NI-42

目录号: HY-101121 纯度: 99.53%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

NI-42 (compound 13-d)，一种 BRPFS 正交结构的化学探针，是有偏向性的 BRPFs 的溴结构域 (BRD) 抑制剂 (IC₅₀: BRPF1/2/3=7.9/48/260 nM; K_d: BRPF1/2/3=40/210/940 nM), 与非分类 IV BRD 蛋白相比具有很好的选择性。

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NI-42 Chemical Structure

CAS No. : 1884640-99-6

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规格	价格	是否有货
1 mg	￥446	In-stock
5 mg	￥1116	In-stock
10 mg	￥1738	In-stock
25 mg	￥2900	In-stock
50 mg	￥4138	In-stock
100 mg	￥5638	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

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生物活性
纯度 & 产品资料
参考文献

生物活性

NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC₅₀s of BRPF1/2/3=7.9/48/260 nM; K_ds of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins^[1].

IC₅₀ & Target

BRPF1

7.9 nM (IC₅₀)

BRPF2

48 nM (IC₅₀)

BRPF3

260 nM (IC₅₀)

BRD9

310 nM (IC₅₀)

BRD4 (BD1)

4500 nM (IC₅₀)

BRPF1

40 nM (Kd)

BRPF2

210 nM (Kd)

BRPF3

940 nM (Kd)

BRD9

1130 nM (Kd)

BRD7

82 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
AGS	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human AGS cells after 72 hrs Growth inhibition of human AGS cells after 72 hrs	[PMID: 28068087]
ASPC1	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human AsPC1 cells after 72 hrs Growth inhibition of human AsPC1 cells after 72 hrs	[PMID: 28068087]
COLO 205	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human COLO205 cells after 72 hrs Growth inhibition of human COLO205 cells after 72 hrs	[PMID: 28068087]
CWR22R	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human 22Rv1 cells after 72 hrs Growth inhibition of human 22Rv1 cells after 72 hrs	[PMID: 28068087]
DMS-114	GI₅₀	16.6 μM Compound: 15; Nl-42	Inhibition of cell proliferation of human DMS114 cells after 72 hrs by MTS assay Inhibition of cell proliferation of human DMS114 cells after 72 hrs by MTS assay	[PMID: 28714688]
HCC1187	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human HCC1187 cells after 72 hrs Growth inhibition of human HCC1187 cells after 72 hrs	[PMID: 28068087]
HepG2	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human HepG2 cells after 72 hrs Growth inhibition of human HepG2 cells after 72 hrs	[PMID: 28068087]
Hs 766	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human Hs766T cells after 72 hrs Growth inhibition of human Hs766T cells after 72 hrs	[PMID: 28068087]
HuP-T4	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human HUPT4 cells after 72 hrs Growth inhibition of human HUPT4 cells after 72 hrs	[PMID: 28068087]
IM-9	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human IM9 cells after 72 hrs Growth inhibition of human IM9 cells after 72 hrs	[PMID: 28068087]
KG-1	GI₅₀	7 μM Compound: 13-d; NI-42	Growth inhibition of human KG1 cells after 72 hrs Growth inhibition of human KG1 cells after 72 hrs	[PMID: 28068087]
LoVo	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human LoVo cells after 72 hrs Growth inhibition of human LoVo cells after 72 hrs	[PMID: 28068087]
LS180	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human LS180 cells after 72 hrs Growth inhibition of human LS180 cells after 72 hrs	[PMID: 28068087]
MV4-11	GI₅₀	9.9 μM Compound: 13-d; NI-42	Growth inhibition of human MV4-11 cells after 72 hrs Growth inhibition of human MV4-11 cells after 72 hrs	[PMID: 28068087]
NCI-H1437	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human NCI-H1437 cells after 72 hrs Growth inhibition of human NCI-H1437 cells after 72 hrs	[PMID: 28068087]
NCI-H1703	GI₅₀	> 30 μM Compound: 15; Nl-42	Inhibition of cell proliferation of human NCI-H1703 cells after 72 hrs by MTS assay Inhibition of cell proliferation of human NCI-H1703 cells after 72 hrs by MTS assay	[PMID: 28714688]
NOMO-1	GI₅₀	4.6 μM Compound: 13-d; NI-42	Growth inhibition of human NOMO1 cells after 72 hrs Growth inhibition of human NOMO1 cells after 72 hrs	[PMID: 28068087]
NUGC-4	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human NUGC4 cells after 72 hrs Growth inhibition of human NUGC4 cells after 72 hrs	[PMID: 28068087]
OCI-AML2	GI₅₀	1.3 μM Compound: 13-d; NI-42	Growth inhibition of human OCI-AML2 cells after 72 hrs Growth inhibition of human OCI-AML2 cells after 72 hrs	[PMID: 28068087]
OCI-LY19	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human OCI-LY19 cells after 72 hrs Growth inhibition of human OCI-LY19 cells after 72 hrs	[PMID: 28068087]
RKO	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human RKO cells after 72 hrs Growth inhibition of human RKO cells after 72 hrs	[PMID: 28068087]
SK-CO-1	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human SKCO1 cells after 72 hrs Growth inhibition of human SKCO1 cells after 72 hrs	[PMID: 28068087]
SNU-5	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human SNU5 cells after 72 hrs Growth inhibition of human SNU5 cells after 72 hrs	[PMID: 28068087]
SW48	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human SW48 cells after 72 hrs Growth inhibition of human SW48 cells after 72 hrs	[PMID: 28068087]
SW-620	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human SW620 cells after 72 hrs Growth inhibition of human SW620 cells after 72 hrs	[PMID: 28068087]
SW948	GI₅₀	1 μM Compound: 13-d; NI-42	Growth inhibition of human SW948 cells after 72 hrs Growth inhibition of human SW948 cells after 72 hrs	[PMID: 28068087]
THP-1	GI₅₀	5.7 μM Compound: 13-d; NI-42	Growth inhibition of human THP1 cells after 72 hrs Growth inhibition of human THP1 cells after 72 hrs	[PMID: 28068087]

