CCT241533
Based on 6 publication(s) in Google Scholar
CCT241533 is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM.
For research use only. We do not sell to patients.
- CAS No.: 1262849-73-9
- Formula: C23H27FN4O4
- Molecular Weight:442.48
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) CCT241533
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Cell Death Differ. 2021 Jul;28(7):2060-2082. [Abstract]
- J Chem Inf Model. 2017 Nov 27;57(11):2699-2706. [Abstract]
- J Cell Biol. 2021 Feb 1;220(2):e201911025. [Abstract]
- Int J Mol Sci. 2022 Oct 14;23(20):12290. [Abstract]
- University of Califomia San Francisco. 2026.
Biological Activity
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Chk2 3 nM (IC50) |
Chk1 245 nM (IC50) |
Chk2 1.16 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | GI50 |
1.4 μM
Compound: 46
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Cytotoxicity against human HT-29 cells by SRB colorimetric assay
Cytotoxicity against human HT-29 cells by SRB colorimetric assay
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[PMID: 21186793] |
CCT241533 hydrochloride inhibits CHK2 with an IC50 of 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, as demonstrated by inhibition of CHK2 autophosphorylation at S516, band-shift mobility changes and HDMX degradation. 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. The cytotoxicity of CCT241533 in HT-29, HeLa and MCF-7, measured as the growth inhibitory IC50(GI50) by SRB assay, is 1.7, 2.2 and 5.1 μM, respectively[1]. 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)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1262849-73-9
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Appearance Solid
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Molecular Weight 442.48
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Formula C23H27FN4O4
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Color White to off-white
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SMILES
COC1=C(OC)C=C(C(N[C@H]2[C@H](C(C)(C)O)CNC2)=NC(C3=C(O)C=CC(F)=C3)=N4)C4=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Cell Death Differ
Control of replication stress and mitosis in colorectal cancer stem cells through the interplay of PARP1, MRE11 and RAD51. [Abstract]2021 Jul;28(7):2060-2082. PMID: 33531658 -
J Chem Inf Model
2017 Nov 27;57(11):2699-2706. PMID: 29035535 -
J Cell Biol
2021 Feb 1;220(2):e201911025. PMID: 33404607 -
Int J Mol Sci
Checkpoint Kinase 2 Inhibition Can Reverse Tamoxifen Resistance in ER-Positive Breast Cancer. [Abstract]2022 Oct 14;23(20):12290. PMID: 36293165 -
Protocol
HT-29, HeLa and MCF-7 cells are exposed to a fixed concentration (GI50) of CCT241533 in combination with increasing concentrations of either PARP inhibitor or cytotoxic drug in a 96 hour SRB assay or 7-10 day colony forming assay. The ability of CCT241533 to enhance cell killing is expressed as a potentiation index (PI) which is the ratio of GI50 for the genotoxic or PARP inhibitor alone: GI50 for the genotoxic or PARP inhibitor in combination with a CHK2 inhibitor. Thus PI>1 indicates potentiation and PI<1 indicates protection[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
References
[1]. Anderson VE, et al. CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors. Cancer Res. 2011 Jan 15;71(2):463-72. [Content Brief]
[2]. Caldwell JJ, et al. Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J Med Chem. 2011 Jan 27;54(2):580-90. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CCT241533 Related Classifications
HY-14715 Related Classifications
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