TPCK (Synonyms: L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK)

目录号: HY-124379 纯度: 98.49%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) 是一种有效的丝氨酸蛋白酶抑制剂，也是 PDK1/Akt 通路的抑制剂。TPCK 能够修饰活角质形成细胞中的 E7 蛋白。TPCK 可诱导细胞凋亡，抑制肿瘤增殖，减少大鼠幼崽缺氧缺血性脑损伤，影响炎症大鼠的血管通透性。

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TPCK Chemical Structure

CAS No. : 402-71-1

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥253	In-stock
5 mg	￥230	In-stock
10 mg	￥350	In-stock
25 mg	￥500	In-stock
50 mg	￥735	In-stock
100 mg	￥1103	In-stock
200 mg		询价
500 mg		询价

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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

•Int J Biol Macromol. 2022 Nov 30;S0141-8130(22)02836-7. [Abstract]

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生物活性
纯度 & 产品资料
参考文献

生物活性

TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is an effective serine protease inhibitor and also a blocker of the PDK1/Akt pathway. TPCK can modify the E7 protein in actively keratinocyte cells. TPCK can induce cellular apoptosis, suppress tumor growth, reduce hypoxic-ischemic brain injury in rat pups, and affect vascular permeability in inflamed rats^[1]^[2]^[3]^[4]^[5].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	10.8 μM Compound: TPCK	Inhibition of TNFalpha-induced NFkappaB (unknown origin) activation expressed in HEK293 cells after 6 hrs by luciferase reporter gene assay Inhibition of TNFalpha-induced NFkappaB (unknown origin) activation expressed in HEK293 cells after 6 hrs by luciferase reporter gene assay	[PMID: 23316950]
HEK293	IC₅₀	3.76 μM Compound: TPCK	Inhibition of TNF-alpha-induced NFkappaB activation in human HEK293 cells after 6 hrs by luciferase reporter gene assay Inhibition of TNF-alpha-induced NFkappaB activation in human HEK293 cells after 6 hrs by luciferase reporter gene assay	[PMID: 21261296]
HEK293	IC₅₀	3.8 μM Compound: TPCK	Cytotoxicity against human HEK293 cells assessed as cell survival by SRB assay Cytotoxicity against human HEK293 cells assessed as cell survival by SRB assay	[PMID: 23316950]
HEK293	IC₅₀	3.8 μM Compound: TPCK	Inhibition of TNF-alpha-activated NFkappaB (unknown origin) transfected in HEK293 cells after 6 hrs by luciferase reporter gene assay Inhibition of TNF-alpha-activated NFkappaB (unknown origin) transfected in HEK293 cells after 6 hrs by luciferase reporter gene assay	[PMID: 27196335]
HEK293	IC₅₀	3.8 μM Compound: TPCK	Inhibition of TNFalpha-induced NF-kappaB activity (unknown origin) transfected in HEK293 cells after 6 hrs by luciferase reporter gene assay Inhibition of TNFalpha-induced NF-kappaB activity (unknown origin) transfected in HEK293 cells after 6 hrs by luciferase reporter gene assay	[PMID: 26343828]
HEK293	IC₅₀	3.8 μM Compound: TPCK	Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay	[PMID: 24992702]
HEK293	IC₅₀	3.8 μM Compound: TPCK	Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay Inhibition of TNF-alpha-induced NF-kappaB activity in HEK293 cells after 6 hrs by luciferase reporter gene assay	[PMID: 24533857]
HEK293	IC₅₀	3.8 μM Compound: TPCK	Inhibition of TNFalpha-induced NF-kappaB activity expressed in human HEK 293 cells after 6 hrs by luciferase reporter gene assay Inhibition of TNFalpha-induced NF-kappaB activity expressed in human HEK 293 cells after 6 hrs by luciferase reporter gene assay	[PMID: 22850207]
HEK293	IC₅₀	3.8 μM Compound: TPCK	Inhibition of TNFalpha-induced nuclear factor-kappa-B activation in human HEK293 cells at by luciferase reporter gene assay Inhibition of TNFalpha-induced nuclear factor-kappa-B activation in human HEK293 cells at by luciferase reporter gene assay	[PMID: 23994869]
HEK293	IC₅₀	4.9 μM Compound: N-tosyl-L-phenylalanine-chloromethyl ketone	Inhibition of TNF-alpha-induced NFkappaB activation in human HEK293 cells after 6 hrs by luciferase assay Inhibition of TNF-alpha-induced NFkappaB activation in human HEK293 cells after 6 hrs by luciferase assay	[PMID: 21978950]
HEK293	IC₅₀	5.05 μM Compound: TPCK	Inhibition of TNF-alpha activated nuclear factor-kappa B in HEK293 cells after 6 hrs by luciferase reporter gene assay Inhibition of TNF-alpha activated nuclear factor-kappa B in HEK293 cells after 6 hrs by luciferase reporter gene assay	[PMID: 26048799]
HEK293	IC₅₀	5.09 μM Compound: TPCK	Inhibition of TNF-alpha induced NF-kappaB transcriptional activity in HEK293 cells expressing NF-kappaB-Luc measured after 48 hrs by luciferase assay Inhibition of TNF-alpha induced NF-kappaB transcriptional activity in HEK293 cells expressing NF-kappaB-Luc measured after 48 hrs by luciferase assay	[PMID: 27155469]
HEK293	IC₅₀	5.09 μM Compound: TPCK	Inhibition of TNFalpha-activated nuclear factor-kappa B activity (unknown origin) expressed in HEK293 cells incubated for 6 hrs by luciferase reporter gene based assay Inhibition of TNFalpha-activated nuclear factor-kappa B activity (unknown origin) expressed in HEK293 cells incubated for 6 hrs by luciferase reporter gene based assay	[PMID: 27210437]
HEK293	IC₅₀	5.09 μM Compound: TPCK	Inhibition of TNFalpha-induced NF-kappaB activity expressed in HEK293 cells by luciferase reporter gene assay Inhibition of TNFalpha-induced NF-kappaB activity expressed in HEK293 cells by luciferase reporter gene assay	[PMID: 23142320]
HEK293	IC₅₀	5.09 μM Compound: TPCK	Inhibition of TNF-alpha activated NF-kappaB expressed in HEK293 cells by luciferase reporter gene assay Inhibition of TNF-alpha activated NF-kappaB expressed in HEK293 cells by luciferase reporter gene assay	[PMID: 22386564]
HEK293	IC₅₀	5.09 μM Compound: TPCK	Inhibition of TNFalpha-activated NF-kappaB expressed in HEK293 cells by luciferase reporter gene assay Inhibition of TNFalpha-activated NF-kappaB expressed in HEK293 cells by luciferase reporter gene assay	[PMID: 22115839]
HEK293	IC₅₀	5.09 μM Compound: TPCK	Inhibition of NF-kappaB expressed in human HEK293 cells by luciferase reporter gene based luminometric analysis Inhibition of NF-kappaB expressed in human HEK293 cells by luciferase reporter gene based luminometric analysis	[PMID: 21105712]
HEK293	IC₅₀	5.1 μM Compound: TPCK	Inhibition of TNFalpha-induced human NFkappaB activity in HEK293 cells incubated for 6 hrs followed by compound wash out measured after 5 mins by by luciferase assay Inhibition of TNFalpha-induced human NFkappaB activity in HEK293 cells incubated for 6 hrs followed by compound wash out measured after 5 mins by by luciferase assay	[PMID: 22712432]
HEK293	IC₅₀	5.3 μM Compound: TPCK	Inhibition of TNFalpha-induced NFkappaB activation in human HEK293 cells after 6 hrs by luciferase assay Inhibition of TNFalpha-induced NFkappaB activation in human HEK293 cells after 6 hrs by luciferase assay	[PMID: 32163285]

