- VX-222 (VCH-222, Lomibuvir)
- Gambogic Acid
- CHM 1
- Fidaxomicin
- T 705
| Actinomycin DRNA polymerase inhibitor |
Sample solution is provided at 25 µL, 10mM.
- 1. Cao H, Yu D, et al. "Hypoxia destroys the microstructure of microtubules and causes dysfunction of endothelial cells via the PI3K/Stathmin1 pathway." Cell Biosci. 2019 Feb 18;9:20.PMID:30820314
- 2. Oladimeji PO, Wright WC, et al. "RNA interference screen identifies NAA10 as a regulator of PXR transcription." Biochem Pharmacol. 2018 Dec 16;160:92-109.PMID:30566892
- 3. Bao L, Yuan L, et al. "A FUS-LATS1/2 Axis Inhibits Hepatocellular Carcinoma Progression via Activating Hippo Pathway." Cell Physiol Biochem. 2018;50(2):437-451.PMID:30308519
- 4. Song H, Xu Y, et al. "LncRNA THOR increases the stemness of gastric cancer cells via enhancing SOX9 mRNA stability." Biomed Pharmacother. 2018 Sep 15;108:338-346.PMID:30227327
- 5. Rahnamoun H, Lee et al. "RNAs interact with BRD4 to promote enhanced chromatin engagement and transcription activation." Nat Struct Mol Biol. 2018 Aug;25(8):687-697.PMID:30076409
- 6. Caihua Wang, Yonghong Zhang, et al ."miR-204 enhances p27 mRNA stability by targeting Brd4 in head and neck squamous cell carcinoma." Oncology Letters. July 19, 2018.
- 7. WEICHENG PAN, JINHUI PANG, et al. "RNA binding protein HuR promotes osteosarcoma cell progression via suppressing the miR-142-3p/HMGA1 axis." ONCOLOGY LETTERS. 2018 May 31.
- 8. Wang X, Hu H, et al. "RNA binding protein Lin28B confers gastric cancer cells stemness via directly binding to NRP-1." Biomed Pharmacother. 2018 May 19;104:383-389.PMID:29787985
- 9. Yang L, Zhang Y, et al. "RNPC1 inhibits non-small cell lung cancer progression via regulating miR-181a/CASC2 axis." Biotechnol Lett. 2017 Dec 29.PMID:29288351
- 10. Wang Z, Pang J, et al. "RNA binding protein Lin28A promotes osteocarcinoma cells progression by associating with the long noncoding RNA MALAT1." Biotechnol Lett. 2017 Dec 4.PMID:29204769
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Quality Control & MSDS
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- Purity = 98.20%
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Chemical structure
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| Cell experiment [1]: | |
Cell lines | Rat adipocytes |
Preparation method | The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months. |
Reaction Conditions | 0, 0.1, 1 or 10 μM; 24 hrs |
Applications | Actinomycin D reduced the loss of leptin mRNA accumulation over the 24-hr incubation, exhibiting maximal inhibition at the concentration of 0.1 μM. |
| Animal experiment [2]: | |
Animal models | Wistar rats |
Dosage form | 6 μg/μL; intrahippocampally or intracerebroventricularly |
Applications | Both intrahippocampal and intracerebroventricular injection of Actinomycin D prevented a late stage of LTP in the dentate gyrus in vivo. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Fain JN, Bahouth SW. Stimulation of leptin release by actinomycin D in rat adipocytes. Biochem Pharmacol. 1998;55(8):1309-14. [2]. Frey U, Frey S, Schollmeier F, Krug M. Influence of actinomycin D, a RNA synthesis inhibitor, on long-term potentiation in rat hippocampal neurons in vivo and in vitro. J Physiol. 1996 Feb 1;490 ( Pt 3):703-11. | |
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| Cas No. | 50-76-0 | SDF | Download SDF |
| Synonyms | ActD | ||
