NH2-PEG3-C2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
PEGs
体外研究 (In Vitro)
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1]
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
277.36
Formula
C13H27NO5
CAS 号
252881-74-6
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.
Tesirine (SG3249) is an antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. Tesirine combines potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics. SG3199 (HY-101161) is the released warhead component of the ADC payload Tesirine. SG3199 retains picomolar activity in a panel of cancer cell lines. PBD dimers are highly efficient DNA minor groove cross-linking agents with potent cytotoxicity[1][2].
IC50 & Target
Pyrrolobenzodiazepines
体外研究 (In Vitro)
SG3199 (HY-101161) is the released warhead component of the ADC payload Tesirine. SG3199 inhibits K562, NCIN87, BT474, and SKBR3 cancer cells with IC50s of 150 pM, 20 pM, 1 nM and 320 pM[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
1496.65
Formula
C75H101N9O23
CAS 号
1595275-62-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light, stored under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶解性数据
In Vitro:
DMSO : 200 mg/mL (133.63 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
0.6682 mL
3.3408 mL
6.6816 mL
5 mM
0.1336 mL
0.6682 mL
1.3363 mL
10 mM
0.0668 mL
0.3341 mL
0.6682 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
[1]. Tiberghien AC, et al. Design and Synthesis of Tesirine, a Clinical Antibody-Drug Conjugate Pyrrolobenzodiazepine Dimer Payload. ACS Med Chem Lett. 2016;7(11):983-987. Published 2016 May 24.
[2]. Hartley JA, et al. Pre-clinical pharmacology and mechanism of action of SG3199, the pyrrolobenzodiazepine (PBD) dimer warhead component of antibody-drug conjugate (ADC) payload tesirine. Sci Rep. 2018;8(1):10479. Published 2018 Jul 11.
Monensin sodium salt(Synonyms: Monensin A sodium salt) 纯度: ≥98.0%
Monensin sodium salt 是由肉桂链霉菌 (Streptomyces cinnamonensis) 分泌的抗生素。Monensin sodium salt 是一种介导 Na+/H+ 交换的离子载体。Monensin sodium salt 引起细胞多泡体 (MVBs) 增大并调节外泌体的分泌。
Monensin sodium salt Chemical Structure
CAS No. : 22373-78-0
规格
价格
是否有货
数量
Free Sample (0.1-0.5 mg)
Apply now
10 mM * 1 mL in Ethanol
￥440
In-stock
100 mg
￥400
In-stock
200 mg
询价
500 mg
询价
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Monensin sodium salt 相关产品
•相关化合物库:
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Microbial Metabolite Library
生物活性
Monensin sodium salt is an antibiotic secreted by the bacteria Streptomyces cinnamonensis. Monensin sodium salt is an ionophore that mediates Na+/H+ exchange. Monensin sodium salt causes a marked enlargement of the multivesicular bodies (MVBs) and regulates exosome secretion[1][2][3][4].
IC50 & Target
bacterial[1]
体外研究 (In Vitro)
Monensin sodium salt is an antibiotic secreted by the bacteria Streptomyces cinnamonensis. Untreated cells display 2.5% apoptosis; 48 hours treatment with 1 μM Monensin sodium salt shows 4.5% apoptosis whereas 5 μM Monensin sodium salt for 48 hours induces a greater apoptotic response (16.4%). Pretreatment with either 1 or 5 μM Monensin sodium salt for 24 hours followed by 10 μM erlotinib treatment for another 24 hours results in a marked increases in apoptotic events (14.6% and 38.7%, respectively) when compare with either Monensin sodium salt or erlotinib treatments alone. Combination of 5 μM Monensin sodium salt with 10 μM erlotinib shows the highest percentage of apoptosis (38.7%)[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.
体内研究 (In Vivo)
Although the numbers of tumors do not change substantially, a significant (P=0.0144) reduction in the average size of lesions is observed in Monensin sodium salt-treated Apc+/Min mice when compare with control animals (mean 0.199 mm2 vs. 0.299 mm2). The total tumor area estimated in one animal is decreased in individuals receiving Monensin sodium salt (mean 10.16 mm2 vs. 16.46 mm2; P=0.0125). Monensin sodium salt treatment increases the numbers of apoptotic cells and cells expressing the p21 cell-cycle inhibitor at the surface area of the neoplastic outgrowths. No changes in the cell proliferation, differentiation, and tissue architecture in the healthy parts of mucosa are noted after exposure to Monensin sodium salt[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
692.85
Formula
C36H61NaO11
CAS 号
22373-78-0
中文名称
莫能菌素钠盐
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Dayekh K, et al. Monensin inhibits epidermal growth factor receptor trafficking and activation: synergistic cytotoxicity in combination with EGFR inhibitors. Mol Cancer Ther. 2014 Nov;13(11):2559-71.
