BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell.

BCI-121 significantly inhibits SMYD3-substrate interaction and chromatin recruitment and is effective in reducing proliferation in various cancer cells types. BCI-121 significantly reduces proliferation of HT29 (by 46%) and HCT116 (by 54%) cells at 72 h and decreases the expression levels of SMYD3 target genes. SMYD3 preferentially methylates histone H4, and the presence of BCI-121 impairs SMYD3-mediated H4 in vitro methylation. Cancer cells treated with BCI-121 show a significant reduction in their growth ability and accumulated in the S phase of the cell cycle. Cells treated with BCI-121 shows a dose-dependent relationship between SMYD3 impairment and both inhibition of proliferation and reduction of targeted methyl marks (H4K5me and H3K4me2). BCI-121 shows antiproliferative properties in cancer cell lines overexpressing SMYD3 and, in general, replicated the effects of SMYD3-targeted RNAi. Experiments performed in cancer cells show that BCI-121 prevents SMYD3 recruitment on the promoters of its target genes and this event is correlated with reduced gene expression^[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.

340.22

C₁₄H₁₈BrN₃O₂

432529-82-3

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 100 mg/mL (293.93 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: ≥ 2.75 mg/mL (8.08 mM); Clear solution

  此方案可获得 ≥ 2.75 mg/mL (8.08 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 27.5 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: ≥ 2.75 mg/mL (8.08 mM); Clear solution

  此方案可获得 ≥ 2.75 mg/mL (8.08 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 27.5 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: ≥ 2.75 mg/mL (8.08 mM); Clear solution

  此方案可获得 ≥ 2.75 mg/mL (8.08 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 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Peserico A, et al. A SMYD3 Small-Molecule Inhibitor Impairing Cancer Cell Growth. J Cell Physiol. 2015 Oct;230(10):2447-2460.

Cell proliferation is determined using the cell proliferation reagent WST-1. Cells are seeded into 96-well plates one day before treatment. After 48 h, 72 h, or 96 h of BCI-121 or DMSO exposure, 10 μL of the Cell Proliferation Reagent WST-1 are added to each well and incubated at 37 °C in a humidified incubator for up to 1 h. Absorbance is measured on a microplate reader at 450/655 nm. The proliferation index is calculated as the ratio of WST-1 absorbance of treated cells to WST-1 absorbance of control 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.

• [1]. Peserico A, et al. A SMYD3 Small-Molecule Inhibitor Impairing Cancer Cell Growth. J Cell Physiol. 2015 Oct;230(10):2447-2460.

BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells^[1][2].

DUSP-MKP^[1]

BCI-215 concentration-dependently increases pERK levels in DUSP-overexpressing cells with IC₅₀ value in the micromolar range^[1].
BCI-215 (1-20 μM; 6 hours) retains fibroblast growth factor hyperactivating and cellular DUSP6/MKP-3 and DUSP1/MKP-1 inhibitory activity but is nontoxic to zebrafish embryos and an endothelial cell line^[1].
BCI-215 inhibits survival and motility of MDA-MB-231 human breast cancer cells but does not affect viability of cultured hepatocytes^[2].
BCI-215 is completely devoid of hepatocyte toxicity up to 100 µM^[2].
BCI-215 does not generate ROS in hepatocytes or in developing Zebrafish larvae. BCI-215 (22 µM) has antimigratory and proapoptotic activities in breast cancer cells that correlate with induction of ERK phosphorylation^[2].
BCI-215 (20 µM; 1 hour) induces mitogenic and stress signaling in cancer cells without generating ROS^[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.

396.32

C₂₂H₂₂BrNO

1245792-67-9

Room temperature in continental US; may vary elsewhere.

DMSO : 33.33 mg/mL (84.10 mM; Need ultrasonic)

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: ≥ 0.83 mg/mL (2.09 mM); Clear solution

  此方案可获得 ≥ 0.83 mg/mL (2.09 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 8.3 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% corn oil

  Solubility: ≥ 0.83 mg/mL (2.09 mM); Clear solution

  此方案可获得 ≥ 0.83 mg/mL (2.09 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 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Korotchenko VN, et al. In vivo structure-activity relationship studies support allosteric targeting of a dual specificity phosphatase. Chembiochem. 2014 Jul 7;15(10):1436-45.

  [2]. Kaltenmeier CT, et al. A Tumor Cell-Selective Inhibitor of Mitogen-Activated Protein Kinase Phosphatases Sensitizes Breast Cancer Cells to Lymphokine-Activated Killer Cell Activity. J Pharmacol Exp Ther. 2017 Apr;361(1):39-50.

BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC₅₀s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5^[1].

317.42

C₂₂H₂₃NO

1245792-51-1

Room temperature in continental US; may vary elsewhere.

DMSO : 125 mg/mL (393.80 mM; Need ultrasonic)

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: 2.08 mg/mL (6.55 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.08 mg/mL (6.55 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 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% corn oil

  Solubility: ≥ 2.08 mg/mL (6.55 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (6.55 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Korotchenko VN, et al. In vivo structure-activity relationship studies support allosteric targeting of a dual specificity phosphatase. Chembiochem. 2014 Jul 7;15(10):1436-45.