体外研究
(In Vitro)

TPCK 对哺乳动物细胞显示出轻微毒性 (CC₅₀ = 138.8 µM)，而对于 L. amazonensis 的 PH8 和 Josefa 株前鞭毛体形态具有显著抑制作用 (IC₅₀ 值分别为 14.6 µM 和 31.7 µM)，对 L. infantum 前鞭毛体形态的 IC₅₀ 值为 11.3 µM。此外，TPCK 对于细胞内的无鞭毛体形态同样有效，对于 L. amazonensis PH8 和 Josefa 株的 IC₅₀ 值分别为 14.2 µM 和 16.6 µM，而对于 L. infantum 无鞭毛体形态的 IC₅₀ 值则为 21.7 µM^[2]。
TPCK (40 μM，1 h) 在 LNCaP 中增强 wortmaninin 依赖性 caspase 活性，但抑制 TRAIL 依赖性 caspase 活性^[3]。
TPCK (40 μM，1 h) 在 PC3 细胞中抑制 TRAIL-DISC 的形成，但不抑制 Fas-DISC 的形成，降低 caspase2 水平^[3]。
TPCK (0-40 μM，24 h) 呈剂量依赖性杀死 PC3 细胞，诱导细胞凋亡^[3]。
TPCK (40 μM，3 h) 在 LNCaP 中降低了 BAD-ser136 的水平，消除了胞浆和颗粒中的 AR^[3]。

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

Western Blot Analysis^[3]

Cell Line:	PC3; LNCaP
Concentration:	40 μM
Incubation Time:	1 h; 3 h
Result:	Reduced the level of caspase-2 and inhibited TRAIL-induced activation of caspase-3, -7, -8, and -9. Did not reduce BAD levels, but reduced the level of BAD-ser136 and eliminated AR in the cytosol and granules.