[2]. Tumova L, et al. Monensin inhibits canonical Wnt signaling in human colorectal cancer cells and suppresses tumor growth in multiple intestinal neoplasia mice. Mol Cancer Ther. 2014 Apr;13(4):812-22.
[3]. Youhua Huang, et al. Autophagy Participates in Lysosomal Vacuolation-Mediated Cell Death in RGNNV-Infected Cells. Front. Microbiol., 30 April 2020.
[4]. Ariel Savina, et al. Rab11 promotes docking and fusion of multivesicular bodies in a calcium-dependent manner. Traffic. 2005 Feb;6(2):131-43.
Cell Assay [1]
One million SCC25 cells are seeded in 10-cm plates and incubated overnight to allow for attachment and recovery. The following day, cells are pretreated with 0, 1, or 5 μM Monensin sodium salt for 24 hours then treated with 10 μM erlotinib alone or in combination with Monensin sodium salt for a further 24 hours. Adherent and cells in suspension are collected by centrifugation and fixed in 3 mL of cold 80% ethanol overnight at -20°C. Before analysis, cell pellets are washed with PBS resuspended in staining buffer containing 25 μg/mL propidium iodide and 40 μg/mL RNase A and incubated for a minimum of 1 hour in the dark at room temperature[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.
Animal Administration [2]
Multiple intestinal neoplasia (Min) mice are used in this study. Four-week-old pups are weaned, genotyped, and randomized. The animals are divided into two groups and treated with Monensin sodium salt (10 mg/kg) or vehicle (DMSO). Daily oral applications continue for 6 weeks. In addition, six pairs of Apc+/Min mice age 7, 10, 13, 16, 19, and 22 weeks are treated with Monensin sodium salt or vehicle for 5 weeks. The mice are sacrificed and the intestines are dissected, washed in PBS, and fixed in 4% formaldehyde (v/v) in PBS for 3 days. Fixed intestines are embedded in paraffin, sectioned and stained. The number and size of the neoplastic lesions are quantified using Ellipse software[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]. Dayekh K, et al. Monensin inhibits epidermal growth factor receptor trafficking and activation: synergistic cytotoxicity in combination with EGFR inhibitors. Mol Cancer Ther. 2014 Nov;13(11):2559-71.
[2]. Tumova L, et al. Monensin inhibits canonical Wnt signaling in human colorectal cancer cells and suppresses tumor growth in multiple intestinal neoplasia mice. Mol Cancer Ther. 2014 Apr;13(4):812-22.
[3]. Youhua Huang, et al. Autophagy Participates in Lysosomal Vacuolation-Mediated Cell Death in RGNNV-Infected Cells. Front. Microbiol., 30 April 2020.
[4]. Ariel Savina, et al. Rab11 promotes docking and fusion of multivesicular bodies in a calcium-dependent manner. Traffic. 2005 Feb;6(2):131-43.
SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G[1].
After a 4 hr preincubation with cathepsin L, SID 26681509 becomes more potent, demonstrating an IC50 of 1.0 nM. SID 26681509 is determined to be a slow-binding and slowly reversible competitive inhibitor. Through a transient kinetic analysis for single-step reversibility, inhibition rate constants are kon = 24,000 M-1s-1 and koff = 2.2 × 10-5 s-1 (Ki = 0.89 nM). Molecular docking studies are undertaken using the experimentally-derived X-ray crystal structure of papain/CLIK-148[1]. SID 26681509 inhibits papain and cathepsins B, K, S, and V with IC50 values determined after one hour ranging from 618 nM to 8.442 μM. SID 26681509 shows no inhibitory activity against the serine protease cathepsin G[1]. SID 26681509 inhibits cathepsin V activity with an IC50 value of 0.5 μM. SID 26681509 (1-30 μM) blocks high-mobility group box 1 (HMGB1)-induced TNF-α production dose dependently without altering cell viability[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)
SID 26681509 treatment significantly improves survival in murine models of sepsis and reduces liver damage following warm liver ischemia/reperfusion (I/R) models[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
539.65
Formula
C27H33N5O5S
CAS 号
958772-66-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
In solvent
-80°C
6 months
-20°C
1 month
参考文献
[1]. Shah PP, et al. Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L. Mol Pharmacol. 2008 Jul;74(1):34-41.
[2]. Pribis JP, et al. The HIV Protease Inhibitor Saquinavir Inhibits HMGB1-Driven Inflammation by Targeting the Interaction of Cathepsin V with TLR4/MyD88. Mol Med. 2015 Dec;21(1):749-757.
