 cells | 97.5 μM | 24 hours | Jaceosidin inhibited Ca9.22 cell proliferation with an IC50 of 97.5 μM, causing morphological changes and cell cycle arrest at the sub-G1 phase. | Evid Based Complement Alternat Med. 2018 May 13;2018:5765047 |
| HSC-3 cells | 82.1 μM | 24 hours | Jaceosidin inhibited HSC-3 cell proliferation with an IC50 of 82.1 μM, causing morphological changes and cell cycle arrest at the sub-G1 phase. | Evid Based Complement Alternat Med. 2018 May 13;2018:5765047 |
| Administration | Dosage | Frequency | Description | References | ||
| C57BL/6 mice | DMM-induced osteoarthritis model | Oral | 50 mg/kg | Every other day for 10 weeks | To evaluate the protective effect of Jaceosidin on DMM-induced cartilage destruction. Results showed that Jaceosidin significantly inhibited cartilage destruction, reduced OARSI scores, and subchondral bone plate thickness. | J Cell Mol Med. 2020 Jul;24(14):8126-8137 |
| Balb/c nude mice | A549 cell xenograft model | Intraperitoneal injection | 25 mg/kg and 50 mg/kg | 7 consecutive days | Evaluate the inhibitory effect of Jaceosidin on tumor growth in A549 cell xenograft model, the results showed that Jaceosidin significantly inhibited tumor growth. | Heliyon. 2023 May 11;9(5):e16158 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.03mL 0.61mL 0.30mL |
15.14mL 3.03mL 1.51mL |
30.28mL 6.06mL 3.03mL |
|
| CAS号 | 18085-97-7 |
| 分子式 | C17H14O7 |
| 分子量 | 330.29 |
| SMILES Code | COC1=C(O)C=CC(=C1)C1=CC(=O)C2=C(O)C(OC)=C(O)C=C2O1 |
| MDL No. | MFCD01081948 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | GLAAQZFBFGEBPS-UHFFFAOYSA-N |
| Pubchem ID | 5379096 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 120 mg/mL(363.32 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 无水乙醇: 7 mg/mL(21.19 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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