62004-35-7
Chemical Structure
LFM-A13
- CAS No.: 62004-35-7
- Formula:C11H8Br2N2O2
- Molecular Weight:360.00
IUPAC Name: (Z)-2-cyano-N-(2,5-dibromophenyl)-3-hydroxybut-2-enamide
InChIKey: UVSVTDVJQAJIFG-VURMDHGXSA-N
SMILES: C/C(O)=C(C#N)/C(NC1=CC(Br)=CC=C1Br)=O
Biological Activity: LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research[1][3][4]
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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LFM-A13 | 98.26% | LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research | ||||||||||||||||||||
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Manitimus | 98.54% | Manitimus is an inhibitor of dehydroorotate dehydrogenase, and a potent immunosuppressive agent. Manitimus is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | ||||||||||||||||||||
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Laflunimus | 99.70% | Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC50 values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor. | ||||||||||||||||||||
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Teriflunomide-d4 | 99.98% | Teriflunomide-d4 is deuterium labeled Teriflunomide. | ||||||||||||||||||||
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DHODH-IN-3 | DHODH-IN-3 (compound 3) is a potent inhibitor of Human Dihydroorotate Dehydrogenases (HsDHODH) with an IC50 value of 261 nM. DHODH-IN-3 binds to the the ubiquinone binding cavities in DHODH with a Kiapp of 32 nM. DHODH-IN-3 has the potential for malaria treatment. | |||||||||||||||||||||
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DHODH-IN-4 | DHODH-IN-4 (compound 17) is a human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) inhibitor, with IC50 values of 4 μM and 0.18 μM for PfDHODH and HsDHODH, respectively. DHODH-IN-4 (compound 17) possess antimalarial activity. | |||||||||||||||||||||
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PfDHODH-IN-1 | 99.12% | PfDHODH-IN-1 is an analogue of the active metabolite of Leflunomide. PfDHODH-IN-1 is a Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor. PfDHODH-IN-1 has antimalarial activity. | ||||||||||||||||||||
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hDHODH-IN-1 | 99.90% | hDHODH-IN-1 is a human dihydroorotate dehydrogenase (hDHODH) inhibitor. hDHODH-IN-1 has anti-inflammatory effect. | ||||||||||||||||||||
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DHODH-IN-8 | DHODH-IN-8 (Compound 27) is an inhibitor of human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) with IC50s of 0.13 μM and 47.4 μM, and Kis of 0.016 μM and 5.6 μM, respectively. DHODH-IN-8 has antimalarial activity. | |||||||||||||||||||||
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Teriflunomide (Standard) | ≥98% | Teriflunomide (Standard) is the analytical standard of Teriflunomide. This product is intended for research and analytical applications. Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation. | ||||||||||||||||||||
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(Z)-LFM-A13 | 99.80% | LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK. | ||||||||||||||||||||
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References
- [1]. Mahajan S, et al. Rational design and synthesis of a novel anti-leukemic agent targeting Bruton's tyrosine kinase (BTK), LFM-A13 [alpha-cyano-beta-hydroxy-beta-methyl-N-(2, 5-dibromophenyl)propenamide]. J Biol Chem. 1999 Apr 2;274(14):9587-99. [Content Brief]
- [3]. Uckun FM, et al. Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK). Bioorg Med Chem. 2007 Jan 15;15(2):800-14. [Content Brief]
- [4]. Sahin K, et al. LFM-A13, a potent inhibitor of polo-like kinase, inhibits breast carcinogenesis by suppressing proliferation activity and inducing apoptosis in breast tumors of mice. Invest New Drugs. 2018 Jun;36(3):388-395. [Content Brief]