Actinomycin D (Dactinomycin) inhibits DNA repair with an IC₅₀ of 0.42 μM. Actinomycin D is an autophagy activator^[1][2][3].

IC50: 0.42 μM (DNA repair)^[1]

Actinomycin D (Dactinomycin) is an inhibitor of DNA transcription and replication^[1]. Actinomycin D markedly reduces the vascular smooth muscle cells (SMC) proliferation via the inhibition of BrdU incorporation at 80 nM. This is further supported by the G1-phase arrest using a flowcytometric analysis. Actinomycin D is extremely potent with an inhibitory concentration IC₅₀ at 0.4 nM, whereas the lethal dose LD50 is at 260 microM. The protein expression levels of proliferating cell nuclear antigen (PCNA), focal adhesion kinase (FAK), and Raf are all suppressed by Actinomycin D. Extracellular signal-regulated kinases (Erk) involved in cell-cycle arrest are found to increase by Actinomycin D^[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.

The pluronic gel containing 80 nM and 80 μM Actinomycin D (Dactinomycin) is applied topically to surround the rat carotid adventitia, the thickness of neointima is substantially reduced (45 and 55%, respectively)^[2]. Mice in the Actinomycin D and NSC 118218 group lives significantly longer than the control group with P values of <0.001 and 0.007, respectively. Interestingly, single treatment with Actinomycin D is superior to NSC 118218 regarding overall survival (P=0.026)^[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.

1255.42

C₆₂H₈₆N₁₂O₁₆

50-76-0

放线菌素 D

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : ≥ 27 mg/mL (21.51 mM)

* “≥” means soluble, but saturation unknown.

*

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。-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：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.08 mg/mL (1.66 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (1.66 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: 2.08 mg/mL (1.66 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.08 mg/mL (1.66 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

• [1]. Barret JM, et al. Evaluation of DNA repair inhibition by antitumor or antibiotic drugs using a chemiluminescence microplateassay. Carcinogenesis. 1997 Dec;18(12):2441-5.

  [2]. Wu CH, et al. The molecular mechanism of actinomycin D in preventing neointimal formation in rat carotid arteries after balloon injury. J Biomed Sci. 2005;12(3):503-12.

  [3]. Merkel O, et al. Actinomycin D induces p53-independent cell death and prolongs survival in high-risk chronic lymphocytic leukemia. Leukemia. 2012 Dec;26(12):2508-16.

Actinomycin D is co-incubated for 3 h at 30°C with a reaction mixture containing: 120 mg of a whole-cell extract of HeLa cells, 70 mM KCl, 0.4 mM each of dGTP, dCTP, dATP, and digoxygenylated-dUTP in reaction buffer containing 40mM Hepes-KOH (pH 7.6), 5 mM MgCl₂, 0.5 mM Dithiotreitol, 2 mM EGTA, 10 mM phosphocreatine, 50 mg/mL creatine phosphate, and 360 mg/mL of bovine serum albumin. During this reaction, DNA damage is recognized and the excised patches are replaced by neosynthesized DNA fragments. Throughout this DNA synthesis, digoxygenylated-dUMPs are incorporated. The DNA repair reaction is stopped by three washes^[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.

Mice^[3]
The original Eμ-TCL1a transgenic mice have been backcrossed to C57BL/6 mice for >9 generations.The C57BL/6 wild-type mice are engrafted with tumor cells from Eμ-TCL-1 transgenic mice. The percentage of CD5+/CD19+ cells in the peripheral blood is routinely checked in mice by taking blood from the tail vein and analyzing it via flow cytometry. When the percentage of tumor cells in the peripheral blood reached 40-60%, treatment is started. Actinomycin D (0.06 mg/kg by 10 days) is applied daily via i.p. injections.

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.

• [1]. Barret JM, et al. Evaluation of DNA repair inhibition by antitumor or antibiotic drugs using a chemiluminescence microplateassay. Carcinogenesis. 1997 Dec;18(12):2441-5.

  [2]. Wu CH, et al. The molecular mechanism of actinomycin D in preventing neointimal formation in rat carotid arteries after balloon injury. J Biomed Sci. 2005;12(3):503-12.

  [3]. Merkel O, et al. Actinomycin D induces p53-independent cell death and prolongs survival in high-risk chronic lymphocytic leukemia. Leukemia. 2012 Dec;26(12):2508-16.