Helicases Inhibitor

DHX9-IN-9 (509) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.0177 μM in DHX9 cellular target engagement. Used in cancer research.

GSK_WRN3 is selective WRN helicase inhibitor (pIC₅₀ = 8.6). SK_WRN3 can selectively inhibit the growth of microsatellite unstable (MSI) cancer cells, induce DNA damage, and cause cell cycle arrest. GSK_WRN3 has anti-tumor activity.

GSK_WRN4 is an orally active WRN helicase inhibitor (pIC₅₀=7.6). GSK_WRN4 induces DNA damage markers (p21, p-γH2AX, p-KAP1). GSK_WRN4 selectively inhibits microsatellite-unstable tumor growth in vitro and in vivo by inducing DNA double-strand breaks, particularly at expanded TA repeats and regions of DNA damage.

WRN inhibitor 3 (example 110), a cyclic vinyl sulfone compound, is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor. WRN inhibitor 3 can be used for the research of cancer.

DHX9-IN-5 (compound 277) is a RNA helicase DHX9 inhibitor with an IC₅₀ of 4.3 nM.

WRN inhibitor 8 is an inhibitor of WRN helicase with an IC₅₀ value of 48 nM. WRN inhibitor 8 can inhibit the proliferation of tumor cells and be used in the study of cancer.

WRN inhibitor 5, a cyclic vinyl sulfone compound, is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor. WRN inhibitor 5 can be used for the research of cancer, including cancers characterized by microsatellite instability (MSI) and/or defective DNA mismatch repair system (dMMR).

Werner syndrome RecQ helicase-IN-3 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC₅₀ value of 0.06 µM. Werner syndrome RecQ helicase-IN-3 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-3 shows anticancer activity.

Adibelivir (IM-250) is an orally active helicase-primase inhibitor. Adibelivir is effective against HSV infection and reduces reactivation of latent HSV. Adibelivir inhibits HSV-1 infection in Vero cells (IC₅₀: ~20 nM). Adibelivir can be used for the study of recurrent herpes disease^[1][2]_.

Brr2-IN-3 is a potent and selective Brr2 helicase allosteric Inhibitor. Brr2-IN-3 inhibits helicase activity in dose-dependent manner with an IC₅₀ value of 1.3 μM.

Werner syndrome RecQ helicase-IN-4 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC₅₀ value of 0.06 µM. Werner syndrome RecQ helicase-IN-4 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-4 shows anticancer activity.

NCGC00029283 is a werner syndrome helicase-nuclease (WRN) helicase inhibitor with IC₅₀s of 2.3 μM, 12.5 μM, and 3.4 μM for WRN, BLM and FANCJ helicase, respectively.

WRN inhibitor 4 is a Werner Syndrome ATP-dependent helicase (WRN) inhibitor. WRN inhibitor 4 can be used for cancer research.

SY-589 is an orally active DNA polymerase Polθ helicase domain inhibitor (IC₅₀=2.29 nM) and DNA damage inducer. SY-589 inhibits the ATPase activity of the Polθ helicase domain and blocks the Polθ-mediated microhomology-mediated end joining (MMEJ) DNA repair pathway (IC₅₀=0.85 nM). SY-589 also induces the accumulation of DNA double-strand breaks by increasing γ-H2AX levels. SY-589 exerts antiproliferative effects on BRCA2-deficient cells and is used in the research of HR-deficient tumors.

WRN inhibitor 1 is a Wemer Syndrome ATP dependent helicase enzyme (WRN) inhibitor that inhibits WRN helicase domain activity. WRN inhibitor 1 can be used in the study of cancer.

MOMA-341 is a selective Werner RecQ like helicase (WRN) inhibitor. MOMA-341 binds to WRN at cysteine 727 through an allosteric and ATP-competitive binding mechanism. MOMA-341 has antitumor activity and can be used for advanced and metastatic solid tumors research.

Werner syndrome RecQ helicase-IN-2 (example 57) is a potent Werner syndrome RecQ DNA helicase enzyme (WRN) inhibitor and can be used in cancer research.

DHX9-IN-6 (Compound 620) is an ATP-dependent inhibitor of RNA helicase A (DHX9) with potential for cancer research.

DHX9-IN-4 (Compound 609) is an ATP-dependent inhibitor of RNA helicase A (DHX9) with potential for cancer research.

WRN inhibitor 11 (Example 17) is an orally active inhibitor of WRN helicase, with the IC₅₀ of 63 nM.