| Chemical Name | 2-amino-4,6-dimethyl-3-oxo-1-N,9-N-bis[7,11,14-trimethyl-2,5,9,12,15-pentaoxo-3,10-di(propan-2-yl)-8-oxa-1,4,11,14-tetrazabicyclo[14.3.0]nonadecan-6-yl]phenoxazine-1,9-dicarboxamide | ||
| Canonical SMILES | CC1C(C(=O)NC(C(=O)N2CCCC2C(=O)N(CC(=O)N(C(C(=O)O1)C(C)C)C)C)C(C)C)NC(=O)C3=C4C(=C(C=C3)C)OC5=C(C(=O)C(=C(C5=N4)C(=O)NC6C(OC(=O)C(N(C(=O)CN(C(=O)C7CCCN7C(=O)C(NC6=O)C(C)C)C)C)C(C)C)C)N)C | ||
| Formula | C62H86N12O16 | M.Wt | 1255.43 |
| Solubility | ≥62.75 mg/mL in DMSO, <6.33 mg/ml="" in="" etoh,=""><6.28 mg/ml="" in="" h2o=""> | Storage | Desiccate at 4°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: Actinomycin D showed a concentration-dependent decrease of DNA repair activity with the IC50 of 0.42 μM [1].Actinomycin D (dactinomycin), a member of actinomycines, which are a class of polypeptide antibiotics isolated from soil bacteria of the genus Streptomyces. Have been used for many years as an older chemotherapy, actinomycin D binds to double- and single-stranded DNA to inhibit DNA and RNA synthesis by binding DNA at the transcription initiation complex and preventing elongation of RNA chain by RNA polymerase. In vitro: A previous study was designed to determine the effects of actinomycin D on leptin release by isolated rat adipocytes during primary culture for 24 hr. Results showed that both actinomycin D and dexamethasone reduced the loss of leptin mRNA seen over the 24-hr incubation. Maximal effects on leptin release and leptin mRNA accumulation required only 0.1 μM of actinomycin D, a concentration that had no significant effect on the 18S RNA content of adipocytes at the end of a 24-hr incubation. In contrast to the reduced loss of leptin mRNA seen at 24 hr, the loss of glyceraldehyde-3-phosphate dehydrogenase messenger ribonucleic acid (GAPDH mRNA) was enhanced in the presence of 0.1 μM of actinomycin D. These results demonstrated a unique regulation of leptin release and leptin mRNA levels by actinomycin D [2]. In vivo: A rat in vivo study showed that the effect of actinomycin D on the time course of the population spike potentiation was more pronounced than the effect on the time course of the EPSP component, suggesting different mechanisms for the two forms of potentiation. Moreover, both intrahippocampal and intracerebroventricular injection of actinomycin D prevented a late stage of LTP in the dentate gyrus in vivo measured as the population spike amplitude [3]. Clinical trial: Actinomycin is intravenously administered and most commonly used in the treatment of a variety of cancers, including gestational trophoblastic neoplasia, wilms" tumor, rhabdomyosarcoma, ewing"s sarcoma and malignant hydatidiform mole. Combined with other drugs in chemotherapy regimens, such as the VAC regimen, it will be used for treating rhabdomyosarcoma and Ewing"s Sarcoma. In addition, it is also used as a radiosensitizer in adjunct to radiotherapies, as it increases the tumor cells radiosensitivity. Reference:[1] Barret JM, Salles B, Provot C, Hill BT. Evaluation of DNA repair inhibition by antitumor or antibiotic drugs using a chemiluminescence microplate assay. Carcinogenesis. 1997 ;18(12):2441-5.[2] Fain JN, Bahouth SW. Stimulation of leptin release by actinomycin D in rat adipocytes. Biochem Pharmacol. 1998;55(8):1309-14.[3] Frey U, Frey S, Schollmeier F, Krug M. Influence of actinomycin D, a RNA synthesis inhibitor, on long-term potentiation in rat hippocampal neurons in vivo and in vitro. J Physiol. 1996;490(Pt 3):703-11.
