CCT241533 hydrochloride

SKU: orb1309859

Description

CCT241533 hydrochloride is a potent and selective ATP-competitive CHK2 inhibitor with a Ki of 1.16 nM. This small molecule is a valuable research tool for studying DNA damage response pathways in both cellular and biochemical assays.

Research Area

Cell Biology

Key Properties

• CAS Number: 1431697-96-9
• MW: 478.95
• Purity: 97.13% (May vary between batches)
• Formula: C₂₃H₂₈ClFN₄O₄
• SMILES: Cl.COc1cc2nc(nc(N[C@@H]3CNC[C@H]3C(C)(C)O)c2cc1OC)-c1cc(F)ccc1O
• Target: Chk
• Solubility: DMSO:100 mg/mL (208.79 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.35 mM)

Bioactivity

• Target IC50:
  Chk2:3 nM|Chk2:1.16 nM (Ki)|Chk1:245 nM
• In Vitro:
  CCT241533 hydrochloride inhibits CHK2 (IC50: 3 nM) and shows minimal cross-reactivity against a panel of kinases at 1 μM. X-ray crystallography confirms that CCT241533 binds to CHK2 in the ATP pocket. CCT241533 blocks CHK2 activity in human tumor cell lines in response to DNA damage. CCT241533 does not potentiate the cytotoxicity of a selection of genotoxic agents in several cell lines. However, CCT241533 significantly potentiates the cytotoxicity of two structurally distinct PARP inhibitors. Clear induction of the pS516 CHK2 signal is seen with a PARP inhibitor alone and this activation is abolished by CCT241533. In HT-29, HeLa, and MCF-7, the cytotoxicity of CCT241533 (GI50) is 1.7, 2.2, and 5.1 μM, respectively . CCT241533 hydrochloride is a potent CHK2 inhibitor (IC50: 3 nM), with selectivity (63-fold) over CHK1(IC50: 190 nM) and low hERG inhibition (IC50: 22 μM) .
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Chk2, Chk1, CCT 241533 Hydrochloride, CCT241533 hydrochloride, CCT241533 Hydrochloride, CCT-241533 Hydrochloride, CCT-241533 hydrochloride

Compound Identifiers

PubChem CID

136218645