ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation^[1].

ITSA1 (50 μM; A549 cells) treatment serves to revert the TSA-arrested population to a normal cell cycle distribution. ITSA1 is also able to effect cell cycle rescue over longer duration^[1].
ITSA1 (50 μM; 5 hours; A549 cells) treatment reduces the number of apoptosis in TSA-treated cells^[1].
ITSA1 (50 μM; 2 hours; A549 and murine ES cells cells) treatment suppresses TSA-induced histone acetylation. Importantly, suppression of acetylation levels is only observable when ITSA1 is added concurrent with or post TSA treatment^[1].
ITSA1 (50 μM; 30 minutes; murine ES cells cells) suppresses TSA-activated transcription in murine ES cells^[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.

ITSA-1 (0.5 mg/kg; intraperitoneal injection; 3 times/week; for 8 weeks; CBS^+/− mice) treatment balances deacetylation activity and suppresses IL-6 and TNF-α expression and thereby attenuated histone acetylationdependent infammatory signaling^[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.

292.12

C₁₃H₇Cl₂N₃O

200626-61-5

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 32 mg/mL (109.54 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。

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: ≥ 2.5 mg/mL (8.56 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.56 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 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: 2.5 mg/mL (8.56 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (8.56 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 25.0 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
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (8.56 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.56 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Koeller KM et al. Chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histoneand tubulin acetylation. Chem Biol. 2003 May;10(5):397-410.

  [2]. Behera J, et al. Hydrogen Sulfide Promotes Bone Homeostasis by Balancing Inflammatory Cytokine Signaling in CBS-Deficient Mice through an Epigenetic Mechanism. Sci Rep. 2018 Oct 15;8(1):15226.