TCS PIM-1 1


CAS No. : 491871-58-0

(Synonyms: SC 204330)

491871-58-0
Price and Availability of CAS No. : 491871-58-0
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5mg $83 In-stock
10mg $130 In-stock
25mg $245 In-stock
50mg $363 In-stock
100mg $540 In-stock
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Cat. No. : HY-18086
M.Wt: 367.20
Formula: C18H11BrN2O2
Purity: >98 %
Solubility: DMSO : 100 mg/mL (ultrasonic)
Introduction of 491871-58-0 :

TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM)[1]. IC50 & Target: IC50: 50 nM (Pim-1)[1] In Vitro: TCS PIM-1 1 (compound 1), a substituted pyridone scaffold, binds convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggests that TCS PIM-1 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2. Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors. TCS PIM-1 1 serves both as a starting point for SAR chemical syntheses and was used for co-crystallization with Pim-1 protein[1].

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