Molecular structure of Wee1 Inhibitor, CAS Number: 622855-37-2
Wee1 Inhibitor (CAS 622855-37-2)
Alternate Names:
4-(2-Chlorophenyl)-9-hydroxypyrrolo[3,4-c]carbazole-1,3-(2H,6H)-dione
Application:
Wee1 Inhibitor is a pyrrolocarbazole compound that acts as a potent, ATP-binding site-targeting inhibitor of Wee1
CAS Number:
622855-37-2
Molecular Weight:
362.77
Molecular Formula:
C20H11ClN2O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
QUICK LINKS
Ordering Information
Description
Technical Information
Safety Information
SDS & Certificate of Analysis
Wee1 Inhibitor is a pyrrolocarbazole compound that acts as a potent, ATP-binding site-targeting inhibitor of Wee1 (IC50 = 11 nM) in an ATP-competitive manner and displays ~40-fold selectivity over the related checkpoint kinase Chk1 (IC50 = 440 nM). Wee1 is a protein kinase involved in cell cycle regulation, particularly in the control of the G2-M checkpoint. By inhibiting Wee1, these inhibitors can interfere with the normal cell cycle progression and promote cell cycle arrest or induce premature entry into mitosis. This disruption of the cell cycle can have various effects on cell proliferation. Wee1 Inhibitor has been investigated as a potential anticancer agent due to its ability to induce DNA damage and promote cell death in cancer cells. It also inhibits the ATPase activity of LptB, an enzyme involved in the transport and assembly of LPS (IC50 = 25 µM for the E. coli enzyme).
Wee1 Inhibitor (CAS 622855-37-2) References
- 4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution. | Palmer, BD., et al. 2006. J Med Chem. 49: 4896-911. PMID: 16884302
- Cell cycle regulation by the Wee1 inhibitor PD0166285, pyrido [2,3-d] pyimidine, in the B16 mouse melanoma cell line. | Hashimoto, O., et al. 2006. BMC Cancer. 6: 292. PMID: 17177986
- CHK1 plays a critical role in the anti-leukemic activity of the wee1 inhibitor MK-1775 in acute myeloid leukemia cells. | Qi, W., et al. 2014. J Hematol Oncol. 7: 53. PMID: 25084614
- A regimen combining the Wee1 inhibitor AZD1775 with HDAC inhibitors targets human acute myeloid leukemia cells harboring various genetic mutations. | Zhou, L., et al. 2015. Leukemia. 29: 807-18. PMID: 25283841
- Functional Genetic Screen Identifies Increased Sensitivity to WEE1 Inhibition in Cells with Defects in Fanconi Anemia and HR Pathways. | Aarts, M., et al. 2015. Mol Cancer Ther. 14: 865-76. PMID: 25673822
- A haploid genetic screen identifies the G1/S regulatory machinery as a determinant of Wee1 inhibitor sensitivity. | Heijink, AM., et al. 2015. Proc Natl Acad Sci U S A. 112: 15160-5. PMID: 26598692
- A WEE1 Inhibitor Analog of AZD1775 Maintains Synergy with Cisplatin and Demonstrates Reduced Single-Agent Cytotoxicity in Medulloblastoma Cells. | Matheson, CJ., et al. 2016. ACS Chem Biol. 11: 921-30. PMID: 26745241
- Suppression of Sirt1 sensitizes lung cancer cells to WEE1 inhibitor MK-1775-induced DNA damage and apoptosis. | Chen, G., et al. 2017. Oncogene. 36: 6863-6872. PMID: 28869605
- Identification of a rhodium(iii) complex as a Wee1 inhibitor against TP53-mutated triple-negative breast cancer cells. | Yang, GJ., et al. 2018. Chem Commun (Camb). 54: 2463-2466. PMID: 29367998
- ATM, ATR, CHK1, CHK2 and WEE1 inhibitors in cancer and cancer stem cells. | Ronco, C., et al. 2017. Medchemcomm. 8: 295-319. PMID: 30108746
- Combined Aurora Kinase A (AURKA) and WEE1 Inhibition Demonstrates Synergistic Antitumor Effect in Squamous Cell Carcinoma of the Head and Neck. | Lee, JW., et al. 2019. Clin Cancer Res. 25: 3430-3442. PMID: 30755439
- Sequential Therapy with PARP and WEE1 Inhibitors Minimizes Toxicity while Maintaining Efficacy. | Fang, Y., et al. 2019. Cancer Cell. 35: 851-867.e7. PMID: 31185210
- Upregulation of Myt1 Promotes Acquired Resistance of Cancer Cells to Wee1 Inhibition. | Lewis, CW., et al. 2019. Cancer Res. 79: 5971-5985. PMID: 31594837
- Antitumor effect of a WEE1 inhibitor and potentiation of olaparib sensitivity by DNA damage response modulation in triple-negative breast cancer. | Ha, DH., et al. 2020. Sci Rep. 10: 9930. PMID: 32555285
- WEE1 inhibition induces anti-tumor immunity by activating ERV and the dsRNA pathway. | Guo, E., et al. 2022. J Exp Med. 219: PMID: 34825915
Inhibitor of:
Wee 1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Wee1 Inhibitor, 1 mg | sc-311555 | 1 mg | $189.00 |