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Mithramycin A

Catalog No.: GC15060Purity:>98.00%Synonyms: Mithramycin A
COASDSData Sheet
Mithramycin A is an antibiotic isolated from S. grieseus. As a selective inhibitor of specific protein 1 (Sp1), Mithramycin A binds to DNA sequences rich in GC, replacing the Sp1 transcription factor that binds to oncogenes, thereby inhibiting gene expression.

المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.

Mithramycin A
Cas No.: 18378-89-7
1mgIn Stock
$69.00
1
5mgIn Stock
$266.00
1
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المراجع (Citations)

5 publicationsمنشورات الباحثين الذين استخدموا هذا المنتج

الوصف (Description)

Mithramycin A is an antibiotic isolated from S. grieseus [1]. As a selective inhibitor of specific protein 1 (Sp1), Mithramycin A binds to DNA sequences rich in GC, replacing the Sp1 transcription factor that binds to oncogenes, thereby inhibiting gene expression [2]. Mithramycin A has anti-tumor and neuroprotective effects [3].

In vitro, Mithramycin A (0-400nM, 24 hours) can dose-dependently inhibit the expression of GSTM2 protein in BFTC 905 and 5637 cells [4]. Mithramycin A (75μM; 24 hours) significantly increases the apoptosis of TNF-induced TF-1 cells, and the enhanced cytotoxicity of Mithramycin A on TNF occurs at the FADD level or its downstream position [5].

In vivo, Mithramycin A (0.2mg/kg/day; three times per week for 29 days; i.p.) significantly reduces the tumor volume of human cervical cancer cell xenograft mice and increases the number of TUNEL-positive cells in the tumor xenografts [6]. Mithramycin A (150μg/kg/day; 60 days; i.p.) treatment can effectively inhibit the Sp1 activation level in APPswe/PS1dE9 mice, significantly reduce the Aβ level and plaque load in the mouse brain, and reduce tau hyperphosphorylation, and increase synaptic markers [7].

References:
[1] Sleiman SF, Berlin J, Basso M, Karuppagounder SS, Rohr J, Ratan RR. Histone Deacetylase Inhibitors and Mithramycin A Impact a Similar Neuroprotective Pathway at a Crossroad between Cancer and Neurodegeneration. Pharmaceuticals (Basel). 2011;4(8):1183-1195.
[2] Choi ES, Nam JS, Jung JY, Cho NP, Cho SD. Modulation of specificity protein 1 by mithramycin A as a novel therapeutic strategy for cervical cancer. Sci Rep. 2014;4:7162.
[3] Sleiman SF, Langley BC, Basso M, et al. Mithramycin is a gene-selective Sp1 inhibitor that identifies a biological intersection between cancer and neurodegeneration. J Neurosci. 2011;31(18):6858-6870.
[4] Shen CH, Wu JY, Wang SC, et al. The suppressive role of phytochemical-induced glutathione S-transferase Mu 2 in human urothelial carcinoma cells. Biomed Pharmacother. 2022;151:113102.
[5] Duverger V, Murphy AM, Sheehan D, et al. The anticancer drug mithramycin A sensitises tumour cells to apoptosis induced by tumour necrosis factor (TNF). Br J Cancer. 2004;90(10):2025-2031.
[6] Choi ES, Nam JS, Jung JY, Cho NP, Cho SD. Modulation of specificity protein 1 by mithramycin A as a novel therapeutic strategy for cervical cancer. Sci Rep. 2014;4:7162.
[7] Wei C, Zhang W, Zhou Q, et al. Mithramycin A Alleviates Cognitive Deficits and Reduces Neuropathology in a Transgenic Mouse Model of Alzheimer's Disease. Neurochem Res. 2016;41(8):1924-1938.

البروتوكول (Protocol)

Cell experiment [1]:

Cell lines

 TF-1 cells

Preparation Method

 For GM-CSF withdrawal experiments, TF-1 cells were washed twice in Hank's buffered saline solution, then resuspended in RPMI 1640 medium containing 10% FCS in the presence or absence of 75nM mithramycin. For combination experiments with TNF (20ng/ml), cells were maintained in complete medium and treated with Mithramycin A simultaneously to the different drugs. Collect the cells after 24 hours of co-culture. Cell cycle status and quantification of DNA fragmentation was performed by propidium iodide (PI) staining. DNA content was determined using a FACSCalibur flow cytometer. Quantification of apoptosis by phosphatidylserine exposure was assessed by annexin V staining using the Alexa Flour 488 kit according to the manufacturer's instruction.

Reaction Conditions

 75μM; 24h

Applications

 Mithramycin A increased apoptosis in TNF-induced TF-1 cells. The enhanced cytotoxic effect of Mithramycin A on TNF was observed at the FADD level or at its downstream location.
Animal experiment [2]:

Animal models

Nude mouse (xenograft model)

Preparation Method

 KB cells were suspended in sterile PBS and injected subcutaneously into the right flank of mice. Mice were randomized into two groups containing five mice each and treated with 0.2mg/kg/day of Mithramycin A (i.p.) three times per week for 29 days. Control mice received an equal volume of vehicle. After 29 days, bodies, organs and tumors were weighed and tumor volumes determined. Tumors were measured along the two diameter axis with calibers to allow calculation of tumor volume.

Dosage form

 0.2mg/kg/day; three times per week for 29 days; i.p.

Applications

 Mithramycin A significantly reduces the tumor volume in mice with human cervical cancer cell xenografts.

References:
[1] Duverger V, Murphy AM, Sheehan D, et al. The anticancer drug mithramycin A sensitises tumour cells to apoptosis induced by tumour necrosis factor (TNF). Br J Cancer. 2004;90(10):2025-2031.
[2] Choi ES, Nam JS, Jung JY, Cho NP, Cho SD. Modulation of specificity protein 1 by mithramycin A as a novel therapeutic strategy for cervical cancer. Sci Rep. 2014;4:7162.

وثائق المنتج (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

الخصائص الكيميائية (Chemical Properties)

رقم CAS
18378-89-7
المرادفات
Mithramycin A
الاسم الكيميائي
(1S)-5-Deoxy-1-C-[(2S,3S)-7-[[2,6-dideoxy-3-O-(2,6-dideoxy--D-arabino-hexopyranosyl)--D-arabino-hexopyranosyl]oxy]-3-[(O-2,6-dideoxy-3-C-methyl--D-ribo-hexopyranosyl-(1.fwdarw.3)-O-2,6-dideoxy--D-lyxo-hexopyranosyl-(1.fwdarw.3)-2,6-dideoxy--D-arabino-hexo
SMILES
CC1C(C(CC(O1)OC2CC(OC(C2O)C)OC3=CC4=CC5=C(C(=O)C(C(C5)C(C(=O)C(C(C)O)O)OC)OC6CC(C(C(O6)C)O)OC7CC(C(C(O7)C)O)OC8CC(C(C(O8)C)O)(C)O)C(=C4C(=C3C)O)O)O)O
الصيغة الجزيئية
C52H76O24
الوزن الجزيئي
1085.16
الذوبانية
DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 10 mg/ml,PBS (pH 7.2): 2 mg/ml
التخزين
Desiccate at -20°C
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.

الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية

g/mol

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