Prexasertib | CHK1/2 inhibitor

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Prexasertib (1234015-54-3) is a potent inhibitor of CHK1 (IC50 = <1 nM) and CHK2 (IC50 = 8 nM).1 It also inhibits RSK1 (IC50 = 9 nM).1 Prexasertib displayed efficacy in various cancer models alone and in combination with other agents including anti-PD-L1 therapy.2-6 It promoted neuroprotection, axon regeneration, and functional recovery after CNS injury.7 The cytotoxic effects of prexasertib have been attributed to dual inhibition of CHK1 and AMPK.8

References/Citations:

  1. King et al. (2015), LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms; Mol. Cancer Ther. 14 2004
  2. Huang et al. (2024), Inhibition of Chk1 with Prexasertib Enhances the Anticancer Activity of Ciclopirox in Non-Small Cell Lung Cancer Cells; Cells 13 1752
  3. Zhang et al. (2025), Prexasertib exerts a synergistic effect on the antitumor activity of Lenvatinib through ALOX15-mediated ferroptosis in hepatocellular carcinoma; Int. Immunopharmacol. 150 114278
  4. Chen et al. (2025), Combined CHK1 and PD-L1 blockade as a novel therapeutic strategy against stemness and immunosuppression in ovarian cancer.; Cancer Immunol. Immunother. 74 365
  5. Zhang et al. (2026), CHK1 inhibition by prexasertib sensitizes cisplatin-resistant malignant tumor cells via checkpoint abrogation and STAT1-driven PD-L1 upregulation; Int. Immunopharmacol. 171 116126
  6. Morimoto et al. (2026), Chk1 inhibition emerges as the most effective partner for PARP inhibition in BRCA-proficient pancreatic cancer.; Discov. Oncol. Online ahead of print
  7. Taylor et al. (2022), Inhibition of Chk2 promotes peuroprotection, axon regeneration, and functional recovery after CNS injury; Sci. Adv. 8 eabq2611
  8. Guo et al. (2026), The cytotoxic effect of prexasertib is a consequence of dual inhibition on both CHK1 and AMPK; Cell Chem. Biol. 33 767
1234015-54-3, Chk1/2 inhibitor, LY2606368, prexasertib, prexasertib dihydrochloride, Prexasertib supplier, Selective CHK inhibitor
Alternate Name:
LY2606368

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Prexasertib (1234015-54-3) is a potent inhibitor of CHK1 (IC50 = <1 nM) and CHK2 (IC50 = 8 nM).1 It also inhibits RSK1 (IC50 = 9 nM).1 Prexasertib displayed efficacy in various cancer models alone and in combination with other agents including anti-PD-L1 therapy.2-6 It promoted neuroprotection, axon regeneration, and functional recovery after CNS injury.7 The cytotoxic effects of prexasertib have been attributed to dual inhibition of CHK1 and AMPK.8

References/Citations:

  1. King et al. (2015), LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms; Mol. Cancer Ther. 14 2004
  2. Huang et al. (2024), Inhibition of Chk1 with Prexasertib Enhances the Anticancer Activity of Ciclopirox in Non-Small Cell Lung Cancer Cells; Cells 13 1752
  3. Zhang et al. (2025), Prexasertib exerts a synergistic effect on the antitumor activity of Lenvatinib through ALOX15-mediated ferroptosis in hepatocellular carcinoma; Int. Immunopharmacol. 150 114278
  4. Chen et al. (2025), Combined CHK1 and PD-L1 blockade as a novel therapeutic strategy against stemness and immunosuppression in ovarian cancer.; Cancer Immunol. Immunother. 74 365
  5. Zhang et al. (2026), CHK1 inhibition by prexasertib sensitizes cisplatin-resistant malignant tumor cells via checkpoint abrogation and STAT1-driven PD-L1 upregulation; Int. Immunopharmacol. 171 116126
  6. Morimoto et al. (2026), Chk1 inhibition emerges as the most effective partner for PARP inhibition in BRCA-proficient pancreatic cancer.; Discov. Oncol. Online ahead of print
  7. Taylor et al. (2022), Inhibition of Chk2 promotes peuroprotection, axon regeneration, and functional recovery after CNS injury; Sci. Adv. 8 eabq2611
  8. Guo et al. (2026), The cytotoxic effect of prexasertib is a consequence of dual inhibition on both CHK1 and AMPK; Cell Chem. Biol. 33 767