1. Neuronal Signaling Membrane Transporter/Ion Channel
  2. CaMK P2X Receptor
  3. KN-62

KN-62 是一种选择性的、可逆的钙调蛋白依赖性蛋白激酶 II (CaMK-II) 抑制剂,对大鼠脑 CaMK-II 的 IC50 值为 0.9 μM。KN-62 直接与 CaMK-II 酶的钙调蛋白结合位点结合。KN-62 是非竞争性的 P2X7 受体拮抗剂,IC50 约为 15 nM。

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KN-62 Chemical Structure

KN-62 Chemical Structure

CAS No. : 127191-97-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1270
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1 mg ¥363
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5 mg ¥800
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10 mg ¥1360
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50 mg ¥5500
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100 mg ¥8800
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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.

IC50 & Target[1][2]

P2X7 Receptor

 

CaMK II

0.9 μM (Ki)

体外研究
(In Vitro)

KN-62 potently antagonizes ATP-stimulated Ba2+ influx into fura-2 loaded human lymphocytes with an IC50 of 12.7 nM and complete inhibition of the flux at a concentration of 500 nM[1].
? KN-62 does not inhibit the activity of autophosphorylated Ca2+/CaM kinase II. KN-62 inhibits the Ca2+/calmodulin-dependent autophosphorylation of both alpha (50 kDa) and beta (60 kDa) subunits of Ca2+/CaM kinase II dose dependently in the presence or absence of exogenous substrate[2].
? In human leukemic B lymphocytes, KN-62 reduces the rate of permeability increase to larger permeant cations, like ethidium, induced by Bz-ATP with an IC50 of 13.1 nM[4].

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

体内研究
(In Vivo)

KN62 (5?mg/kg/day; ip; three times a week for 6 weeks) significantly reduces the liver metastatic tumor burden in five weeks old BALB/c athymic nude mice inoculated with TAMR-MCF-7 cells[3].
? KN-62 (1 μg/site, i.c.v.) prevents the antidepressant-like behavior and antidepressant-like behaviors of ZnCl2 (10 mg/kg, p.o.)[5].

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

分子量

721.84

Formula

C38H35N5O6S2

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 1 year
-20°C 6 months
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 100 mg/mL (138.53 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" 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 1.3853 mL 6.9267 mL 13.8535 mL
5 mM 0.2771 mL 1.3853 mL 2.7707 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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

  • 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

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

  • 方案 一

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

    Solubility: ≥ 2.5 mg/mL (3.46 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。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

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

    Solubility: ≥ 2.5 mg/mL (3.46 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: 99.45%

参考文献
Kinase Assay
[1]

Lymphocytes (1×107/mL) are cultured with [3H]-oleic acid (2-5 μCi/mL, specific activity 10 Ci/mmol) for 20-24 h in RPMI-1640 medium supplemented with Gentamicin (40 μg/mL), 10% heat inactivated foetal calf serum (FCS) at 37°C to label membrane phospholipids. Labelled cells are washed twice in HEPES buffered saline followed by a final wash in either HEPES buffered saline or 150 mM KCl medium containing HEPES 10 mM, pH 7.4, bovine serum albumin (BSA) 1 g/L and D-glucose 5 mM and CaCl2 1 mM. Three mL aliquots containing 1.1×10< sup>7/mL lymphocytes are warmed to 37°C and incubated with or without KN-62 or KN-04 (1 nM-500 nM) for 5 min, then 900 mL aliquots are added to 100 uL butanol (final concentration 30 mM) for a further 5 min, and stimulated with 1 mM ATP for 15 min with gentle mixing in the continued presence of inhibitor or diluent. The phospholipase D reaction is terminated by addition of 1 mL of 20 mM MgCl2 followed by centrifugation and addition of 1 mL ice cold methanol. Membrane lipids are extracted into chloroform/HCl at 4°C under N2, and separated by silica gel thin layer chromatography (t.l.c.) with the solvent system, ethyl acetate/iso-octane/acetic acid/water (13:2:3:10, v/v) under saturating conditions. Sample spots are located by autoradiography and [3H]-phosphatidylbutanol ([3H]-PBut) spots identified by an authentic standard. [3H]-PBut and [3H]-phospholipid spots are scraped into scintillant fluid (PPO in toluene, 4 g/L) and counted in a liquid scintillation counter. The quantity of [3H]-PBut is presented as a percentage of total 3H labelled-cellular phospholipids. Phospholipase D assays are performed in triplicate[1].

