Home Cell Cycle DNA/RNA Synthesis inhibitor - Apoptosis related activator RK-33 For research use only.

RK-33

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.

RK-33 Chemical Structure

RK-33 Chemical Structure

CAS No. 1070773-09-9

Purity & Quality Control

RK-33 Related Products

Signaling Pathway

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by WST1 assay, IC50 = 2.5 μM. 21572541
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by WST1 assay, IC50 = 2.56 μM. 23290252
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by WST1 assay, IC50 = 2.8 μM. 21572541
H460 Cytotoxicity assay 72 hrs Cytotoxicity against human H460 cells after 72 hrs by WST1 assay, IC50 = 2.87 μM. 23290252
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by WST1 assay, IC50 = 4.01 μM. 21572541
MDA-MB-231 Cytotoxicity assay 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by WST1 assay, IC50 = 4.05 μM. 23290252
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by WST1 assay, IC50 = 4.8 μM. 21572541
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by WST1 assay, IC50 = 4.9 μM. 23290252
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by WST1 assay, IC50 = 7.5 μM. 21572541
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by WST1 assay, IC50 = 7.59 μM. 23290252
OVCAR3 Cytotoxicity assay 72 hrs Cytotoxicity against human OVCAR3 cells after 72 hrs by WST1 assay, IC50 = 14.5 μM. 21572541
OVCAR3 Cytotoxicity assay 72 hrs Cytotoxicity against human OVCAR3 cells after 72 hrs by WST1 assay, IC50 = 14.5 μM. 23290252
Click to View More Cell Line Experimental Data

Biological Activity

Description 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.
Targets
DDX3 [1]
In vitro
In vitro RK-33 binds specifically to DDX3, but not to the closely related proteins DDX5 and DDX17. RK-33 inhibits cancer growth and radiosensitizes lung cancer cells in a DDX3-dependent manner. RK-33 has no effect on either mitochondrial respiration or ATP generation. RK-33 curbs proliferation and induces apoptosis in a DDX3-dependent fashion. Wnt signaling is mediated by DDX3 and inhibited by RK-33. RK-33 impairs radiation-induced DNA damage repair by inhibiting NHEJ activity[1].
Cell Research Cell lines MDA-MB-231 cells
Concentrations 7.5 μM
Incubation Time 12 h
Method

Healthy, 60-70% confluent MDA-MB-231 cells are transduced with shDDX3 lentivirus particles. Knockdown of DDX3 expression is confirmed both by qRT-PCR and immunoblotting. MDA-MB-231 cells are treated with RK-33 (7.5 μM) for 12 h and harvested for RNA. Microarray experiments are performed.
Experimental Result Images Methods Biomarkers Images PMID
Western blot DDX3 Cyclin D1 / Cyclin E1 30292066
Growth inhibition assay Cell viability 27634756
In Vivo
In vivo RK-33 in combination with radiation induces tumor regression in multiple mouse models of lung cancer. RK-33, at the dose used, is non-toxic in SCID mice. RK-33-treated mice do not exhibit any discernable morphological changes[1].
Animal Research Animal Models SCID mice
Dosages 20 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 428.44 Formula

C23H20N6O3
CAS No. 1070773-09-9 SDF Download RK-33 SDF
Smiles COC1=CC=C(C=C1)CN2C=NC3=C2N=CN=C4C3=NC(=O)N4CC5=CC=C(C=C5)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 40 mg/mL ( (93.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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