Pyridostatin (RR82) TFA is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin TFA promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin TFA targets the proto-oncogene Src. Pyridostatin TFA reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells[1][2][3].
体外研究 (In Vitro)
Pyridostatin (RR82) hydrochloride (10 μM; 48 hours) induces cell cycle arrest[1]. Pyridostatin TFA is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure. Pyridostatin TFA causes neurite retraction, synaptic loss, and dose-dependent neuronal death. In cultured primary neurons, Pyridostatin TFA induces the formation of DNA DSBs. Remarkably, Pyridostatin TFA (1-5 μM, overnight) downregulates the BRCA1 protein, a protein that guards and repairs the neuronal genome, at the transcriptional level[3].
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:
Over 60 different cancer cell lines
Concentration:
10 μM
Incubation Time:
48 hours
Result:
Predominantly accumulated in the G2 phase of the cell cycle over 60 different cancer cell lines.
分子量
710.66
Formula
C33H33F3N8O7
CAS 号
1472611-44-1
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]. Rodriguez R, et al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012;8(3):301-310. Published 2012 Feb 5.
[2]. Koirala D, et al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011;3(10):782-787. Published 2011 Aug 28.
[3]. Moruno-Manchon JF, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017;9(9):1957-1970.
Pyridostatin (RR82) TFA is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin TFA promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin TFA targets the proto-oncogene Src. Pyridostatin TFA reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells[1][2][3].
体外研究 (In Vitro)
Pyridostatin (RR82) hydrochloride (10 μM; 48 hours) induces cell cycle arrest[1]. Pyridostatin TFA is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure. Pyridostatin TFA causes neurite retraction, synaptic loss, and dose-dependent neuronal death. In cultured primary neurons, Pyridostatin TFA induces the formation of DNA DSBs. Remarkably, Pyridostatin TFA (1-5 μM, overnight) downregulates the BRCA1 protein, a protein that guards and repairs the neuronal genome, at the transcriptional level[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.
Cell Viability Assay[1]
Cell Line:
Over 60 different cancer cell lines
Concentration:
10 μM
Incubation Time:
48 hours
Result:
Predominantly accumulated in the G2 phase of the cell cycle over 60 different cancer cell lines.
分子量
710.66
Formula
C33H33F3N8O7
CAS 号
1472611-44-1
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]. Rodriguez R, et al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012;8(3):301-310. Published 2012 Feb 5.
[2]. Koirala D, et al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011;3(10):782-787. Published 2011 Aug 28.
[3]. Moruno-Manchon JF, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017;9(9):1957-1970.
Pyridostatin (RR82) TFA is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin TFA promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin TFA targets the proto-oncogene Src. Pyridostatin TFA reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells[1][2][3].
体外研究 (In Vitro)
Pyridostatin (RR82) hydrochloride (10 μM; 48 hours) induces cell cycle arrest[1]. Pyridostatin TFA is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure. Pyridostatin TFA causes neurite retraction, synaptic loss, and dose-dependent neuronal death. In cultured primary neurons, Pyridostatin TFA induces the formation of DNA DSBs. Remarkably, Pyridostatin TFA (1-5 μM, overnight) downregulates the BRCA1 protein, a protein that guards and repairs the neuronal genome, at the transcriptional level[3].
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:
Over 60 different cancer cell lines
Concentration:
10 μM
Incubation Time:
48 hours
Result:
Predominantly accumulated in the G2 phase of the cell cycle over 60 different cancer cell lines.
分子量
710.66
Formula
C33H33F3N8O7
CAS 号
1472611-44-1
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]. Rodriguez R, et al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012;8(3):301-310. Published 2012 Feb 5.
[2]. Koirala D, et al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011;3(10):782-787. Published 2011 Aug 28.
[3]. Moruno-Manchon JF, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017;9(9):1957-1970.
RR6-d5 is the deuterium labeled RR6. RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540 nM for recombinant vanin-1. RR6 also potently inhibits human, bovine and rat serum pantetheinase with IC50 values of 40 nM, 41 nM and 87 nM, respectively[1].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
298.39
Formula
C16H18D5NO4
CAS 号
2714413-24-6
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Jansen PA et al. Discovery of small molecule vanin inhibitors: new tools to study metabolism and disease. ACS Chem Biol. 2013 Mar 15;8(3):530-4.
