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  3. TL12-186

TL12-186 #54268

    Product Information

    Product Usage Information

    TL12-186 is supplied as a lyophilized powder. For a 5 mM stock, reconstitute 5 mg of powder in 1.07 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

    Storage

    Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

    Product Description

    Molecular Weight 931.5 g/mol
    Purity 98%
    Molecular Formula C44H51CIN10O9S
    CAS 2250025-88-6
    Solubility Soluble in DMSO at 95 mg/mL.

    Background

    TL12-186 is a pan-kinase PROTAC (proteolysis-targeting chimera) compound that links a cereblon (CRBN)-recruiting pomalidomide moiety and a promiscuous kinase inhibitor (1). The inhibitor moiety competes with ATP for binding to the kinase catalytic site. TL12-186 exhibits a binding affinity (IC50) of 12 nM for CRBN. At a concentration of 1 μM, TL12-186 induces >90% inhibition of 193 kinases according to a kinase selectivity assay. When administered at 100 nM for four hours in human MOLM-14 and MOLT-4 cells, TL12-186 degrades 28 kinases by 50% or more, including BTK, PTK2, PTK2B, FLT3, AURKA/B, TEC, ULK1, ITK, and nine members of the CDK family.

    This compound is valuable for assessing the susceptibility of kinases to degradation in various model systems. In one study, a platelet model system treated with TL12-186 showed that BTK degradation has advantages over simple inhibition in preventing thrombosis (2). Additionally, TL12-186 was used to experimentally validate a computational model that predicts which substrate lysines are most likely to be ubiquitinated by CRBN-dependent PROTACs (3).

    Limited Uses

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    For Research Use Only. Not for Use in Diagnostic Procedures.
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