TDI-11055 | ENL YEATS inhibitor | Probechem Biochemicals

Chemical Structure : TDI-11055

CAS No.: 3057216-63-1

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TDI-11055 (TDI 11055)

货号: PC-49300Not For Human Use, Lab Use Only.

TDI-11055 (TDI 11055) is a potent, selective and orally bioavailable inhibitor of the acyl-lysine reader ENL/AF9 YEATS domain with IC50 of 0.05 and 0.07 uM, respectively.

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10 mg	￥3580	In stock
25 mg	￥5480	In stock
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生物&药学活性

TDI-11055 (TDI 11055) is a potent, selective and orally bioavailable inhibitor of the acyl-lysine reader ENL/AF9 YEATS domain with IC50 of 0.05 and 0.07 uM, respectively.
TDI-11055 shows no inhibition of the YEATS domains of GAS41 and YEATS2 (IC50 > 100 μM), the other two YEATS domain-containing proteins.
TDI-11055 shows direct binding affinity to the ENL YEATS domain with Kd of 119 nM in isothermal titration calorimetry (ITC) assays.
TDI-11055 binds to and stabilizes endogenously expressed ENL but not GAS41 or YEATS2 in cells, binds directly to the acyl-binding site in ENL and engages with key acyl-recognizing residues.
TDI-11055 treatment led to a substantial displacement of ENL from target genes, including well-established leukemogenic genes in AML such as MYC and the HOXA cluster, TDI-11055 is a validated chemical tool for efficiently and specifically perturbing the chromatin reader function of ENL in living cells.
TDI-11055 inhibits the growth of MLL-r and NPM1-mutated leukemia cells in vitro (MV4;11 cell viability IC50=0.27 uM), decreases the expression of several key oncogenes in AML, including MYC, HOXA9/10, and MYB.
TDI-11055 impairs the clonogenic potential and induces differentiation of MLL-r and NPM1-mutated primary AML patient samples, blocks disease progression in models of MLL-r leukemia.

物理化学性质&存储条件

分子量	388.475
分子式	C22H24N6O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-1-methyl-N-(2-((2-methylpyrrolidin-1-yl)methyl)-1H-pyrrolo[3,2-c]pyridin-6-yl)-1H-indazole-5-carboxamide

参考文献

1. Yiman Liu, et al. Cancer Discov. 2022 Sep 2;CD-21-1307.

TDI-11055 (TDI 11055)

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物理化学性质&存储条件

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TDI-11055 (TDI 11055)

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