Cell Viability Assay^[3]

Cell Line:	PC3
Concentration:	0, 2.5, 5, 10, 20, 40 μM
Incubation Time:	24 h
Result:	Killed PC3 cells in a dose-dependent manner.

体内研究
(In Vivo)

TPCK (15-60 mg/kg，腹腔注射，一周三次，十次) 减轻小鼠体内抗利什曼原虫活性^[2]。
TPCK (5-100 mg/kg，腹腔注射，单次剂量) 在新生幼鼠缺氧-缺血性脑损伤模型减少了 DNA 片段化、一氧化氮产生及脑损伤^[4]。
TPCK (0.5-20 mg/kg，注射到气囊腔中，单次剂量) 增加炎症大鼠血管通透性，随后下降^[5]。

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

Animal Model:	BALB/c mice infected with L. amazonensis ^[2]
Dosage:	15, 30, 45, 60 mg/kg; three times a week; 10 times
Administration:	Intraperitoneal injection (i.p.)
Result:	Reduced lesion size and parasite burden in foot pads and spleen.

Animal Model:	7-day-old rats with right carotid artery ligation^[4]
Dosage:	5, 10, 20, 50, 100 mg/kg; single dose
Administration:	Intraperitoneal injection (i.p.)
Result:	Reduced the weight of the right hemisphere of the brain, reduced the number of DNA breaks in cells, abolished the increase in nitrate/nitrite metabolites within 6 hours after injury, and reduced DNA fragmentation, nitric oxide production, and brain damage.

Animal Model:	Carrageenan-air sac inflammation rats^[5]
Dosage:	0.5, 4, 20 mg/kg; single dose
Administration:	Injection into the air sac
Result:	Showed that vascular permeability increased rapidly and then gradually decreased.

分子量

351.85

Formula

C₁₇H₁₈ClNO₃S

CAS 号

402-71-1

性状

固体

颜色

White to off-white

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 (284.21 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	2.8421 mL	14.2106 mL	28.4212 mL
5 mM	0.5684 mL	2.8421 mL	5.6842 mL
10 mM	0.2842 mL	1.4211 mL	2.8421 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

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 98.55%

选择批次：

Data Sheet (631 KB) SDS (393 KB)

COA (289 KB) HNMR (246 KB) RP-HPLC (205 KB) MS (179 KB) OR (170 KB)

产品使用指南 (1538 KB)

参考文献

[1]. H Stöppler, et al. The serine protease inhibitors TLCK and TPCK react with the RB-binding core of HPV-18 E7 protein and abolish its RB-binding capability. Virology. 1996 Mar 15;217(2):542-53. [Content Brief]

[2]. Patrícia de A Machado, et al. Effects of a Serine Protease Inhibitor N- p-Tosyl-L-phenylalanine Chloromethyl Ketone (TPCK) on Leishmania amazonensis and Leishmania infantum. Pharmaceutics.2022 Jun 29;14(7):1373. [Content Brief]

[3]. M H LeBlanc, et al. N-tosyl-L-phenylalanyl-chloromethylketone reduces hypoxic-ischemic brain injury in rat pups. Eur J Pharmacol. 2000 Mar 3;390(3):249-56 [Content Brief]

[4]. K Watanabe, et al. Vascular permeability changes by proteinase inhibitors in carrageenin-induced inflammation in rats. Agents Actions. 1986 Mar;17(5-6):472-7. [Content Brief]

TPCK 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	2.8421 mL	14.2106 mL	28.4212 mL	71.0530 mL
	5 mM	0.5684 mL	2.8421 mL	5.6842 mL	14.2106 mL
	10 mM	0.2842 mL	1.4211 mL	2.8421 mL	7.1053 mL
	15 mM	0.1895 mL	0.9474 mL	1.8947 mL	4.7369 mL
	20 mM	0.1421 mL	0.7105 mL	1.4211 mL	3.5527 mL
	25 mM	0.1137 mL	0.5684 mL	1.1368 mL	2.8421 mL
	30 mM	0.0947 mL	0.4737 mL	0.9474 mL	2.3684 mL
	40 mM	0.0711 mL	0.3553 mL	0.7105 mL	1.7763 mL
	50 mM	0.0568 mL	0.2842 mL	0.5684 mL	1.4211 mL
	60 mM	0.0474 mL	0.2368 mL	0.4737 mL	1.1842 mL
	80 mM	0.0355 mL	0.1776 mL	0.3553 mL	0.8882 mL
	100 mM	0.0284 mL	0.1421 mL	0.2842 mL	0.7105 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.

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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

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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）

TPCK (Synonyms: L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK)

Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献