1. PROTAC
    Cell Cycle/DNA Damage
  2. PROTAC
    CDK
  3. TL12-186

TL12-186 

Cat. No.: HY-130665
Handling Instructions

TL12-186 is a CRBN-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM).

For research use only. We do not sell to patients.

TL12-186 Chemical Structure

TL12-186 Chemical Structure

CAS No. : 2250025-88-6

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Description

TL12-186 is a CRBN-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM)[1].

IC50 & Target[1]

Cereblon

 

cdk2/cyclin A

73 nM (IC50)

CDK9/cyclinT1

55 nM (IC50)

In Vitro

TL12-186 displays >90% inhibition of 193 kinases at a screening concentration of 1 μM[1].
TL12-186 displays potent binding to CRBN (IC50=12 nM) using an AlphaScreen engagement assay[1].
TL12-186 (1-10000 nM; 2 days) exhibits a CRBN-dependent pharmacological effect, displaying 13 to 15-fold more potent inhibition of survival of the WT cells than the CRBN-/- cells[1].
TL12-186 (10-10000 nM; 4 hours) inhibits STAT1 phosphorylation without causing JAK1/2 degradation[1].

Cell Proliferation Assay[1]

Cell Line: WT and CRBN-/- MOLM-14 cells; WT and CRBN-/- MOLT-4 cells
Concentration: 1, 10, 100, 1000, 10000 nM
Incubation Time: 2 days
Result: Exhibited a CRBN-dependent pharmacological effect, displaying 13 to 15-fold more potent inhibition of survival of the WT cells than the CRBN-/- cells.

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 10, 100, 1000, 10000 nM
Incubation Time: 4 hours
Result: Inhibited IFN-γ (10 ng/mL)-stimulated STAT1 phosphorylation (Y701) without causing degradation of JAK1 or JAK2.
Molecular Weight

931.46

Formula

C₄₄H₅₁ClN₁₀O₉S

CAS No.

2250025-88-6

SMILES

O=C(NCCOCCOCCN1CCN(C2=CC=C(NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3)C=C2)CC1)CNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

TL12-186PROTACCDKProteolysis-targeting chimeraCyclin dependent kinaseCRBNBTKFLT3Aurora kinasesTECULKITKCDK2cyclin ACDK9cyclin T1Inhibitorinhibitorinhibit

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TL12-186
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HY-130665
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