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TL4-12

CAS No. 1620820-12-3

TL4-12( —— )

Catalog No. M34138 CAS No. 1620820-12-3

TL4-12 is a specific MAP4K2/GCK inhibitor that inhibits IKZF1 and BCL-6.TL4-12 inhibits MM cell proliferation and induces apoptosis, and can be used in the study of multiple myeloma (MM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    TL4-12
  • Note
    Research use only, not for human use.
  • Brief Description
    TL4-12 is a specific MAP4K2/GCK inhibitor that inhibits IKZF1 and BCL-6.TL4-12 inhibits MM cell proliferation and induces apoptosis, and can be used in the study of multiple myeloma (MM).
  • Description
    TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory agent resistance in multiple myeloma (MM).
  • In Vitro
    TL4 12 (0-5 μM; 4 days) shows antiproliferation activity with an IC50 value of 37 nM for MM cells, and with IC50s of 1.62, 3.7, 4.4, 5.7, 10, 32, 49, 19 μM for JJN3, MM1.S, H929, RPMI-8226, MOLP-8, SKMM2, LP-1, U266 cells, respectively.TL4-12 (0, 1, 3 μM; 24 h) dose-dependently decreases IKZF1, c-MYC, and BCL-6 protein expression and increases p53 level in K-RASG12A MM.1S cells.TL4-12 dose-dependently increases Annexin-V positive cell from 6% (dimethyl sulfoxide) to 13% (1 μM) and 22% (3 μM), respectively.TL4-12 induces apoptosis and cell-cycle arrest in the G0/G1 phase in MM.1S, RPMI-8226, RPMI-8226 cells.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Immunology/Inflammation related | BCL | Apoptosis
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1620820-12-3
  • Formula Weight
    500.52
  • Molecular Formula
    C25H27F3N6O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 8.33 mg/mL (16.64 mM; Ultrasonic (<60°C)
  • SMILES
    O=C(NC=1C=C(C=C(C1)C(F)(F)F)N2CCN(C)CC2)C3=CC=C(C(OC4=NC=NC(=C4)NC)=C3)C
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Shirong Li, et al. Targeting the GCK pathway: a novel and selective therapeutic strategy against RAS-mutated multiple myeloma. Blood. 2021 Apr 1;137(13):1754-1764.?
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