MALT1 inhibitor MI-2

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MALT1 inhibitor MI-2  纯度: 99.88%

MALT1 inhibitor MI-2 是一种 MALT1 抑制剂 (IC50=5.84 μM),MALT1 inhibitor MI-2 直接与 MALT1 结合,不可逆地抑制蛋白酶功能,并伴有 NF-κB 报告子活性抑制、c-REL 核定位抑制和 NF-κB 靶基因下调。MALT1 inhibitor MI-2 对动物无毒。

MALT1 inhibitor MI-2

MALT1 inhibitor MI-2 Chemical Structure

CAS No. : 1047953-91-2

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10 mM * 1 mL in DMSO ¥1210 In-stock
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50 mg ¥4800 In-stock
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生物活性

MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals[1].

IC50 & Target

IC50: 5.84 μM (MALT1)[1]

体外研究
(In Vitro)

MALT1 inhibitor MI-2 (1-1000 nM; 48 hours) selectively suppresses MALT1-dependent DLBCL cell lines, and the GI50 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells is 0.2, 0.5, 0.4, and 0.4 µM, respectively[1].
MALT1 inhibitor MI-2 (62-1000 nM; 24 hours) causes a dose-dependent decrease in MALT1-mediated cleavage[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.

Cell Proliferation Assay[1]

Cell Line: HBL-1, TMD8, OCI-Ly3, OCI-Ly10 cells
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 48 hours
Result: The GI50 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells was 0.2, 0.5, 0.4, and 0.4 µM, respectively.

Western Blot Analysis[1]

Cell Line: HBL-1 cells
Concentration: 62, 125, 250, 500, 1000 nM
Incubation Time: 24 hours
Result: Inhibits MALT1 cleavage of CYLD in HBL-1 cells.

体内研究
(In Vivo)

MALT1 inhibitor MI-2 (25 mg/kg; i.p.; daily for 14 days) profoundly suppresses the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts[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.

Animal Model: Eight-week-old male SCID NOD (bearing HBL-1 and TMD8 cells)[1]
Dosage: 25 mg/kg
Administration: Intraperitoneal injection; daily for 14 days
Result: Profoundly suppressed the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts versus vehicle.

分子量

455.72

Formula

C19H17Cl3N4O3

CAS 号

1047953-91-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 46 mg/mL (100.94 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1943 mL 10.9716 mL 21.9433 mL
5 mM 0.4389 mL 2.1943 mL 4.3887 mL
10 mM 0.2194 mL 1.0972 mL 2.1943 mL

*

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: ≥ 2.5 mg/mL (5.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.49 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% corn oil

    Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.49 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Fontan L, et al. MALT1 small molecule inhibitors specifically suppress ABC-DLBCL in vitro and in vivo. Cancer Cell. 2012 Dec 11;22(6):812-24.

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