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.
KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.
IC50 & Target
Ki: 44 nM (c-Src)[1] Kd: 86 nM (c-Src)[1]
体外研究 (In Vitro)
KB SRC 4 (Compound 4) is a potent, highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM. KB SRC 4 is selective between Src family members, with >2-fold selectivity over both Lck (Kd, 160 nM) and Fgr (Kd, 240 nM), 8-fold selectivity over c-Yes (Kd, 720 nM), and >40-fold selectivity over Lyn (Kd, 3200 nM), Hck (Kd, 4400 nM), and Fyn (Kd, >40000 nM). KB SRC 4 inhibits the growth of cancer cell lines, with GI50s of 11 μM, 12 μM, 11 μM, 6.0 μM against HT-29, SK-BR-3, MCF7, MDA-MB-453, and NIH-3T3, respectively[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
555.03
Formula
C32H23ClN8
CAS 号
1380088-03-8
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]. Brandvold KR, et al. Development of a highly selective c-Src kinase inhibitor. ACS Chem Biol. 2012 Aug 17;7(8):1393-8.
T338C Src-IN-1 is a potent mutant-Src T338C inhibitor; exhibited the most potent inhibition of T338C(IC50=111 nM) relative to WT c-Src (10-fold increase).
分子量
372.44
Formula
C17H20N6O2S
CAS 号
1351926-90-3
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]. Garske AL, et al. Chemical genetic strategy for targeting protein kinases based on covalent complementarity. Proc Natl Acad Sci U S A. 2011 Sep 13;108(37):15046-52.
T338C Src-IN-2 is a potent mutant c-Src T338C kinase inhibitor with IC50 of 317 nM; also inhibits T338C/V323A and T338C/V323S with IC50 of 57 nM/19 nM.
分子量
327.36
Formula
C17H18FN5O
CAS 号
1351927-00-8
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]. Garske AL, et al. Chemical genetic strategy for targeting protein kinases based on covalent complementarity. Proc Natl Acad Sci U S A. 2011 Sep 13;108(37):15046-52.
SU6656 is a Src family kinases inhibitor with IC50s of 280, 20, 130, 170 nM for Src, Yes, Lyn, and Fyn, respectively. SU6656 inhibits FAK phosphorylation at Y576/577, Y925, Y861 sites. SU6656 also inhibits p-AKT.
体外研究 (In Vitro)
SU6656 decreases phosphorylation of Src family kinases (SFKs) in HNSCC cells[2].
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.
体内研究 (In Vivo)
SU6656 (2-4 mg/kg; i.p.; once) significantly decreases ischemic postconditioning (IPoCo) mediated increase in fall down time[5].
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:
Swiss albino male mice[5]
Dosage:
2, 4 mg/kg
Administration:
Intraperitoneal injection; once
Result:
Significantly decreased IPoCo mediated increase in fall down time.
分子量
371.45
Formula
C19H21N3O3S
CAS 号
330161-87-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Blake RA, et al. SU6656, a selective src family kinase inhibitor, used to probe growth factor signaling. Mol Cell Biol. 2000 Dec;20(23):9018-27.
[2]. Veracini L, et al. Elevated Src family kinase activity stabilizes E-cadherin-based junctions and collective movement of head and neck squamous cell carcinomas. Oncotarget. 2014 Dec 26.
[3]. Wu ML, et al. Divergent signaling pathways cooperatively regulate TGFβ induction of cysteine-rich protein 2 in vascular smooth muscle cells. Cell Commun Signal. 2014 Mar 28;12:22.
[4]. Ondrusová L, et al. Inhibition of mTORC1 by SU6656, the selective Src kinase inhibitor, is not accompanied by activation of Akt/PKB signalling in melanoma cells. Folia Biol (Praha). 2013;59(4):162-7.
[5]. Kumar A, et al. Pharmacological investigations on possible role of Src kinases in neuroprotective mechanism of ischemic postconditioning in mice. Int J Neurosci. 2014 Oct;124(10):777-86.
[6]. Liu XF, et al. Antitumor effects of immunotoxins are enhanced by lowering HCK or treatment with SRC kinase inhibitors. Mol Cancer Ther. 2014 Jan;13(1):82-9.
Src Inhibitor 3 是一种有效的、口服活性的 c 末端 Src 激酶 (CSK)，在 CSK HTRF 和 Caliper 实验中IC50 值分别为低于 3 nM 和 4 nM。Src Inhibitor 3 具有增强 T 细胞受体信号转导诱导的 T 细胞增殖的能力。
Src Inhibitor 3 Chemical Structure
CAS No. : 2380027-49-4
规格
价格
是否有货
数量
10 mM * 1 mL in DMSO
￥5910
In-stock
5 mg
￥4000
In-stock
10 mg
￥6800
In-stock
25 mg
￥13500
In-stock
50 mg
询价
100 mg
询价
* Please select Quantity before adding items.
Src Inhibitor 3 相关产品
•相关化合物库:
Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Pancreatic Cancer Compound Library
Angiogenesis Related Compound Library
生物活性
Src Inhibitor 3 is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. Src Inhibitor 3 shows the ability to increase T cell proliferation induced by T cell receptor signaling[1].
Src Inhibitor 3 reduces inhibitory LCK phosphorylation in vivo upon oral dosing and shows the ability to enhance T cell activation in response to antigen stimulation[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
671.12
Formula
C34H32ClFN8O4
CAS 号
2380027-49-4
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. O’Malley DP, et al. Discovery of Pyridazinone and Pyrazolo[1,5-a]pyridine Inhibitors of C-Terminal Src Kinase. ACS Med Chem Lett. 2019 Sep 25;10(10):1486-1491.
Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
IC50 & Target
IC50: 44 nM (Src), 88 nM (Lck)[1]
体外研究 (In Vitro)
Src-I1 is competitive with both ATP and peptide binding sites of the kinase. The IC50 values are 44 and 88 nM for Src and Lck, respectively[1]. Src-I1, is found to be a potent inhibitor of Src (IC50=0.18 μM), but also inhibited other Src family members, such as Lck, Csk and Yes with similar potency to Src, and RIP2 (IC50=0.026 μM) with even greater potency. In addition, it inhibited CHK2 with similar potency to Src, and Aurora B with slightly lower potency[2].
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
373.40
Formula
C22H19N3O3
CAS 号
179248-59-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Tian G, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91.
[2]. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
Kinase Assay [2]
Assays (25.5 μL volume) are carried out robotically at room temperature (21°C) and are linear with respect to time and enzyme concentration under the conditions used. Assays are performed for 30 min using Multidrop Micro reagent dispensers in a 96-well format. The concentration of magnesium acetate in the assays is 10 mM and [γ-33P]ATP (800 c.p.m./pmol) is used at 5, 20 or 50 μM as indicated, in order to be at or below the Kmfor ATP for each enzyme.The assays are initiated with MgATP, stopped by the addition of 5 μL of 0.5 M orthophosphoric acid and spotted on to P81 filter plates using a unifilter harvester. The IC50 values of inhibitors are determined after carrying out assays at ten different concentrations of each compound[2].
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.
参考文献
[1]. Tian G, et al. Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. Biochemistry. 2001 Jun 19;40(24):7084-91.
[2]. Bain J, et al. The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
![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)
