rna helicase

Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase and a potent first-in-class anti-cancer agent, inducing cell apoptosis and inhibiting the growth of TNBC cancer cell lines (IC50s: 10 nM - 20 nM).

Brr2-IN-3 (Brr2 Inhibitor C9) is an allosteric inhibitor of the spliceosomal RNA helicase Brr2. Brr2 is implicated in autosomal-dominant retinitis pigmentosa (a group of progressive retinal degenerative disorders).

YK 4-279, an inhibitor of RNA Helicase A (RHA), binds to the oncogenic transciption factor EWS-FLI1.

HRO761 (Werner syndrome RecQ helicase-IN-1, Example 42) is a small molecule inhibitor, a potent WRN inhibitor with high efficacy, and can be used for research on cancers such as colon cancer and gastric cancer.

MIRA-1 (WRN Helicase Inhibitor) is a restorer of wild-type p53 conformation/cellular function and selectively inhibits Werner syndrome WRN helicase activity with an IC50 of 20 µM.

NCGC00029283 is a potent inhibitor of Werner syndrome helicase-nuclease (WRN), displaying inhibitory activity against WRN helicase with an IC 50 value of 2.3 μM. Additionally, it exhibits inhibitory effects on Bloom syndrome protein helicase (BLM) and Fanconi anemia group J protein helicase (FANCJ) with IC 50 values of 12.5 μM and 3.4 μM, respectively.

CMLD012073 is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. It inhibits NIH/3T3 cells (IC50: 10 nM). CMLD012073 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A).

GBM CSCs-IN-1 (Compound (−)-20), a rocaglate derivative, potently inhibits glioblastoma stem cells (GBM CSCs) and exhibits an EC50 of 45 nM by targeting the RNA helicase DDX3. Additionally, it induces apoptosis in these cells.

SARS-CoV-2 nsp13-IN-7 (Compound 6r) is an inhibitor of SARS-CoV-2 nsp13, with an IC50 of 0.28 μM. This compound disrupts the helicase function of nsp13 by binding to its 5' RNA site and ATP binding site, and it serves as a lead compound for developing antiviral drugs targeting SARS-CoV-2 nsp13.

Fli-1-IN-1 (compound 21) fumarate is an FLI1-targeting agent that binds directly to and inhibits the interaction of the EWS-FLI1 protein. Since EWS-FLI1 interacts with RNA helicase A, Fli-1-IN-1 fumarate's inhibition of EWS-FLI1 suggests potential anticancer properties.

DHX9-IN-18 is an inhibitor of RNA helicase DHX9 with an EC50 of 16.4 μM and a biochemical infection point of 0.32 μM. This compound can be used as a research tool in cancer-related research fields.

CHIKV nsP2 protease-IN-2 (Compound 2o) is an allosteric inhibitor of the non-structural protein 2 helicase (nsP2hel), with IC50 values of 0.5 μM for nsP2 ATPase and 0.9 μM for RNA helicase. It exhibits broad-spectrum antiviral activity against alphaviruses, effectively targeting Chikungunya virus (CHIKV), Mayaro virus (MAYV), and Venezuelan equine encephalitis virus (VEEV), with an EC50 of 0.12 μM against CHIKV-nLuc. This compound is useful for research on alphavirus infections.

Pritelivir (BAY 57-1293) (BAY 57-1293) is a potent helicase-primase inhibitor with active against HSV-1 and HSV-2 (IC50: 20 nM).

Avenanthramide A is a naturally occurring, orally active plant defensin that binds to and inhibits RNA helicase DDX3, induces mitochondrial swelling and CRC cell apoptosis, increases ROS production, exhibits antitumor activity, and can be used in colorectal cancer research.

Amenamevir (ASP2151) is a novel helicase-primase inhibitor that is active against varicella-zoster virus and herpes simplex virus types 1 and 2 (EC50: 14 ng/mL).

ML216 (CID-49852229) is a small molecule inhibitor of BLM helicase with an IC50 of 1.8 μM, demonstrating 28-fold selectivity against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC50s > 50 μM).

RK33 (RK 33) is a first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells.

DHX9-IN-2 is an inhibitor targeting ATP-dependent RNA de-helicase A (DHX9) with anticancer and antitumor activity for cancer research.

DHX9-IN-1 is an inhibitor of ATP-dependent RNA helicase DHX9, with an intracellular EC50 value of 6.94 μM. DHX9-IN-1 exhibits antitumor activity and can be used for the research of DHX9-related cancers.

DHX9-IN-10 (49) serves as an inhibitor of the RNA helicase DHX9, exhibiting an EC50 of 9.04 μM for DHX9 cellular target engagement. It is primarily utilized in cancer research [1].

DHX9-IN-11 (469) serves as an inhibitor of the RNA helicase DHX9, exhibiting an EC 50 value of 0.0838 μM in assays measuring cellular target engagement. This compound is utilized in cancer research [1].

DHX9-IN-12 (83) serves as an inhibitor of the RNA helicase DHX9, exhibiting an EC 50 of 0.917 μM for DHX9 cellular target engagement. It is utilized in the field of cancer research [1].

DHX9-IN-13 (389) serves as an inhibitor of the RNA helicase DHX9, demonstrating a cellular target engagement EC50 of 3.4 μM. It is primarily utilized in cancer research [1].

DHX9-IN-14 (161), an RNA helicase DHX9 inhibitor, has an EC50 of 3.4 μM in DHX9 cellular target engagement and is utilized in cancer research [1].