1. Apoptosis Autophagy
  2. c-Myc Autophagy
  3. KJ Pyr 9

KJ Pyr 9 是 MYC 的抑制剂。体外实验中, KJ Pyr 9 抑制 MYC 的 Kd 值为 6.5±1.0 nM。

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KJ Pyr 9 Chemical Structure

KJ Pyr 9 Chemical Structure

CAS No. : 581073-80-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥605
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1 mg ¥220
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5 mg ¥550
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10 mg ¥880
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50 mg ¥2640
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100 mg ¥4225
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500 mg   询价  

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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

KJ Pyr 9 is an inhibitor of MYC with a Kd of 6.5 nM in in vitro assay.

IC50 & Target

Kd: 6.5±1.0 nM (MYC)[1]

体外研究
(In Vitro)

KJ Pyr 9 (KJ-Pyr-9) 在蛋白质片段互补试验中干扰细胞中 MYC-MAX 复合物的形成[1]
KJ Pyr 9 在细胞培养中特异性抑制 MYC 诱导的致癌转化,对几种不相关的癌蛋白的致癌活性无或仅微弱影响[1]
KJ Pyr 9 优先干扰 MYC 过表达的人类和禽类细胞的增殖,并特异性地降低 MYC 驱动的转录特征[1]
KJ Pyr 9 对三种细胞系 (NCI-H460, MDA-MB-231 和 SUM-159PT) 的作用已知依赖于 MYC 活性的增加[1]
KJ pyr 9 对 IC50 值在 5-10 μM 的所有细胞系均有抑制作用[1]
KJ Pyr 9 对 c-MYC 组成型高表达的 Burkitt 淋巴瘤细胞系的增殖更敏感 (IC50 值在 1-2.5 μM 之间)[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

KJ Pyr 9 (腹腔注射;10 mg/kg;每天一次,共 31 天) 具有阻止肿瘤生长的能力[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

385.37

Formula

C22H15N3O4

CAS 号
性状

固体

颜色

Light yellow to yellow

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 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (324.36 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5949 mL 12.9745 mL 25.9491 mL
5 mM 0.5190 mL 2.5949 mL 5.1898 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

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

    Solubility: 2.5 mg/mL (6.49 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.49 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    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。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.62%

参考文献
Cell Assay
[1]

Assays used staining with the redox dye resazurin to measure cell viability. Cells are seeded at 103 per 100 μL well in 96-well plates and grown in the presence of 2.5% FBS. MDA-MB-231 cells are cultured in DMEM; SUM-159PT cells are cultured in HAM’s F12; and NCI-H460 cells are cultured in RPMI-1640. MDA-MB-231 cells are exposed to KJ Pyr 9 (KJ-Pyr-9) for 216 h with fresh compound-containing medium supplied at 120 and 192 h; SUM-159PT cells are exposed to the compound for 120 h and fresh medium with the appropriate compound concentrations is supplied at 48 h; and NCI-H460 cells are grown with compound for 72 h. Triplicate cultures of P493-6 cells are grown in six-well plates from a starting density of 1×105 cells per mL in 4 mL culture medium per well. Compounds are added immediately following cell seeding. Following compound addition, cells are distributed by vortexing the plate at 400 rpm for 10 s. One hundred-microliter samples are taken after vortexing and counted using a Beckman Coulter Z1 counter at 0, 12, 24, 36, 48, 60, 72, and 96 h of incubation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Ten 8-wk-old female nude mice (HSD:athymic nude-Foxn1nu) are injected with 5×106 MDA-MB-231 cells s.c. into the left and right flanks. Cells are suspended in high-concentration Matrigel before injection. Xenograft tumors are allowed to grow until the average volume of the tumors reached 100 mm3, as measured by external calipers. At this point, the mice are divided into two groups. One receive 10 mg/kg KJ Pyr 9 and the other receive vehicle only, dosed daily by i.p. injection. Tumor volume and mouse weight are measured daily. Vehicle used in all cases is 10:10:80 Tween 80:DMSO:5% dextrose in water. The mice are treated for a period of 31 d. At the end of the experiment, the mice are euthanized and tumors are excised. Tumors are weighed. Samples of each tumor are fixed in formalin for histology and frozen for Western blotting.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5949 mL 12.9745 mL 25.9491 mL 64.8727 mL
5 mM 0.5190 mL 2.5949 mL 5.1898 mL 12.9745 mL
10 mM 0.2595 mL 1.2975 mL 2.5949 mL 6.4873 mL
15 mM 0.1730 mL 0.8650 mL 1.7299 mL 4.3248 mL
20 mM 0.1297 mL 0.6487 mL 1.2975 mL 3.2436 mL
25 mM 0.1038 mL 0.5190 mL 1.0380 mL 2.5949 mL
30 mM 0.0865 mL 0.4325 mL 0.8650 mL 2.1624 mL
40 mM 0.0649 mL 0.3244 mL 0.6487 mL 1.6218 mL
50 mM 0.0519 mL 0.2595 mL 0.5190 mL 1.2975 mL
60 mM 0.0432 mL 0.2162 mL 0.4325 mL 1.0812 mL
80 mM 0.0324 mL 0.1622 mL 0.3244 mL 0.8109 mL
100 mM 0.0259 mL 0.1297 mL 0.2595 mL 0.6487 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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KJ Pyr 9
目录号:
HY-19735
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