3-Methyladenine (3-MA) 是 PI3K 的抑制剂。它通过抑制class III PI3K广泛作为自噬 (autophagy) 的抑制剂使用。
3-Methyladenine Chemical Structure
CAS No. : 5142-23-4
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生物活性
3-Methyladenine (3-MA) is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K[1].
IC50 & Target[1]
PtdIns3Kγ
60 μM (IC50, Cell Assay)
Vps34
25 μM (IC50, Cell Assay)
Autophagy
Mitophagy
Human Endogenous Metabolite
体外研究 (In Vitro)
3-Methyladenine (0-10 mM; 0-48 hours) induces caspase-dependent cell death in HeLa cells in a time-and dose-dependent manner[2]. 3-Methyladenine (5 mM; 24 hours) suppresses autophagy in HeLa cells under both glucose-free conditions and normal conditions[2]. 3-Methyladenine (5 mM; 0-48 hours) suppresses conversion of LC3-I to LC3-II (autophagy markers) between 12hours and 48 hours, confirms the inhibitory effects on autophagy[2]. 3-Methyladenine induces cell death is independent of autophagy inhibition[2]. 3-Methyladenine significantly shortens the duration of nocodazole-induced-prometaphase arrest[2]. Note: 在体外细胞培养实验中，3-MA 常用的浓度为 0.5-10 mM，所以优先推荐直接称取本次实验所需粉末量，用培养基完全溶解，0.22 μm 过滤器过滤除菌之后使用。建议溶液现配现用，尽快用完。
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[2]
Cell Line:
HeLa cells
Concentration:
0 mM, 2.5 mM or 5 mM, 10 mM
Incubation Time:
0 hour, 24 hours and 48 hours
Result:
Decreased cell viability in a time-and dose-dependent manner, and was associated with caspase-3 activation.
Cell Autophagy Assay[2]
Cell Line:
HeLa cells
Concentration:
5 mM
Incubation Time:
24 hours
Result:
Suppressed autophagy in HeLa cells under both glucose-free conditions and normal conditions.
Western Blot Analysis[2]
Cell Line:
HeLa cells
Concentration:
5 mM
Incubation Time:
0 hour, 12 hours, 24 hours and 48 hours
Result:
Suppressed conversion of LC3-I to LC3-II between 12 hours and 48 hours.
体内研究 (In Vivo)
3-Methyladenine (1.5 mg/100 g; intraperitoneal injection; 3-24 hours) treatment alleviates sodium taurocholate-induced severe acute pancreatitis (SAP) in rats at both 12 hours and 24 hours[3]. 3-Methyladenine inhibits autophagy of pancreatic acinar cells in sodium taurocholate-tnduced SAP[3]. 3-Methyladenine also shows inhibitory effects on PI3K/Akt signaling pathway and NF-κB signaling pathway in sodium taurocholate-induced SAP[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
10–12 weeks Specific pathogen free- (SPF-) grade healthy male Sprague-Dawley (SD) rats (250–290 g)[3]
Dosage:
1.5 mg/100 g (1000 μM)
Administration:
Intraperitoneal injection
Result:
Alleviated Sodium Taurocholate-Induced SAP.
分子量
149.15
Formula
C6H7N5
CAS 号
5142-23-4
中文名称
3-甲基腺嘌呤
运输条件
Room temperature in continental US; may vary elsewhere.
Solubility: 4 mg/mL (26.82 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
[1]. Miller S, et al. Finding a fitting shoe for Cinderella: searching for an autophagy inhibitor. Autophagy. 2010 Aug;6(6):805-7.
[2]. Hou H, et al. Inhibitors of phosphatidylinositol 3′-kinases promote mitotic cell death in HeLa cells. PLoS One. 2012;7(4):e35665.
[3]. Wang X, et al. Acanthopanax versus 3-Methyladenine Ameliorates Sodium Taurocholate-Induced Severe Acute Pancreatitis by Inhibiting the Autophagic Pathway in Rats.Mediators Inflamm. 2016;2016:8369704.
MA242 is a specific dual inhibitor of MDM2 and NFAT1. MA242 directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 induces apoptosis in pancreatic cancer cell lines regardless of p53 status[1].
