BTX161

• CAT Number: I045541
• CAS Number: 2052301-24-1
• Molecular Formula: C15H16N2O3
• Molecular Weight: 272.30
• Purity: ≥95%
• Synonyms: (3S)-3-(7-methyl-3-oxo-1H-isoindol-2-yl)azepane-2,7-dione
• InChI: InChI=1S/C15H16N2O3/c1-9-4-2-5-10-11(9)8-17(15(10)20)12-6-3-7-13(18)16-14(12)19/h2,4-5,12H,3,6-8H2,1H3,(H,16,18,19)/t12-/m0/s1
• InChIKey: CNIZBMYCKRUTHY-LBPRGKRZSA-N
• SMILES: CC1=C2CN(C(=O)C2=CC=C1)C3CCCC(=O)NC3=O

BTX161, a Thalidomide analog, is a potent CKIα degrader. BTX161 mediates degradation of CKIα better than Lenalidomide in human AML cells and activates DNA damage response (DDR) and p53, while stabilizing the p53 antagonist MDM2[1].
BTX161 (25 μM; 4 hours; MV4-11 cells) upregulates all the Wnt targets including MYC and did not affect MDM2 mRNA expression[1].
BTX161 (10 μM; 6 hours; MV4-11 cells), on its own, augmented p53 and MDM2 protein expression, yet in combination with THZ1, and particularly with both THZ1 and CDK9, further augmented p53 and induced maximal caspase 3 activation[1].

Reference

[1]. Minzel W, et al. Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. Cell. 2018;175(1):171-185.e25.
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