I3MT-3 - CAS:459420-09-8

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I3MT-3 (Synonyms:HMPSNE)

目录号 : KM10519 CAS No. : 459420-09-8 纯度 : 98%

Data Sheet 产品使用指南

I3MT-3 (HMPSNE) 是有效、选择性和具有细胞膜渗透性的 3-巯基丙酮酸硫转移酶 (3MST) (IC₅₀=2.7 μM) 的抑制剂，对其他硫化氢/磺胺制硫酶没有活性。I3MT-3 靶向位于 3MST 活性位点的过硫半胱氨酸残基。

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10mg		In-stock
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50mg		In-stock
100mg	询价	In-stock

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生物活性

I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC₅₀=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes. I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST.

体外研究

I3MT-3 (1 μM) is selective for 3MST and shows a high inhibitory activity (80–90%) even at 10 μM in cell lysate of 3MST-overexpressing HEK293 cells. Besides, it is almost inactive towards the other two H2S-producing enzymes even at 100 μM.
I3MT-3 (1 μM) shows a high selectivity for 3MST, it completely suppresses the 3MST activity in COS7 cells living cells.
I3MT-3 produces a concentration-dependent inhibition of the AzMC (the fluorescent H2S probe) signal when incubated with purified human recombinant enzyme, the inhibition of the catalytic activity of 3-MST produces a concentration-dependent inhibition of H2S production with an IC₅₀ of 13.6 µM.
I3MT-3 shows a dose-dependent inhibition of 3-MST activity from CT26 homogenates, which contain the murine form of the enzyme. The IC₅₀ of HMPSNE for murine 3-MST is calculated as 2.3 µM with a cozncentration-dependent decrease of AzMC fluorescence.
I3MT-3 (10 µM-100 µM; after 3 h probe AzMC) causes a partial inhibition of the signal, while at 100 µM, HMPSNE causes a complete inhibition of the AzMC-guided H2S fluorescence at 100 µM, Additionally, HMPSNE is capable of inhibiting its target in situ in CT26 cells (with an IC₅₀ of approximately 30 µM).
I3MT-3 (0-300 μM; 5-50 hours) does not enhance MTT conversion at 10 µM, while at 100 and 300 µM it produces an inhibitory response, without increasing the LDH signal, i.e., without inducing any detectable degree of cell necrosis. It also produces a decreased oxygen consumption rate (OCR) profiles in CT26 cells.
I3MT-3 (0-300 μM; 48 hours) inhibits CT26 cells proliferate with increasing concentrations of I3MT-3. Confluence of cells treated with HMPSNE is recorded each hour for 48 h by the IncuCyte method.

Cell Proliferation Assay

Cell Line:	CT26 cells
Concentration:	0 μM; 10 μM; 30 μM; 100 μM; 300 μM
Incubation Time:	48 hours
Result:	Slowed down proliferation of CT26 cells.

分子式

C₁₇H₁₄N₂O₂S

分子量

310.37

CAS号

459420-09-8

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

In Vitro:

DMSO : 125 mg/mL (402.75 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2220 mL	16.1098 mL	32.2196 mL
5 mM	0.6444 mL	3.2220 mL	6.4439 mL
10 mM	0.3222 mL	1.6110 mL	3.2220 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 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (6.70 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.70 mM) 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 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。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.70 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.70 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。