2. NF-κB JAK/STAT Signaling Stem Cell/Wnt Epigenetics Protein Tyrosine Kinase/RTK
  3. IKK JAK
  4. BMS-066

BMS-066 是 IKKβ/Tyk2 的抑制剂，其 IC50 值分别为 9 nM，72 nM。

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BMS-066 Chemical Structure

BMS-066 Chemical Structure

CAS No. : 914946-88-6

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BMS-066 相关抗体

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IKK-α IKK-β IKK IKKε TBK1

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JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.

IC50 & Target[1][2]

IKKβ

9 nM (IC50)

Tyk2

72 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
PBMC IC50
150 nM
Compound: 4m, BMS-066
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release treated for 5 mins before LPS challenge measured after 4 hrs by ELISA
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release treated for 5 mins before LPS challenge measured after 4 hrs by ELISA
[PMID: 22018461]
体外研究
(In Vitro)

BMS-066 is shown to inhibit IKKβ-catalyzed phosphorylation of IKKβ in vitro with an IC50 of 9 nM and is more than 500-fold selective for IKKβ over the closely related IKKα. To understand the selectivity on a more comprehensive scale, BMS-066 is assayed against 155 additional kinases at 10 μM, and only six of these kinases are inhibited more than 75%. This indicates that BMS-066 is more than 400-fold selective for IKKβ over more than 95% of the kinases tested. For the six kinases showing more than 75% inhibition at 10 μM, IC50 values are determined in dose-response assays and BMS-066 is shown to be more than 30-fold selective against even the next most potently inhibits kinase (Brk). BMS-066 inhibits LPS-stimulated cytokine production in human peripheral blood mononuclear cells, both at the protein and message level, with IC50 values of approximately 200 nM against these endpoints. BMS-066 inhibits the IKKβ-catalyzed phosphorylation of IkBα in LPS stimulated cells with a similar IC50 value[1]. BMS-066 shows IC50 values of 72 and 1020 nM against the Tyk2 pseudokinase domain probe displacement and IL-23-stimulated reporter assays, respectively[2].

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

BMS-066 相关抗体:
体内研究
(In Vivo)

Once daily oral doses of 5 and 10 mg/kg starting at the time of adjuvant injection on day 1 significantly reduces paw swelling compared with vehicle-treated rats at the end of the study, with the high dose showing nearly complete suppression. The talocrural (ankle) joint space is narrowed. Inflammatory exudates containing neutrophils and cell debris are also evident within the joint space. The joints from animals receiving 10 mg/kg BMS-066 are normal or show minimal changes in both inflammation and bone resorption. Clear reduction of inflammation is also evident in the low dose of BMS-066 (5 mg/kg) and the bone resorption seems to be more focal and less severe compared with the control. Microcomputed tomography of the hind limbs also show that BMS-066 provides a dose-dependent protection against the pitting, loss of bone mass, woven porous bone, and fusion of the small bones evident in the rats. Bone density measurements also show a clear dose-dependent benefit of treatment with BMS-066. Serum drug level measurements in satellite animals on the first day of dosing show that a single dose provides coverage for approximately 3 h (6 h daily with twice daily dosing) of the mouse whole-blood IC50 value against LPS-induced TNF-α. It is also showed that IKKβ inhibitors suppress TNF-α and IL-1β production within these tissues in experimental arthritis model[1].

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

379.42

Formula

C19H21N7O2
CAS 号
性状

固体

颜色

Off-white to light 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 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (263.56 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 2.6356 mL 13.1780 mL 26.3560 mL
5 mM 0.5271 mL 2.6356 mL 5.2712 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, 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。

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.59 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。

    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；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 (6.59 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。

    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。

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

只
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
参考文献
Cell Assay
[1]

When measuring the inhibition by BMS-066 of the phosphorylation of IkBα in human PBMCs, cells at a density of 1×107 per mL in RPMI 1640 medium supplemented with 10% FBS are preincubated for 30 min BMS-066 at 37°C. Cells are then stimulated for 5 min with LPS (100 ng/mL) and pelleted by rapid centrifugation; the pellets are solubilized by use of ice-cold 10×cell lysis buffer. To measure effects on transcription, human PBMCs are plated on 24-well plates at a density of 3×106 cells/well in RPMI 1640 medium plus 10% FBS and HEPES with varying concentrations of BMS-066 (0-10 μM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats, Mice[1]
Male Lewis rats (225 g) are used. Vehicle (0.02 N HCl) or BMS-066 in vehicle is administered by oral gavage beginning on the day of adjuvant challenge. Eight animals are included in each treatment group. Male Lewis rats (250 g) are immunized intraperitoneally with 200 μg/rat of keyhole limpet hemocyanin diluted in phosphate-buffered saline. BMS-066 in 0.02 N HCl is administered by oral gavage once daily beginning on the day of immunization. Blood samples were collected on day 7 and on day 14 under isoflurane anesthesia. Male DBA/1 mice (20-25 g) are immunized with 200 μg/mouse of bovine type II collagen in 0.1 mL at the base of the tail on day 0 and on day 21. Vehicle (0.02 N HCl) or BMS-066 in vehicle is administered by oral gavage twice daily beginning on day 21. Mice were monitored after the second immunization for the development of paw inflammation. Each paw was individually scored as follows: 0, normal; 1, one or more swollen digits; 2, mild paw swelling; 3, moderate paw swelling; 4, fusion of joints/ankylosis[1].

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

BMS-066 相关分类

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, 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6356 mL 13.1780 mL 26.3560 mL 65.8900 mL
5 mM 0.5271 mL 2.6356 mL 5.2712 mL 13.1780 mL
10 mM 0.2636 mL 1.3178 mL 2.6356 mL 6.5890 mL
15 mM 0.1757 mL 0.8785 mL 1.7571 mL 4.3927 mL
20 mM 0.1318 mL 0.6589 mL 1.3178 mL 3.2945 mL
25 mM 0.1054 mL 0.5271 mL 1.0542 mL 2.6356 mL
30 mM 0.0879 mL 0.4393 mL 0.8785 mL 2.1963 mL
40 mM 0.0659 mL 0.3295 mL 0.6589 mL 1.6473 mL
50 mM 0.0527 mL 0.2636 mL 0.5271 mL 1.3178 mL
60 mM 0.0439 mL 0.2196 mL 0.4393 mL 1.0982 mL
80 mM 0.0329 mL 0.1647 mL 0.3295 mL 0.8236 mL
100 mM 0.0264 mL 0.1318 mL 0.2636 mL 0.6589 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.

Keywords:

BMS-066914946-88-6BMS066BMS 066IKKJAKIκB kinaseI kappa B kinase Janus kinaseInhibitorinhibitorinhibit

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