YK-3-237

目录号: HY-19634 纯度: 99.54%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

YK-3-237 是一种 SIRT1 激活剂，靶向突变体 p53。YK-3-237 抑制三阴性乳腺癌细胞的增殖。

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YK-3-237 Chemical Structure

CAS No. : 1215281-19-8

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥867	In-stock
1 mg	￥266	In-stock
5 mg	￥1059	In-stock
10 mg	￥1825	In-stock
25 mg	￥3688	In-stock
50 mg	￥5450	In-stock
100 mg	现货	询价
200 mg	现货	询价
500 mg		询价
1 g		询价

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Customer Review

YK-3-237 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Sirtuin 亚型特异性产品:

查看所有亚型

Sirtuin SIRT1 SIRT2 SIRT3 SIRT6 SIRT5 SIRT7

生物活性
纯度 & 产品资料
参考文献

生物活性

YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells^[1].

IC₅₀ & Target^[1]

SIRT1

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
786-0	GI₅₀	0.39 μM Compound: 4	Growth inhibition of human 786-0 cells after 48 hrs by SRB assay Growth inhibition of human 786-0 cells after 48 hrs by SRB assay	[PMID: 20006519]
A10	EC₅₀	16.5 μM Compound: 4	Inhibition of tubulin in rat A10 cells assessed as induction of cellular microtubule disassembly after 18 hrs by indirect immunofluorescence technique Inhibition of tubulin in rat A10 cells assessed as induction of cellular microtubule disassembly after 18 hrs by indirect immunofluorescence technique	[PMID: 20006519]
A498	GI₅₀	4.76 μM Compound: 4	Growth inhibition of human A498 cells after 48 hrs by SRB assay Growth inhibition of human A498 cells after 48 hrs by SRB assay	[PMID: 20006519]
A549	GI₅₀	0.45 μM Compound: 4	Growth inhibition of human A549 cells after 48 hrs by SRB assay Growth inhibition of human A549 cells after 48 hrs by SRB assay	[PMID: 20006519]
ACHN	GI₅₀	0.52 μM Compound: 4	Growth inhibition of human ACHN cells after 48 hrs by SRB assay Growth inhibition of human ACHN cells after 48 hrs by SRB assay	[PMID: 20006519]
BT-549	GI₅₀	0.021 μM Compound: 4	Growth inhibition of human BT549 cells after 48 hrs by SRB assay Growth inhibition of human BT549 cells after 48 hrs by SRB assay	[PMID: 20006519]
CAKI-1	GI₅₀	6.39 μM Compound: 4	Growth inhibition of human Caki1 cells after 48 hrs by SRB assay Growth inhibition of human Caki1 cells after 48 hrs by SRB assay	[PMID: 20006519]
CCRF-CEM	GI₅₀	2.39 μM Compound: 4	Growth inhibition of human CCRF-CEM cells after 48 hrs by SRB assay Growth inhibition of human CCRF-CEM cells after 48 hrs by SRB assay	[PMID: 20006519]
COLO 205	GI₅₀	2.2 μM Compound: 4	Growth inhibition of human COLO205 cells after 48 hrs by SRB assay Growth inhibition of human COLO205 cells after 48 hrs by SRB assay	[PMID: 20006519]
DU-145	GI₅₀	0.05 μM Compound: 4	Growth inhibition of human DU145 cells after 48 hrs by SRB assay Growth inhibition of human DU145 cells after 48 hrs by SRB assay	[PMID: 20006519]
EKVX	GI₅₀	1.31 μM Compound: 4	Growth inhibition of human EKVX cells after 48 hrs by SRB assay Growth inhibition of human EKVX cells after 48 hrs by SRB assay	[PMID: 20006519]
HCC 2998	GI₅₀	0.41 μM Compound: 4	Growth inhibition of human HCC2998 cells after 48 hrs by SRB assay Growth inhibition of human HCC2998 cells after 48 hrs by SRB assay	[PMID: 20006519]
HCT-116	GI₅₀	0.37 μM Compound: 4	Growth inhibition of human HCT116 cells after 48 hrs by SRB assay Growth inhibition of human HCT116 cells after 48 hrs by SRB assay	[PMID: 20006519]
HCT-15	GI₅₀	< 0.01 μM Compound: 4	Growth inhibition of human HCT15 cells after 48 hrs by SRB assay Growth inhibition of human HCT15 cells after 48 hrs by SRB assay	[PMID: 20006519]
