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LDC4297

Chemical Structure : LDC4297

CAS No.: 1453834-21-3

LDC4297 (LDC 4297, LDC044297)

Catalog No.: PC-20316Not For Human Use, Lab Use Only.

LDC4297 (LDC044297) is a potent, highly specific CDK7 inhibitor with IC50 of 7.4 nM in ATP competition assays (3.5 mM ATP), weakly inhibits CDK2 (IC50>2 uM).

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Biological Activity

LDC4297 (LDC044297) is a potent, highly specific CDK7 inhibitor with IC50 of 7.4 nM in ATP competition assays (3.5 mM ATP), weakly inhibits CDK2 (IC50>2 uM).
LDC4297 prevents RNA polymerase II (RNAPII) transcription in an inducible-gene setting, reduces in vitro transcription by RNAPII.
LDC4297 causes tumor cell death and cell-type-dependent cell cycle delay in A549 cells and HCT116 cells.
LDC4297 effectively blocks the replication of human cytomegalovirus (HCMV) in primary human fibroblasts with EC50 of 24.5 nM, interferes HCMV-driven inactivation of retinoblastoma protein (Rb), a regulatory step generally considered a hallmark of herpesviral replication.

Physicochemical Properties

M.Wt 432.53
Formula C23H28N8O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(2-(1H-pyrazol-1-yl)benzyl)-8-isopropyl-2-(piperidin-3-yloxy)pyrazolo[1,5-a][1,3,5]triazin-4-amine

References

1. Kelso TW, et al. Mol Cell Biol. 2014 Oct 1;34(19):3675-88.

2. Hutterer C, et al. Antimicrob Agents Chemother. 2015 Apr;59(4):2062-71.

3. Ghezzi C, et al. Nat Commun. 2019 Nov 29;10(1):5444.

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