体外研究
(In Vitro)

NI-42 shows IC₅₀s of 82, 310, and 4500 nM for BRD7, BRD9, and BRD4 (BD1), respectively, and has a K_d of 1130 nM for BRD9^[1].

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

分子量

353.40

Formula

C₁₈H₁₅N₃O₃S

CAS 号

1884640-99-6

性状

固体

颜色

Off-white to pink

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 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 (282.97 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	2.8297 mL	14.1483 mL	28.2965 mL
5 mM	0.5659 mL	2.8297 mL	5.6593 mL
10 mM	0.2830 mL	1.4148 mL	2.8297 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

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 (7.07 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 (7.07 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。
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

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

纯度: 99.53%

选择批次：

Data Sheet (621 KB) SDS (393 KB)

COA (285 KB) HNMR (259 KB) LCMS (93 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Igoe N, et al. Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies. J Med Chem. 2017 Jan 26;60(2):668-680. [Content Brief]

NI-42 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8297 mL	14.1483 mL	28.2965 mL	70.7414 mL
	5 mM	0.5659 mL	2.8297 mL	5.6593 mL	14.1483 mL
	10 mM	0.2830 mL	1.4148 mL	2.8297 mL	7.0741 mL
	15 mM	0.1886 mL	0.9432 mL	1.8864 mL	4.7161 mL
	20 mM	0.1415 mL	0.7074 mL	1.4148 mL	3.5371 mL
	25 mM	0.1132 mL	0.5659 mL	1.1319 mL	2.8297 mL
	30 mM	0.0943 mL	0.4716 mL	0.9432 mL	2.3580 mL
	40 mM	0.0707 mL	0.3537 mL	0.7074 mL	1.7685 mL
	50 mM	0.0566 mL	0.2830 mL	0.5659 mL	1.4148 mL
	60 mM	0.0472 mL	0.2358 mL	0.4716 mL	1.1790 mL
	80 mM	0.0354 mL	0.1769 mL	0.3537 mL	0.8843 mL
	100 mM	0.0283 mL	0.1415 mL	0.2830 mL	0.7074 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:

NI-421884640-99-6NI42NI 42Epigenetic Reader DomainInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

NI-42

Customer Review