HOP-62	GI₅₀	0.098 μM Compound: 4	Growth inhibition of human HOP62 cells after 48 hrs by SRB assay Growth inhibition of human HOP62 cells after 48 hrs by SRB assay	[PMID: 20006519]
HOP-92	GI₅₀	0.38 μM Compound: 4	Growth inhibition of human HOP92 cells after 48 hrs by SRB assay Growth inhibition of human HOP92 cells after 48 hrs by SRB assay	[PMID: 20006519]
Hs-578T	GI₅₀	0.046 μM Compound: 4	Growth inhibition of human Hs 578T cells after 48 hrs by SRB assay Growth inhibition of human Hs 578T cells after 48 hrs by SRB assay	[PMID: 20006519]
IGROV-1	GI₅₀	0.088 μM Compound: 4	Growth inhibition of human IGROV1 cells after 48 hrs by SRB assay Growth inhibition of human IGROV1 cells after 48 hrs by SRB assay	[PMID: 20006519]
K562	GI₅₀	3.46 μM Compound: 4	Growth inhibition of human K562 cells after 48 hrs by SRB assay Growth inhibition of human K562 cells after 48 hrs by SRB assay	[PMID: 20006519]
KM12	GI₅₀	15.4 μM Compound: 4	Growth inhibition of human KM12 cells after 48 hrs by SRB assay Growth inhibition of human KM12 cells after 48 hrs by SRB assay	[PMID: 20006519]
LOX IMVI	GI₅₀	0.06 μM Compound: 4	Growth inhibition of human LOXIMVI cells after 48 hrs by SRB assay Growth inhibition of human LOXIMVI cells after 48 hrs by SRB assay	[PMID: 20006519]
M14	GI₅₀	1.19 μM Compound: 4	Growth inhibition of human M14 cells after 48 hrs by SRB assay Growth inhibition of human M14 cells after 48 hrs by SRB assay	[PMID: 20006519]
Malme-3M	GI₅₀	5.49 μM Compound: 4	Growth inhibition of human MALME-3M cells after 48 hrs by SRB assay Growth inhibition of human MALME-3M cells after 48 hrs by SRB assay	[PMID: 20006519]
MCF7	GI₅₀	0.034 μM Compound: 4	Growth inhibition of human MCF7 cells after 48 hrs by SRB assay Growth inhibition of human MCF7 cells after 48 hrs by SRB assay	[PMID: 20006519]
MCF7	IC₅₀	0.9 μM Compound: 4	Antiproliferative activity against human MCF7 cells after 24 hrs by SRB assay Antiproliferative activity against human MCF7 cells after 24 hrs by SRB assay	[PMID: 20006519]
MDA-MB-231	GI₅₀	0.11 μM Compound: 4	Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay	[PMID: 20006519]
MDA-MB-435	GI₅₀	1.95 μM Compound: 4	Growth inhibition of human MDA-MB-435 cells after 48 hrs by SRB assay Growth inhibition of human MDA-MB-435 cells after 48 hrs by SRB assay	[PMID: 20006519]
MOLT-4	GI₅₀	3.6 μM Compound: 4	Growth inhibition of human MOLT4 cells after 48 hrs by SRB assay Growth inhibition of human MOLT4 cells after 48 hrs by SRB assay	[PMID: 20006519]
NCI/ADR-RES	GI₅₀	0.05 μM Compound: 4	Growth inhibition of human NCI/ADR-RES cells after 48 hrs by SRB assay Growth inhibition of human NCI/ADR-RES cells after 48 hrs by SRB assay	[PMID: 20006519]
NCI-H226	GI₅₀	4.14 μM Compound: 4	Growth inhibition of human NCI-H226 cells after 48 hrs by SRB assay Growth inhibition of human NCI-H226 cells after 48 hrs by SRB assay	[PMID: 20006519]
NCI-H23	GI₅₀	0.14 μM Compound: 4	Growth inhibition of human NCI-H23 cells after 48 hrs by SRB assay Growth inhibition of human NCI-H23 cells after 48 hrs by SRB assay	[PMID: 20006519]
NCI-H322M	GI₅₀	8.44 μM Compound: 4	Growth inhibition of human NCI-H322M cells after 48 hrs by SRB assay Growth inhibition of human NCI-H322M cells after 48 hrs by SRB assay	[PMID: 20006519]
NCI-H460	GI₅₀	0.028 μM Compound: 4	Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay	[PMID: 20006519]
NCI-H522	GI₅₀	0.2 μM Compound: 4	Growth inhibition of human NCI-H522 cells after 48 hrs by SRB assay Growth inhibition of human NCI-H522 cells after 48 hrs by SRB assay	[PMID: 20006519]
OVCAR-3	GI₅₀	2.08 μM Compound: 4	Growth inhibition of human OVCAR-3 cells after 48 hrs by SRB assay Growth inhibition of human OVCAR-3 cells after 48 hrs by SRB assay	[PMID: 20006519]