RR6-d5 is the deuterium labeled RR6. RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540 nM for recombinant vanin-1. RR6 also potently inhibits human, bovine and rat serum pantetheinase with IC50 values of 40 nM, 41 nM and 87 nM, respectively[1].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
298.39
Formula
C16H18D5NO4
CAS 号
2714413-24-6
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Jansen PA et al. Discovery of small molecule vanin inhibitors: new tools to study metabolism and disease. ACS Chem Biol. 2013 Mar 15;8(3):530-4.
RR6-d5 is the deuterium labeled RR6. RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540 nM for recombinant vanin-1. RR6 also potently inhibits human, bovine and rat serum pantetheinase with IC50 values of 40 nM, 41 nM and 87 nM, respectively[1].
体外研究 (In Vitro)
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
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.
分子量
298.39
Formula
C16H18D5NO4
CAS 号
2714413-24-6
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]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Jansen PA et al. Discovery of small molecule vanin inhibitors: new tools to study metabolism and disease. ACS Chem Biol. 2013 Mar 15;8(3):530-4.
Peptide derived from the sequence of a region that contains the major phosphorylation site for cAMP-dependent protein kinase in rat hepatic ribosomal protein S6.
溶解度
分子量
1519.7
化学式
C64H106N22O21
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
Pyridostatin (RR82) 是一种高选择性的 G-quadruplex DNA 稳定剂 (Kd=490 nM)。Pyridostatin 通过诱导复制和转录依赖的 DNA 损伤促进人类癌细胞生长停滞。Pyridostatin 靶向原癌基因 Src。Pyridostatin 降低人乳腺癌细胞 SRC 蛋白水平和 SRC 依赖的细胞运动。
Pyridostatin Chemical Structure
CAS No. : 1085412-37-8
规格
是否有货
100 mg
询价
250 mg
询价
500 mg
询价
* Please select Quantity before adding items.
Pyridostatin 的其他形式现货产品:
Pyridostatin hydrochloride
生物活性
Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets the proto-oncogene Src. Pyridostatin reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells[1][2].
IC50 & Target
Kd: 490 nM (G-quadruplexe)[1]
体外研究 (In Vitro)
Pyridostatin (RR82) (10 μM; 48 hours) induces cell cycle arrest[1]. Pyridostatin is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure. Pyridostatin causes neurite retraction, synaptic loss, and dose-dependent neuronal death. In cultured primary neurons, Pyridostatin induces the formation of DNA DSBs. Remarkably, Pyridostatin (1-5 μM, overnight) downregulates the BRCA1 protein, a protein that guards and repairs the neuronal genome, at the transcriptional level[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.
Cell Viability Assay[1]
Cell Line:
Over 60 different cancer cell lines
Concentration:
10 μM
Incubation Time:
48 hours
Result:
Predominantly accumulated in the G2 phase of the cell cycle over 60 different cancer cell lines.
分子量
596.64
Formula
C31H32N8O5
CAS 号
1085412-37-8
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]. Rodriguez R, et al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012;8(3):301-310. Published 2012 Feb 5.
[2]. Koirala D, et al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011;3(10):782-787. Published 2011 Aug 28.
[3]. Moruno-Manchon JF, Koellhoffer EC, Gopakumar J, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017;9(9):1957-1970.
RR-11a is a synthetic enzyme inhibitor of Legumain (IC50=31-55 nM). RR-11a can be used for the research of cancer and acute myocardial infarction (AMI)[1][2][3].
IC50 & Target[2]
Legumain
31-55 nM (IC50)
体外研究 (In Vitro)
Legumain-targeted RR-11a-coupled nanoparticles reveal high ligand-receptor affinity, enhance solid-tumor penetration and uptake by tumor cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Treatment of tumor-bearing mice with RR-11a-coupled NPs encapsulating doxorubicin results in improved tumor selectivity and drug sensitivity, leading to complete inhibition of tumor growth[1]. RR-11a (20 mg/kg; daily i.p. for 30 days) improves cardiac function, decreases cardiac rupture rate, and attenuates left chamber dilation and wall thinning post-AMI in mice[3].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
560.51
Formula
C24H28N6O10
CAS 号
1361390-56-8
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]. Liao D, et al. Synthetic enzyme inhibitor: a novel targeting ligand for nanotherapeutic drug delivery inhibiting tumor growth without systemic toxicity. Nanomedicine. 2011 Dec;7(6):665-73.