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

Cell Assay
[4]

All experiments are performed using adherent HEK293 cells stably transfected with cDNA encoding the human P2X7 receptor. Adherent cells on 12-well polylysine-coated plates are incubated at 37°C in 1 mL physiological salt solution (125 mM NaCl, 5 mM KCl, 1 mM MgCl2, 1.5 mM CaCl2, 25 mM NaHEPES (pH 7.5), 10 mM D-glucose, 1 mg/mL BSA). Antagonists(e.g., KN-62) are added from 1,000× stock solutions dissolved in DMSO. Cells are preincubated with antagonists (e.g., KN-62) for 15 min prior to stimulation for 10 min with 3 mM ATP (final concentration). Reactions are terminated by rapid aspiration of the extracellular medium in each well. The adherent cells in each well are then extracted overnight with 1 mL 10% HNO3. K+ content in these nitric acid extracts is assayed by atomic absorbance spectrophotometry. Duplicate or triplicate wells are run for all test conditions in each separate experiment[4].

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

Animal Administration
[5]

Mice[3]
Female Swiss mice (45-55 days old, weighing 30-45 g) are used. The following drugs are used: ZnCl2 (1 or 10 mg/kg), H-89 (1 μg/site, PKA inhibitor), KN-62 (1 μg/site, CAMKII inhibitor), chelerythrine (1 μg/site, PKC inhibitor), PD98059 (5 μg/site, MAPKK/MEK 1/2 inhibitor), U0126 (5 μg/site, MEK1/2 inhibitor), LY294002 (10 nmol/site, PI3K inhibitor), AR-A014418 (0.001 μg/site, selective GSK-3β inhibitor). ZnCl2 is dissolved in distilled water and administered orally (p.o.). H-89, KN-62, chelerythrine, PD98059, U0126, LY294002, AR-A014418 are dissolved in saline (0.9% NaCl) at a final concentration of 1% dimethyl sulfoxide (DMSO) and administered by intracerebroventricular (i.c.v.) route. The drugs are freshly prepared before treatment and administered in a volume of 10 mL/kg body weight (p.o. route) or 5 μL/site (i.c.v. route). Control animals receive the appropriate vehicle.

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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3853 mL 6.9267 mL 13.8535 mL 34.6337 mL
5 mM 0.2771 mL 1.3853 mL 2.7707 mL 6.9267 mL
10 mM 0.1385 mL 0.6927 mL 1.3853 mL 3.4634 mL
15 mM 0.0924 mL 0.4618 mL 0.9236 mL 2.3089 mL
20 mM 0.0693 mL 0.3463 mL 0.6927 mL 1.7317 mL
25 mM 0.0554 mL 0.2771 mL 0.5541 mL 1.3853 mL
30 mM 0.0462 mL 0.2309 mL 0.4618 mL 1.1545 mL
40 mM 0.0346 mL 0.1732 mL 0.3463 mL 0.8658 mL
50 mM 0.0277 mL 0.1385 mL 0.2771 mL 0.6927 mL
60 mM 0.0231 mL 0.1154 mL 0.2309 mL 0.5772 mL
80 mM 0.0173 mL 0.0866 mL 0.1732 mL 0.4329 mL
100 mM 0.0139 mL 0.0693 mL 0.1385 mL 0.3463 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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KN-62
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HY-13290
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