2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. WDR5-IN-1

WDR5-IN-1 是一种有效的选择性 WD 重复结构域 5 (WDR5) 抑制剂，Kd 为 <0.02 nM。WDR5-IN-1 抑制 MLL1 组蛋白甲基转移酶活性 (HMT)，IC50为 2.2 nM。WDR5-IN-1 减少 WDR5 移位基因的 MYC 募集，并在 CHP-134 (神经母细胞瘤) 和 Ramos (Burkitt淋巴瘤) 细胞系中显示出有效的抗增殖作用。

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WDR5-IN-1 Chemical Structure

WDR5-IN-1 Chemical Structure

CAS No. : 2408842-51-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥5660
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1 mg ￥2000
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5 mg ￥5000
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WDR5-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHP-134 GI50
0.26 μM
Compound: 16
Antiproliferative activity against human CHP134 cells expressing wild type p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
Antiproliferative activity against human CHP134 cells expressing wild type p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
[PMID: 31858797]
Daudi GI50
0.58 μM
Compound: 16
Antiproliferative activity against human Daudi cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
Antiproliferative activity against human Daudi cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
[PMID: 31858797]
K562 GI50
8000 nM
Compound: 16
Antiproliferative activity against human K562 cells assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay
Antiproliferative activity against human K562 cells assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay
[PMID: 31858797]
K562 GI50
8000 nM
Compound: 1
Anti-proliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titre Glo luminescent assay
Anti-proliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titre Glo luminescent assay
[PMID: 35436124]
MOLM-13 GI50
78 nM
Compound: 16
Antiproliferative activity against human MOLM13 cells expressing wild type p53 assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay
Antiproliferative activity against human MOLM13 cells expressing wild type p53 assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay
[PMID: 31858797]
MOLM-13 GI50
78 nM
Compound: 1
Anti-proliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titre Glo luminescent assay
Anti-proliferative activity against human MOLM-13 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titre Glo luminescent assay
[PMID: 35436124]
MV4-11 GI50
38 nM
Compound: 16
Antiproliferative activity against human MV4-11 cells expressing wild type p53 assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay
Antiproliferative activity against human MV4-11 cells expressing wild type p53 assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay
[PMID: 31858797]
MV4-11 GI50
38 nM
Compound: 1
Anti-proliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titre Glo luminescent assay
Anti-proliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 5 days by Cell Titre Glo luminescent assay
[PMID: 35436124]
Raji GI50
1.2 μM
Compound: 16
Antiproliferative activity against human Raji cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
Antiproliferative activity against human Raji cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
[PMID: 31858797]
Ramos GI50
0.49 μM
Compound: 16
Antiproliferative activity against human Ramos cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
Antiproliferative activity against human Ramos cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
[PMID: 31858797]
SW480 GI50
> 22 μM
Compound: 16
Antiproliferative activity against human SW480 cells assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
Antiproliferative activity against human SW480 cells assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
[PMID: 31858797]
SW-620 GI50
3.2 μM
Compound: 16
Antiproliferative activity against human SW620 cells assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
Antiproliferative activity against human SW620 cells assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
[PMID: 31858797]
体外研究
(In Vitro)

WDR5-IN-1 (1 μM；48 小时) 显示 G2M 期细胞明显减少[1]。
WDR5-IN-1 (0.01-3 μM；24-48 小时) 增加 p53 和 p21 蛋白水平[1]。WDR5-IN-1 在 MYC 驱动的癌症 (CHP-134、Ramos、Raji、Daudi、SW620、SW480 细胞) 中表现出抗增殖活性，GI50 范围为 0.26-3.2 μM[1]。

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

WDR5-IN-1 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MV4:11 cells
Concentration: 1 µM
Incubation Time: 48 hours
Result: Showed an approximate 4 fold increased SubG1 cells.

Western Blot Analysis[1]

Cell Line: MV4:11 cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 µM
Incubation Time: 24, 48 hours
Result: p53 and p21 protein levels started to increase from 8 h post treatment of compound 16 at 300 nM and continued to elevate up to 32 h.
分子量

514.59

Formula

C30H31FN4O3
CAS 号
性状

固体

颜色

Light yellow to brown

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 (194.33 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 1.9433 mL 9.7165 mL 19.4329 mL
5 mM 0.3887 mL 1.9433 mL 3.8866 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 (4.86 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.86 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    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。
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

WDR5-IN-1 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 1.9433 mL 9.7165 mL 19.4329 mL 48.5824 mL
5 mM 0.3887 mL 1.9433 mL 3.8866 mL 9.7165 mL
10 mM 0.1943 mL 0.9716 mL 1.9433 mL 4.8582 mL
15 mM 0.1296 mL 0.6478 mL 1.2955 mL 3.2388 mL
20 mM 0.0972 mL 0.4858 mL 0.9716 mL 2.4291 mL
25 mM 0.0777 mL 0.3887 mL 0.7773 mL 1.9433 mL
30 mM 0.0648 mL 0.3239 mL 0.6478 mL 1.6194 mL
40 mM 0.0486 mL 0.2429 mL 0.4858 mL 1.2146 mL
50 mM 0.0389 mL 0.1943 mL 0.3887 mL 0.9716 mL
60 mM 0.0324 mL 0.1619 mL 0.3239 mL 0.8097 mL
80 mM 0.0243 mL 0.1215 mL 0.2429 mL 0.6073 mL
100 mM 0.0194 mL 0.0972 mL 0.1943 mL 0.4858 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:

WDR5-IN-12408842-51-1Histone MethyltransferaseApoptosisMYCproliferativelymphomaneuroblastomaapoptosiscycleturmorigenesischromatin,Inhibitorinhibitorinhibit

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