Ochromycinone ((Rac)-STA-21) is a natural antibiotic and a STAT3 inhibitor. Ochromycinone can inhibits STAT3 DNA binding activity, STAT3 dimerization. Ochromycinone has anticancer and antimicrobial activity[1][2].
IC50 & Target[2]
STAT3
体外研究 (In Vitro)
STA-21 inhibits STAT3 DNA binding activity, STAT3 dimerization, and STAT3-dependent luciferase activity. Moreover, STA-21 reduces the survival of breast carcinoma cells with constitutive STAT3 signaling but has minimal effect on the cells in which constitutive STAT3 signaling is absent[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
306.31
Formula
C19H14O4
CAS 号
111540-00-2
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Song H, et al. A low-molecular-weight compound discovered through virtual database screening inhibits Stat3 function in breast cancer cells. Proc Natl Acad Sci U S A. 2005 Mar 29;102(13):4700-5.
[2]. Nataliya I. Kalinovskaya, et al. New Angucyclinones from the Marine Mollusk Associated Actinomycete Saccharothrix espanaensis An 113. Natural product communications. 2008, 3(10):1611-1616.
(Rac)-Arnebin 1 ((Rac)-β,β-Dimethylacrylalkannin) is the racemate of β,β-Dimethylacrylalkannin and/or β,β-Dimethylacrylshikonin. β,β-Dimethylacrylalkannin and β,β-Dimethylacrylshikonin are napthoquinones isolated from Arnebia nobilis. β,β-Dimethylacrylshikonin has anti-tumor activity[1].
分子量
370.40
Formula
C21H22O6
CAS 号
5162-01-6
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]. Zeng Z, et al. Arnebin-1 promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. Int J Mol Med. 2015 Sep;36(3):685-97.
Tetrahydrobiopterin ((Rac)-Sapropterin) is a cofactor of the aromatic amino acid hydroxylases enzymes and also acts as an essential cofactor for all nitric oxide synthase (NOS) isoforms.
IC50 Target
Human Endogenous Metabolite
;
体外研究 (In Vitro)
MicMicroglial cell cultures under hyperoxia are supplemented or not with an effective dose of Tetrahydrobiopterin (BH4) (100 μM). Exposure of microglial cells to hyperoxia-induced oxidative stress for 24 h reveals a robust increase in TSP-1 mRNA expression and protein compare to normoxia (21% O2). Tetrahydrobiopterin supplementation significantly prevents hyperoxia-induced microglial activation by diminishing Iba-1 and TSP-1 expression and prevents microvascular injury in choroidal explants[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
To assess the levels of Tetrahydrobiopterin in the retina, three to five pools of retinas are collected from WT and hph-1mice at postnatal age 7, 14, and 22 and evaluated by LC-MS/MS. LC-MS/MS analysis confirm a significant decrease by approximately 90% in the concentration levels of Tetrahydrobiopterin in retinal tissue from hph-1 mice (0.0009±0.0006; p<0.0001, 0.01±0.001; p<0.0001 and 2.45±0.40; p<0.005) compare to the WT group (0.014±0.001, 0.092±0.01, and 23.13±6.44) at P7, P14, and P22, respectively[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
241.25
Formula
C9H15N5O3
CAS 号
17528-72-2
中文名称
四氢生物蝶呤;沙丙蝶呤
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Rivera JC, et al. Tetrahydrobiopterin (BH4) deficiency is associated with augmented inflammation and microvascular degeneration in the retina. J Neuroinflammation. 2017 Sep 6;14(1):181.
