Leflunomide (HWA486) - Moligand™, 10mM in DMSO , Dihydroorotate dehydrogenase inhibitor, CAS No.75706-12-6, Dihydroorotate dehydrogenase inhibitor

CAS: 75706-12-6 Cat. No.: L408176 Peso molecular: 270.21 Número EC: 616-254-6

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

RS-34821, SU101, Arava | 5-methyl-N-(4-(trifluoromethyl)phenyl)isoxazole-4-carboxamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Leflunomide (HWA486) Leflunomide (HWA486, RS-34821, SU101, Arava) is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibit
In vitro

Leflunomide is actually a prodrug that is processed in vivo to the active metabolite A771726，which has been shown to inhibit proliferation of mononuclear and T-cells. Leflunomide is an inhibitor of several protein tyrosine kinases, with IC50 values between 30 mM and 100 mM in vitro cellular and enzymatic assays. Leflunomide is capable of inhibiting anti-CD3- and interleukin-2 (IL-2)-stimulated T cell proliferation. Leflunomide is able to inhibit p59fyn and p56lck activity in in vitro tyrosine kinase assays. Leflunomide also inhibits Ca2+ mobilization in Jurkat cells stimulated by anti-CD3 antibody but not in those stimulated by ionomycin. Leflunomide also inhibits distal events of anti-CD3 monoclonal antibody stimulation, namely, IL-2 production and IL-2 receptor expression on human T lymphocytes. Leflunomide also inhibits tyrosine phosphorylation in CTLL-4 cells stimulated by IL-2. Leflunomide is an immunomodulatory drug that may exert its effects by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH), which plays a key role in the de novo synthesis of the pyrimidine ribonucleotide uridine monophosphate (rUMP). Leflunomide prevents the expansion of activated and autoimmune lymphocytes by interfering with the cell cycle progression due to inadequate production of rUMP and utilizing mechanisms involving p53.

In vivo

Leflunomide is able to prevent and reverse allograft and xenograft rejection in rodents, dogs, and monkeys.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

RS-34821, SU101, Arava | 5-methyl-N-(4-(trifluoromethyl)phenyl)isoxazole-4-carboxamide

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Leflunomide (HWA486, RS-34821, SU101, Arava) is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydr

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Dihydroorotate dehydrogenase inhibitor

Propiedades del producto

• ALogP: 2.5

Nombres e identificadores

• Isómeros SMILES: CC1=C(C=NO1)C(=O)NC2=CC=C(C=C2)C(F)(F)F
• WGK Alemania: 3
• RTECS: NY2354200
• Peso molecular: 270.21
• Reaxy-Rn: 4323174
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4323174&ln=

Objetivos asociados (humanos)

CYP1A2 Tchem Cytochrome P450 1A2 (2 Activities)

Discover Target: CYP1A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DHODH Tclin Dihydroorotate dehydrogenase (quinone), mitochondrial (2 Activities)

Discover Target: DHODH

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Punto de fusión (°C): 166.5°C

Referencias

1. Qinqin Cui, Hongyun Bi, Zhanyun Lv, Qigui Wu, Jianfeng Hua, Bokai Gu, Chanjuan Huo, Mingmin Tang, Yanqin Chen, Chongjiu Chen, Sihan Chen, Xinrui Zhang, Zhangrui Wu, Zhengkai Lao, Nengyin Sheng, Chengyong Shen, Yongdeng Zhang, Zhi-Ying Wu, Zhigang Jin, Peiguo Yang, Huaqing Liu, Jinsong Li, Ge Bai.  (2023)  Diverse CMT2 neuropathies are linked to aberrant G3BP interactions in stress granules.  CELL,      [PMID:36738734] [10.1016/j.cell.2022.12.046]

2. Yizhou Gao, Xiaohui Xiong, Hui Wang, Jiajing Wang, Yan Bi, Yuqing Yan, Zhongye Cao, Dayong Li, Fengming Song.  (2021)  Ero1-Pdi1 module-catalysed dimerization of a nucleotide sugar transporter, FonNst2, regulates virulence of Fusarium oxysporum on watermelon.  ENVIRONMENTAL MICROBIOLOGY,  24  (3): (1200-1220).  [PMID:34587346] [10.1111/1462-2920.15789]

3. Fenfen Ji, Pingmei Huang, Qiming Zhou, Lok Hin Ko, Qinyao Wei, Charis Cheuk-Lok Chan, Danyu Chen, Huarong Chen, Wei Kang, Alvin Ho-Kwan Cheung, Cillian H. Cheng, Jianming Shen, Yasi Pan, Ying Jiao, Lin Zhu, Tat Wai Chik, Peisi Xie, Xiao Liang, Onno Kranenburg, Zongwei Cai, Jun Yu, Chi Chun Wong.  (2026)  Compartmentalized branched-chain amino acid metabolism orchestrates colorectal cancer dissemination via an UMP-vimentin axis.  Cell Metabolism,      [PMID:41653924] [10.1016/j.cmet.2026.01.007]