[2]. Ralph A, et al. Nanoparticle-based tumor-targeted drug delivery. Patent: CA2809617C
[3]. Yang H, et al. Legumain is a predictor of all-cause mortality and potential therapeutic target in acute myocardial infarction. Cell Death Dis. 2020;11(11):1014. Published 2020 Nov 26.
Animal Administration [1]
Mice[1]
Mice bearing 4T1 orthothopic tumors of approximately 500 mm3 are injected once intravenously with RR-11a+ or RR-11a-nanoparticles labeled with rhodamine B. Alternatively, mice are injected intravenously 3 times at 48-hour intervals with RDZ-218, NP-DOX, free DOX, or saline. Twenty-four hours after the final treatment, animals are sacrificed and spleen, kidney, lungs, liver, heart and tumor are collected, frozen in OCT compound, immediately sectioned and imaged by fluorescence microscopy[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Liao D, et al. Synthetic enzyme inhibitor: a novel targeting ligand for nanotherapeutic drug delivery inhibiting tumor growth without systemic toxicity. Nanomedicine. 2011 Dec;7(6):665-73.
[2]. Ralph A, et al. Nanoparticle-based tumor-targeted drug delivery. Patent: CA2809617C
[3]. Yang H, et al. Legumain is a predictor of all-cause mortality and potential therapeutic target in acute myocardial infarction. Cell Death Dis. 2020;11(11):1014. Published 2020 Nov 26.
RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540 nM for recombinant vanin-1. RR6 also potently inhibits human, bovine and rat serum pantetheinase with IC50 values of 40 nM, 41 nM and 87 nM, respectively[1].
体内研究 (In Vivo)
Oral administration of RR6 in Wistar rats (150-200 g) completely inhibited plasma vanin activity and caused alterations of plasma lipid concentrations upon fasting. RR6 at 3 mg/mL in rats caused a nearly complete inhibition of plasma vanin[1].
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.
Clinical Trial
分子量
293.36
Formula
C16H23NO4
CAS 号
1351758-37-6
运输条件
Room temperature in continental US; may vary elsewhere.
Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin hydrochloride promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin hydrochloride targets the proto-oncogene Src. Pyridostatin hydrochloride reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells[1][2].
IC50 & Target
Kd: 490 nM (G-quadruplexe)[1]
体外研究 (In Vitro)
Pyridostatin (RR82) hydrochloride (10 μM; 48 hours) induces cell cycle arrest[1]. Pyridostatin hydrochloride is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure. Pyridostatin hydrochloride causes neurite retraction, synaptic loss, and dose-dependent neuronal death. In cultured primary neurons, Pyridostatin hydrochloride induces the formation of DNA DSBs. Remarkably, Pyridostatin hydrochloride (1-5 μM, overnight) downregulates the BRCA1 protein, a protein that guards and repairs the neuronal genome, at the transcriptional level[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.
Cell Viability Assay[1]
Cell Line:
Over 60 different cancer cell lines
Concentration:
10 μM
Incubation Time:
48 hours
Result:
Predominantly accumulated in the G2 phase of the cell cycle over 60 different cancer cell lines.
分子量
778.94
Formula
C31H37Cl5N8O5
CAS 号
1781882-65-2
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Rodriguez R, et al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012;8(3):301-310. Published 2012 Feb 5.
[2]. Koirala D, et al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011;3(10):782-787. Published 2011 Aug 28.
[3]. Moruno-Manchon JF, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017;9(9):1957-1970.
![RR-SRC 编码 [81156-93-6]](http://www.fluoroprobe.com/wp-content/uploads/2022/10/20221006_633ed7f889ca4.png)
![RR-SRC 编码 [81156-93-6]](http://www.fluoroprobe.com/wp-content/uploads/2022/10/20221006_633ed7f8df81a.jpg)
![RR-SRC 编码 [81156-93-6]](http://www.fluoroprobe.com/wp-content/uploads/2022/10/20221006_633ed7f0c44cc.png)
![RR-SRC 编码 [81156-93-6]](http://www.fluoroprobe.com/wp-content/uploads/2022/10/20221006_633ed7f124b37.jpg)
