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S-三苯甲基-L-半胱氨酸

S-三苯甲基-L-半胱氨酸用途

S-三苯基-L-半胱氨酸(NSC 83265)是一种选择性变构驱动蛋白Eg5抑制剂,IC50为1μM,用于抑制基础ATP酶活性,140 nM用于抑制微管激活的ATP酶活性。S-三苯基-L-半胱氨酸具有抗肿瘤活性[1][2]。

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S-三苯甲基-L-半胱氨酸名称

[ CAS 号 ]:
2799-07-7

[ 中文名 ]:
S-三苯甲基-L-半胱氨酸

[ 英文名 ]:
S-Tritylcysteine

[中文别名 ]:

三苯甲基-L-半胱氨酸

[英文别名 ]:

S-Triphenylmethyl-L-cysteine
EG5 INHIBITOR II
Cys(Trt)-OH
3-tritylthio-L-alanine
Alanine, 3- (tritylthio)-, D-
L-Cys(trt)-OH
DL-Cysteine, S-(triphenylmethyl)-
L-CYSTEINE, S-(TRIPHENYLMETHYL)-
EINECS 218-195-8
S-Tritylcysteine

S-三苯甲基-L-半胱氨酸生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> 驱动蛋白

信号通路 >> 细胞骨架 >> 驱动蛋白

[ 靶点 ]

Eg5

[体外研究]

S-三苯基-L-半胱氨酸结合到由二级结构元件(螺旋a2/环L5/螺旋a3)形成的Eg5运动域中的一个独特口袋中【1】。S-三苯基-L-半胱氨酸(1-20µM；72小时)可以剂量依赖性地介导细胞凋亡和细胞周期阻滞。S-三苯基-L-半胱氨酸介导的凋亡和细胞周期阻滞是由丝裂原活化蛋白激酶和核因子kB信号通路的激活触发的【1】。S-三苯基-L-半胱氨酸诱导具有特征性单星形纺锤体的HeLa细胞有丝分裂阻滞(IC50为700 nM)[2]。

[参考文献]

[1]. Wei Wu, et al. S-trityl-L-cysteine, a novel Eg5 inhibitor, is a potent chemotherapeutic strategy in neuroblastoma. Oncol Lett. 2018 Jul;16(1):1023-1030.

[2]. Salvatore DeBonis, et al. In vitro screening for inhibitors of the human mitotic kinesin Eg5 with antimitotic and antitumor activities. Mol Cancer Ther. 2004 Sep;3(9):1079-90.

S-三苯甲基-L-半胱氨酸物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
524.7±50.0 °C at 760 mmHg

[ 熔点 ]:
182-183 °C (dec.)(lit.)

[ 分子式 ]:
C₂₂H₂₁NO₂S

[ 分子量 ]:
363.47

[ 闪点 ]:
271.2±30.1 °C

[ 精确质量 ]:
363.129303

[ PSA ]:
88.62000

[ LogP ]:
5.56

[ 外观性状 ]:
近乎于白色至淡黄色粒状的粉末

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.642

[ 储存条件 ]:
-20°C

S-三苯甲基-L-半胱氨酸MSDS

详细MSDS(安全技术说明书)

S-三苯甲基-L-半胱氨酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AY7710000

CHEMICAL NAME :: Alanine, 3-(tritylthio)-, L-

CAS REGISTRY NUMBER :: 2799-07-7

BEILSTEIN REFERENCE NO. :: 2339626

LAST UPDATED :: 199801

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C22-H21-N-O2-S

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >540 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB81-109993

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 45 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB81-109993

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 936 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NCISP* National Cancer Institute Screening Program Data Summary, Developmental Therapeutics Program. (Bethesda, MD 20205) Volume(issue)/page/year: JAN1986

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 396 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NCISP* National Cancer Institute Screening Program Data Summary, Developmental Therapeutics Program. (Bethesda, MD 20205) Volume(issue)/page/year: JAN1986

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 59460 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB288-358

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 750 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

REFERENCE :: NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB81-109993

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

REFERENCE :: NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB81-109993

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Liver - jaundice, other or unclassified Blood - hemorrhage

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 29,95,1974 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 250 mg/kg/5D-I

TOXIC EFFECTS :: Cardiac - pulse rate Lungs, Thorax, or Respiration - dyspnea Related to Chronic Data - death

REFERENCE :: NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB216-419

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 375 mg/kg/33D-I

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases Related to Chronic Data - death

REFERENCE :: NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB216-419

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 250 mg/kg/5D-I

TOXIC EFFECTS :: Liver - other changes Kidney, Ureter, Bladder - other changes Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

REFERENCE :: NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB216-419

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S-三苯甲基-L-半胱氨酸安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
AY7710000

[ 海关编码 ]:
2930909090

S-三苯甲基-L-半胱氨酸合成路线

详细合成路线

S-三苯甲基-L-半胱氨酸上下游产品

S-三苯甲基-L-半胱氨酸上游产品

S-三苯甲基-L-半胱氨酸下游产品

S-三苯甲基-L-半胱氨酸海关

[ 海关编码 ]: 2930909090

[ 中文概述 ]:
2930909090. 其他有机硫化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2930909090. other organo-sulphur compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

S-三苯甲基-L-半胱氨酸文献

Cdk1 phosphorylates the Rac activator Tiam1 to activate centrosomal Pak and promote mitotic spindle formation.

Nat. Commun. 6 , 7437, (2015)

Centrosome separation is critical for bipolar spindle formation and the accurate segregation of chromosomes during mammalian cell mitosis. Kinesin-5 (Eg5) is a microtubule motor essential for centroso...

Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.

J. Med. Chem. 51 , 1115-25, (2008)

The human kinesin Eg5 is a potential drug target for cancer chemotherapy. Eg5 specific inhibitors cause cells to block in mitosis with a characteristic monoastral spindle phenotype. Prolonged metaphas...

Dynamics of Human Telomerase Holoenzyme Assembly and Subunit Exchange across the Cell Cycle.

J. Biol. Chem. 290 , 21320-35, (2015)

Human telomerase acts on telomeres during the genome synthesis phase of the cell cycle, accompanied by its concentration in Cajal bodies and transient colocalization with telomeres. Whether the regula...

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