TCMDC-135051

CAS No. 2413716-15-9

TCMDC-135051( —— )

Catalog No. M33139 CAS No. 2413716-15-9

TCMDC-135051 is a potent and selective PfCLK3 protein kinase inhibitor demonstrating significant antiparasiticidal activity (EC50=320 nM) while exhibiting minimal off-target toxicity.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 120 Get Quote
5MG 186 Get Quote
10MG 320 Get Quote
25MG 490 Get Quote
50MG 638 Get Quote
100MG 859 Get Quote
500MG 1737 Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    TCMDC-135051
  • Note
    Research use only, not for human use.
  • Brief Description
    TCMDC-135051 is a potent and selective PfCLK3 protein kinase inhibitor demonstrating significant antiparasiticidal activity (EC50=320 nM) while exhibiting minimal off-target toxicity.
  • Description
    TCMDC-135051 is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 has antiparasiticidal activity (EC50=320 nM).
  • In Vitro
    TCMDC-135051 shows potent activity against P. berghei sporozoites in a liver invasion and development assay in which the compound shows a pEC50 value of 6.17 (EC50=0.40 μM).The kinase assays using recombinant PvCLK3 (P. vivax) and PbCLK3 (P. berghei) show that TCMDC-135051 has near-equipotent inhibition at these two orthologs, with pIC50 values of 7.47 (IC50=0.033 μM) and 7.86 (IC50=0.013 μM), respectively.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Others
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2413716-15-9
  • Formula Weight
    471.59
  • Molecular Formula
    C29H33N3O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 250 mg/mL (530.12 mM; Ultrasonic )
  • SMILES
    CCN(CC)Cc1ccc(OC)c(c1)-c1cc2c(ccnc2[nH]1)-c1ccc(C(O)=O)c(c1)C(C)C
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Alam MM, et al. Validation of the protein kinase PfCLK3 as a multistage cross-species malarial drug target. Science. 2019 Aug 30;365(6456). pii: eaau1682.?
molnova catalog
related products
  • LS-102

    LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment.

  • Tranilast

    A compound that exhibits anti-inflammatory and immunomodulatory effects by inhibiting lipid mediator and cytokine release from inflammatory cells and interfering with PDGF- and TGF-β1-induced proliferation and migration of vascular medial smooth muscle cells.

  • Mequitazine

    Mequitazine is an effective, nonsedative and long-acting histamine H1 antagonist.