IC50 & Target
MDM2, NFAT1[1]
体外研究 (In Vitro)
MA242 (0.05-5 μM; 72 hours) significantly inhibits pancreatic cancer cell growth, with IC50s ranging from 0.1 to 0.4 μM, regardless of the p53 status of the cells. However, MA242 shows minimal effects on the growth of normal HPDE cells (IC50=5.81 μM), indicating that MA242 has selective effects against cancer cells[1]. MA242 (0.1-0.5 μM; 24 hours) significantly decreases the MDM2 and NFAT1 protein levels at a low concentration in all three cell lines[1]. MA242 decreases cell proliferation and induces apoptosis in pancreatic cancer cell lines regardless of p53 status[1]. MA242 alone or in combination with Gemcitabine inhibits pancreatic tumor growth and metastasis without any host toxicity[1]. MA242 exerts cytotoxicity against hepatocellular carcinoma (HCC) cells by inhibiting the NFAT1-MDM2 pathway in vitro, independent of p53. MA242 shows selective cytotoxicity against HCC cells, with IC50 values ranging from 0.1-0.31 μM[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
The human pancreatic cancer HPAC, Panc-1, AsPC-1, Mia-Paca-2 and BxPC-3 cell lines; The human pancreatic ductal epithelium (HPDE) cell line
Concentration:
0.05, 0.5, and 5 μM
Incubation Time:
72 hours
Result:
The IC50s are 0.14, 0.14, 0.15, 0.25, 0.40, and 5.81 μM for Panc-1, Mia-Paca-2, AsPC-1, BxPC-3, HPAC, and HPDE cells, respectively.
Western Blot Analysis[1]
Cell Line:
The human pancreatic cancer HPAC, Panc-1, and AsPC-1 cell lines
Concentration:
0, 0.1, 0.2, and 0.5 μM
Incubation Time:
24 hours
Result:
Decreased the expression of MDM2 and NFAT1.
体内研究 (In Vivo)
MA242 (IP; 2.5, 5, 10 mg/kg) suppresses orthotopic pancreatic tumor growth in vivo, independent of p53[1]. There were no significant differences in the average body weights between the vehicle- and MA242-treated mice in either of the models, did not have significant host toxicity at these effective doses[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
2.5 or 5 mg/kg for Panc-1 tumor-bearing mice; 10 mg/kg for AsPC-1 tumor-bearing mice
Administration:
IP; 2.5 or 5 mg/kg/d, 5 d/wk for five weeks for Panc-1 tumor-bearing mice; IP; 10 mg/kg/d, 5 d/wk for three weeks for AsPC-1 tumor-bearing mice
Result:
Resulted in 56.1% and 82.5% inhibition of tumor growth in nude mice bearing Panc-1 orthotopic tumors, respectively. Significantly suppressed the growth of AsPC-1 orthotopic tumors by 89.5% (P < 0.01) compared with the tumors in control animals. Led to almost complete tumor regression in MD242-treated mice in both models.
分子量
579.98
Formula
C26H21ClF3N3O5S
CAS 号
1049704-18-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Wang W, et al. Discovery and Characterization of Dual Inhibitors of MDM2 and NFAT1 for Pancreatic Cancer Therapy. Cancer Res. 2018 Oct 1;78(19):5656-5667.
[2]. Wei Wang, et al. MDM2-NFAT1 dual inhibitor, MA242: Effective against hepatocellular carcinoma, independent of p53. Cancer Lett. 2019 Sep 10;459:156-167.
Duocarmycin MA 是抗体偶联药物 (ADCs) 中的毒素分子。Duocarmycin 是一种 DNA 烷化剂，靶向 DNA 小沟。Duocarmycin MA 可用于抗多药耐药细胞系。
Duocarmycin MA Chemical Structure
CAS No. : 1613286-57-9
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5 mg
￥12000
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生物活性
Duocarmycin MA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin MA can be used against multi-drug resistant cell lines.
IC50 & Target
Duocarmycins
分子量
611.09
Formula
C34H31ClN4O5
CAS 号
1613286-57-9
中文名称
倍癌霉素 MA
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Searcey M. Duocarmycins–natures prodrugs? Curr Pharm Des. 2002;8(15):1375-89.
