keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TL12-186 is a Cereblon-dependent kinase degrader that degrades CDK, BTK, FLT3, Aurora and other kinases.TL12-186 inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC50s of 73 and 55 nM, respectively.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 116.00 | |
5 mg | In stock | $ 288.00 | |
10 mg | In stock | $ 482.00 | |
25 mg | In stock | $ 892.00 | |
50 mg | In stock | $ 1,220.00 | |
100 mg | In stock | $ 1,650.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 490.00 |
Description | TL12-186 is a Cereblon-dependent kinase degrader that degrades CDK, BTK, FLT3, Aurora and other kinases.TL12-186 inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC50s of 73 and 55 nM, respectively. |
Targets&IC50 | CDK2-CyclinA:73 nM (IC50), CRBN:12nM, CDK9-CyclinT1:55 nM (IC50) |
In vitro | TL12-186 demonstrates over 90% inhibition against 193 kinases at a screening concentration of 1 μM[1]. Utilizing AlphaScreen binding assays, it exhibits potent binding to CRBN with an IC50 of 12 nM[1]. Displaying CRBN-dependent pharmacological effects, TL12-186 (1-10000 nM; 2 days) exerts 13 to 15 times stronger inhibition of cell survival in WT cells compared to CRBN-/- cells[1]. Moreover, at concentrations ranging from 10 to 10000 nM for 4 hours, TL12-186 selectively inhibits STAT1 phosphorylation without inducing degradation of JAK1/2[1]. |
Synonyms | TL12 186, TL12186 |
Molecular Weight | 931.46 |
Formula | C44H51ClN10O9S |
CAS No. | 2250025-88-6 |
keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 200 mg/mL (214.72 mM), Sonication is recommended.
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TL12-186 2250025-88-6 Cell Cycle/Checkpoint PROTAC CDK Ligand for E3 Ligase TL 12186 TL12 186 TL12186 TL-12186 inhibitor inhibit