TC-E 5003 - CAS:17328-16-4

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TC-E 5003

目录号 : KCM11975 CAS No. : 17328-16-4 纯度 : ≥98%

Data Sheet SDS 产品使用指南

TC-E 5003 is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC = 1.5 µM for human PRMT1 in a methylation assay). It is selective for PRMT1 over PRMT4/CARM1 and SET7/9 methyltransferases, with less than 5% inhibition at a concentration of 50 µM for SET7/9. TC-E 5003 inhibits growth of MCF-7a breast cancer and LNCaP prostate cancer cells (GIs = 1.97 and 4.49 µM, respectively) and decreases androgen-dependent gene transcription in vitro. TC-E 5003 (80 mg/kg) also has antimalarial properties and eradicates P. berghei in mice.

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock

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生物活性

TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC₅₀ of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers.

IC₅₀&Target

PRMT1

体外研究

TC-E 5003 (0-1 μM, 24 hours) inhibits LPS induced NO production in RAW264.7 cells.
TC-E 5003 (1 μM, 15-60 minutes) regulates LPS induced AP-1 transcriptional activity by modulating the expression of c-Jun gene in RAW264.7 cells.
TC-E 5003 (10 μM, 4 hours) enhances thermogenesis in primary iWAT cells by increasing UCP1 expression without altering mitochondrial content and activating downstream molecules involved in PKA signaling.
TC-E 5003 (6 μM, 48 hours) has a good inhibitory effect on the proliferation of cancer cells.

Real Time qPCR

Cell Line:	RAW264.7 cells
Concentration:	0-1 μM
Incubation Time:	24 hours
Result:	Significantly and dose-dependently decreased NO production without cytotoxicity in RAW264.7 cells.

Western Blot Analysis

Cell Line:	RAW264.7 cells
Concentration:	1 μM
Incubation Time:	4 hours
Result:	Led significant increase in Ucp1 mRNA and protein expressions up to 24 h in primary iWAT cells.

Cell Viability Assay

Cell Line:	A549, A549-INEI, H1299, MCF-7, and MDAMB-231 cells
Concentration:	6 μM
Incubation Time:	48 hours
Result:	Significantly inhibited the proliferation of A549, A549-INEI, H1299, MCF-7, and MDAMB-231 (77.11%, 45.44%, 80.11%, 86.77%, 71.43%) at 6.0 μM.

Real Time qPCR

Cell Line:	Primary iWAT cells
Concentration:	10 μM
Incubation Time:	4 hours
Result:	Led significant increase in Ucp1 mRNA and protein expressions up to 24 h in primary iWAT cells.

体内研究

TC-E 5003 (0.5-2.0 mg, subcutaneous injection, single dose, lasting for 28 days) has excellent tumor suppression effect in A549 tumor transplantation ICR mouse model.

Animal Model:	A549 tumor xenograft ICR mouse model
Dosage:	0.5-2.0 mg
Administration:	s.c., a single dose for 28 days
Result:	Achieved better antitumor effect in combination with INEI system in A549 tumor xenograft ICR mouse model.

分子式

C₁₆H₁₄Cl₂N₂O₄S

分子量

401.26

CAS号

17328-16-4

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

In Vitro:

DMSO : 125 mg/mL (311.52 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4921 mL	12.4607 mL	24.9215 mL
5 mM	0.4984 mL	2.4921 mL	4.9843 mL
10 mM	0.2492 mL	1.2461 mL	2.4921 mL

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。

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

1.

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

Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.18 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.18 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 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。
3.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.18 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

纯度： ≥98%

Data Sheet

SDS

产品使用指南

Kim E, et al. Protein Arginine Methyltransferase 1 (PRMT1) Selective Inhibitor, TC-E 5003, Has Anti-Inflammatory Properties in TLR4 Signaling. Int J Mol Sci. 2020;21(9):3058. Published 2020 Apr 26.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器