OVCAR-4	GI₅₀	2.06 μM Compound: 4	Growth inhibition of human OVCAR4 cells after 48 hrs by SRB assay Growth inhibition of human OVCAR4 cells after 48 hrs by SRB assay	[PMID: 20006519]
OVCAR-5	GI₅₀	1.81 μM Compound: 4	Growth inhibition of human OVCAR5 cells after 48 hrs by SRB assay Growth inhibition of human OVCAR5 cells after 48 hrs by SRB assay	[PMID: 20006519]
OVCAR-8	GI₅₀	0.3 μM Compound: 4	Growth inhibition of human OVCAR8 cells after 48 hrs by SRB assay Growth inhibition of human OVCAR8 cells after 48 hrs by SRB assay	[PMID: 20006519]
PC-3	GI₅₀	0.25 μM Compound: 4	Growth inhibition of human PC3 cells after 48 hrs by SRB assay Growth inhibition of human PC3 cells after 48 hrs by SRB assay	[PMID: 20006519]
RXF 393	GI₅₀	0.39 μM Compound: 4	Growth inhibition of human RXF393 cells after 48 hrs by SRB assay Growth inhibition of human RXF393 cells after 48 hrs by SRB assay	[PMID: 20006519]
SF-268	GI₅₀	0.8 μM Compound: 4	Growth inhibition of human SF268 cells after 48 hrs by SRB assay Growth inhibition of human SF268 cells after 48 hrs by SRB assay	[PMID: 20006519]
SF-295	GI₅₀	2.73 μM Compound: 4	Growth inhibition of human SF295 cells after 48 hrs by SRB assay Growth inhibition of human SF295 cells after 48 hrs by SRB assay	[PMID: 20006519]
SF-539	GI₅₀	0.035 μM Compound: 4	Growth inhibition of human SF539 cells after 48 hrs by SRB assay Growth inhibition of human SF539 cells after 48 hrs by SRB assay	[PMID: 20006519]
SK-MEL-2	GI₅₀	3.33 μM Compound: 4	Growth inhibition of human SK-MEL-2 cells after 48 hrs by SRB assay Growth inhibition of human SK-MEL-2 cells after 48 hrs by SRB assay	[PMID: 20006519]
SK-MEL-5	GI₅₀	0.31 μM Compound: 4	Growth inhibition of human SK-MEL-5 cells after 48 hrs by SRB assay Growth inhibition of human SK-MEL-5 cells after 48 hrs by SRB assay	[PMID: 20006519]
SK-OV-3	GI₅₀	< 0.01 μM Compound: 4	Growth inhibition of human SKOV3 cells after 48 hrs by SRB assay Growth inhibition of human SKOV3 cells after 48 hrs by SRB assay	[PMID: 20006519]
SN12C	GI₅₀	0.46 μM Compound: 4	Growth inhibition of human SN12C cells after 48 hrs by SRB assay Growth inhibition of human SN12C cells after 48 hrs by SRB assay	[PMID: 20006519]
SNB-19	GI₅₀	< 0.01 μM Compound: 4	Growth inhibition of human SNB19 cells after 48 hrs by SRB assay Growth inhibition of human SNB19 cells after 48 hrs by SRB assay	[PMID: 20006519]
SR	GI₅₀	2.18 μM Compound: 4	Growth inhibition of human SR cells after 48 hrs by SRB assay Growth inhibition of human SR cells after 48 hrs by SRB assay	[PMID: 20006519]
SW-620	GI₅₀	0.037 μM Compound: 4	Growth inhibition of human SW620 cells after 48 hrs by SRB assay Growth inhibition of human SW620 cells after 48 hrs by SRB assay	[PMID: 20006519]
TK-10	GI₅₀	20.9 μM Compound: 4	Growth inhibition of human TK10 cells after 48 hrs by SRB assay Growth inhibition of human TK10 cells after 48 hrs by SRB assay	[PMID: 20006519]
U-251	GI₅₀	0.025 μM Compound: 4	Growth inhibition of human U251 cells after 48 hrs by SRB assay Growth inhibition of human U251 cells after 48 hrs by SRB assay	[PMID: 20006519]
UACC-257	GI₅₀	4.41 μM Compound: 4	Growth inhibition of human UACC257 cells after 48 hrs by SRB assay Growth inhibition of human UACC257 cells after 48 hrs by SRB assay	[PMID: 20006519]
UACC-62	GI₅₀	0.034 μM Compound: 4	Growth inhibition of human UACC62 cells after 48 hrs by SRB assay Growth inhibition of human UACC62 cells after 48 hrs by SRB assay	[PMID: 20006519]
UO-31	GI₅₀	0.32 μM Compound: 4	Growth inhibition of human UO31 cells after 48 hrs by SRB assay Growth inhibition of human UO31 cells after 48 hrs by SRB assay	[PMID: 20006519]