Kinase Assay [1]
Microglia cell line (SIM-A9) is used and cultured. Briefly, microglial cells (800, 000 cells per well) are cultured in 6-well plates with DMEM/F12 (1:1) supplementing with 10% fetal bovine serum (FBS), 5% of horse serum (HS), and 1% penicillin/streptomycin. After 24 h, the cells are starved with DMEM/F12 (1:1) free of FBS and HS for 6 h. Then, microglial cells cultures in presence or absence of 100 μM of Tetrahydrobiopterin are exposed to hyperoxia (75% oxygen and 25% nitrogen) in a modular incubator chamber and maintained in a humidified CO2 incubator at 37 °C for 24 h. Microglial cells in matching controls are incubated at 37 °C in an incubator with 95% air and 5% CO2 and collected at the same time point. Cell lysates are quickly processed for RNA. The conditioning media is stored at -80 and later used in choroidal explant assay[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [1]
Mice pups are exposed with their mothers in a 75% oxygen environment from postnatal day 7 to P9 using oxycycler to induce retinal vaso-obliteration (VO). Animals are anesthetized and injected intravitreally at P7 with 100 μM of Tetrahydrobiopterin or vehicle (sterile PBS 1×) using a syringe equipped with 50-gauge glass capillary. At P9, mice pups are sacrificed and retinas are dissected and stained overnight at 4 °C with fluorescein-labeled Griffonia Simplicifolia Lectin 1 (GSL 1), isolectin B4 (1:100) with 1 mM CaCl2 in PBS. Quantification of VO is assessed using the computer software[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Rivera JC, et al. Tetrahydrobiopterin (BH4) deficiency is associated with augmented inflammation and microvascular degeneration in the retina. J Neuroinflammation. 2017 Sep 6;14(1):181.
(Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
分子量
302.28
Formula
C16H14O6
CAS 号
69097-99-0
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Arya A, et al. Bioflavonoid hesperetin overcome bicalutamide induced toxicity by co-delivery in novel SNEDDS formulations: Optimization, in vivo evaluation and uptake mechanism. Mater Sci Eng C Mater Biol Appl. 2017 Feb 1;71:954-964
[2]. Liu D, et al. Inhibitory Effect of Hesperetin and Naringenin on Human UDP-Glucuronosyltransferase Enzymes: Implications for Herb-Drug Interactions. Biol Pharm Bull. 2016;39(12):2052-2059.
[3]. Shagirtha K, et al. Neuroprotective efficacy of hesperetin against cadmium induced oxidative stress in the brain of rats. Toxicol Ind Health. 2016 Nov 1. pii: 0748233716665301
[4]. Li Q, et al. Hesperetin Induces Apoptosis in Human Glioblastoma Cells via p38 MAPK Activation. Nutr Cancer. 2019 Jul 11:1-8.
(Rac)-Byakangelicin is a racemate of Byakangelicin mainly isolated from the genus Angelica. Byakangelicin is an aldose-reductase inhibitor with an IC50 value of 6.2 μM[1].
分子量
334.32
Formula
C17H18O7
CAS 号
19573-01-4
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]. A. Douglas Kinghorn, et al. Progress in the Chemistry of Organic Natural Products. 2019, volume 108.
[1]. Arya JS, et al. Exploring Mitochondria-Mediated Intrinsic Apoptosis by New Phytochemical Entities: An Explicit Observation of Cytochrome c Dynamics on Lung and Melanoma Cancer Cells. J Med Chem. 2019 Sep 12;62(17):8311-8329.
Isoanthricin ((Rac)-Deoxypodophyllotoxin) is the racemate of Deoxypodophyllotoxin. Deoxypodophyllotoxin is a potent antitumor and anti-inflammatory agent[1][2].
分子量
398.41
Formula
C22H22O7
CAS 号
69222-20-4
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]. Khaled M, et, al. Deoxypodophyllotoxin: a promising therapeutic agent from herbal medicine. J Ethnopharmacol. 2013 Aug 26;149(1):24-34.
[2]. Kozawa M, et, al. [Chemical components of the roots of Anthriscus sylvestris Hoffm. I. Structures of an acyloxycarboxylic acid and a new phenylpropanoidester, anthriscusin (author’s transl)]. Yakugaku Zasshi. 1978 Nov;98(11):1486-90.
[1]. Gao Y, Xing J, et al. Trp(56) of rac1 specifies interaction with a subset of guanine nucleotide exchange factors [published correction appears in J Biol Chem. 2005 Jan 14;280(2):1704]. J Biol Chem. 2001;276(50):47530-47541.