MA242 free base 是特异性的 MDM2 和 NFAT1 双重抑制剂。MA242 free base 以高亲和力直接结合 MDM2 和 NFAT1，诱导 MDM2 和 NFAT1 蛋白降解，并抑制 NFAT1 介导的 MDM2 转录。MA242 free base 在胰腺癌细胞系中诱导凋亡。
MA242 free base Chemical Structure
CAS No. : 1049704-17-7
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100 mg
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250 mg
询价
500 mg
询价
* Please select Quantity before adding items.
生物活性
MA242 free base is a specific dual inhibitor of MDM2 and NFAT1. MA242 free base directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 free base induces apoptosis in pancreatic cancer cell lines regardless of p53 status[1].
IC50 & Target
MDM2, NFAT1[1]
体外研究 (In Vitro)
MA242 (0.05-5 μM; 72 hours) free base significantly inhibits pancreatic cancer cell growth, with IC50s ranging from 0.1 to 0.4 μM, regardless of the p53 status of the cells. However, MA242 free base shows minimal effects on the growth of normal HPDE cells (IC50=5.81 μM), indicating that MA242 has selective effects against cancer cells[1]. MA242 (0.1-0.5 μM; 24 hours) free base significantly decreases the MDM2 and NFAT1 protein levels at a low concentration in all three cell lines[1]. MA242 free base decreases cell proliferation and induces apoptosis in pancreatic cancer cell lines regardless of p53 status[1]. MA242 free base alone or in combination with Gemcitabine inhibits pancreatic tumor growth and metastasis without any host toxicity[1]. MA242 free base exerts cytotoxicity against hepatocellular carcinoma (HCC) cells by inhibiting the NFAT1-MDM2 pathway in vitro, independent of p53. MA242 showed selective cytotoxicity against HCC cells, with IC50 values ranging from 0.1-0.31 μM[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
The human pancreatic cancer HPAC, Panc-1, AsPC-1, Mia-Paca-2 and BxPC-3 cell lines; The human pancreatic ductal epithelium (HPDE) cell line
Concentration:
0.05, 0.5, and 5 μM
Incubation Time:
72 hours
Result:
The IC50s are 0.14, 0.14, 0.15, 0.25, 0.40, and 5.81 μM for Panc-1, Mia-Paca-2, AsPC-1, BxPC-3, HPAC, and HPDE cells, respectively.
Western Blot Analysis[1]
Cell Line:
The human pancreatic cancer HPAC, Panc-1, and AsPC-1 cell lines
Concentration:
0, 0.1, 0.2, and 0.5 μM
Incubation Time:
24 hours
Result:
Decreased the expression of MDM2 and NFAT1.
体内研究 (In Vivo)
MA242 (IP; 2.5, 5, 10 mg/kg) free base suppresses orthotopic pancreatic tumor growth in vivo, independent of p53[1]. There were no significant differences in the average body weights between the vehicle- and MA242 free base-treated mice in either of the models, did not have significant host toxicity at these effective doses[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
2.5 or 5 mg/kg for Panc-1 tumor-bearing mice; 10 mg/kg for AsPC-1 tumor-bearing mice
Administration:
IP; 2.5 or 5 mg/kg/d, 5 d/wk for five weeks for Panc-1 tumor-bearing mice; IP; 10 mg/kg/d, 5 d/wk for three weeks for AsPC-1 tumor-bearing mice
Result:
Resulted in 56.1% and 82.5% inhibition of tumor growth in nude mice bearing Panc-1 orthotopic tumors, respectively. Significantly suppressed the growth of AsPC-1 orthotopic tumors by 89.5% (P < 0.01) compared with the tumors in control animals. Led to almost complete tumor regression in MD242-treated mice in both models.
分子量
465.95
Formula
C24H20ClN3O3S
CAS 号
1049704-17-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Wei Wang, et al. Discovery and Characterization of Dual Inhibitors of MDM2 and NFAT1 for Pancreatic Cancer Therapy. Cancer Res. 2018 Oct 1;78(19):5656-5667.
[2]. Wei Wang, et al. MDM2-NFAT1 dual inhibitor, MA242: Effective against hepatocellular carcinoma, independent of p53. Cancer Lett. 2019 Sep 10;459:156-167.