体外研究
(In Vitro)

YK-3-237 在亚微摩尔浓度下对大多数乳腺癌细胞系表现出抗增殖活性。YK-3-237优先抑制携带 mtp53 的乳腺癌细胞系的增殖^[1]。
YK-3-237 抑制三阴性乳腺癌 (TNBC) HS578T，MDA-MB-453、SUM1315MO2、SUM149PT、BT549、MDA-MB-231、MDA-MB-436、MDA-MB-468、HCC1937 的增殖，IC₅₀ 值为 0.160±0.043、0.241±0.086，0.253±0.028，0.289±0.066，0.353±0.017，0.431±0.136，0.501±0.062，1.436±0.754，5.031±2.010 μM^[1]。
YK-3- 237 抑制 Luminal T47D、MCF7 和 ZR-75-1 的增殖，IC₅₀ 值分别为 1.573±0.370、2.402±0.256、3.822±0.967 μM^[1]。
YK-3-237 抑制 HER2 BT474 和 SK-BR-3 的增殖，IC₅₀ 值分别为 1.249±0.372 和 0.346±0.066 μM^[1]。
YK-3-237 (0.01-10 μM；24 小时) 使 TNBC 细胞系中的 mtp53 去乙酰化^[1]。
YK-3- 237 是 Sirt1 的有效激活剂，使用 NRK-49F 细胞激活肾间质成纤维细胞^[2]。
细胞暴露于 YK-3-237 也呈剂量依赖性显著降低 α-SMA 和纤连蛋白的表达，最大抑制发生在 10 μM^[2]。

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

Cell Viability Assay^[1]

Cell Line:	BT549, MDA-MB-468, HS578T, SUM149PT
Concentration:	0, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 µM
Incubation Time:	24 hours
Result:	Reduced both the acetylation of K382 and the level of mtp53 in a dose-dependent manner in mtp53 TNBC cell lines.

分子量

372.18

Formula

C₁₉H₂₁BO₇

CAS 号

1215281-19-8

性状

固体

颜色

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 (268.69 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	2.6869 mL	13.4344 mL	26.8687 mL
5 mM	0.5374 mL	2.6869 mL	5.3737 mL
10 mM	0.2687 mL	1.3434 mL	2.6869 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 (6.72 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 (6.72 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

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: 99.54%

选择批次：

Data Sheet (634 KB) SDS (393 KB)

COA (285 KB) LCMS (94 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Yong Weon Yi, et al. Targeting mutant p53 by a SIRT1 activator YK-3-237 inhibits the proliferation of triple-negative breast cancer cells. Oncotarget. 2013 Jul;4(7):984-94. [Content Brief]

[2]. Murugavel Ponnusamy, et al. Activation of Sirtuin-1 Promotes Renal Fibroblast Activation and Aggravates Renal Fibrogenesis. J Pharmacol Exp Ther. 2015 Aug;354(2):142-51. [Content Brief]

YK-3-237 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	2.6869 mL	13.4344 mL	26.8687 mL	67.1718 mL
	5 mM	0.5374 mL	2.6869 mL	5.3737 mL	13.4344 mL
	10 mM	0.2687 mL	1.3434 mL	2.6869 mL	6.7172 mL
	15 mM	0.1791 mL	0.8956 mL	1.7912 mL	4.4781 mL
	20 mM	0.1343 mL	0.6717 mL	1.3434 mL	3.3586 mL
	25 mM	0.1075 mL	0.5374 mL	1.0747 mL	2.6869 mL
	30 mM	0.0896 mL	0.4478 mL	0.8956 mL	2.2391 mL
	40 mM	0.0672 mL	0.3359 mL	0.6717 mL	1.6793 mL
	50 mM	0.0537 mL	0.2687 mL	0.5374 mL	1.3434 mL
	60 mM	0.0448 mL	0.2239 mL	0.4478 mL	1.1195 mL
	80 mM	0.0336 mL	0.1679 mL	0.3359 mL	0.8396 mL
	100 mM	0.0269 mL	0.1343 mL	0.2687 mL	0.6717 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:

YK-3-2371215281-19-8SirtuinMutantp53mtp53deacetylationtriple-negativebreastcancerTNBCInhibitorinhibitorinhibit

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参考文献

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稀释计算器

YK-3-237 相关分类

完整储备液配制表

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YK-3-237 相关抗体:

摩尔计算器

稀释计算器

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