research use only

RK-33 DNA/RNA Synthesis inhibitor

Name: RK-33
Brand: Selleck Chemicals
SKU: S8246
Availability: InStock
Rating: 5 (24 reviews)

Cat.No.S8246

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.

Chemical Structure

Molecular Weight: 428.44

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.49%

99.49

Related Targets	CDK Microtubule Associated Ras HSP PD-1/PD-L1 Aurora Kinase Casein Kinase Rho Serine/threonin kinase eIF Chk ROCK Myc Kinesin PLK DHFR PAK PERK DYRK RUNX PP2A PFKFB AP-1 MPS1 Wee1 p21 BMI-1 LIM kinase Nur77 APC
Related Products	CX-5461 (Pidnarulex) SCR7 Favipiravir (T-705) Carmofur Triapine (3-AP) B02 BMH-21 YK-4-279 Bergapten Tegafur (FT-207) Azaguanine-8 Halofuginone Adenine HCl Mizoribine Cyclocytidine HCl Thymidine APX-3330 Nedaplatin 6-Thio-dG Flupirtine maleate JH-RE-06 Pritelivir (BAY 57-1293) TK216 Amenamevir Madrasin Tubercidin BC-LI-0186 CRT0044876 PFM01 Adenine

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Chemical Information, Storage & Stability

Molecular Weight	428.44	Formula	C₂₃H₂₀N₆O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1070773-09-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	COC1=CC=C(C=C1)CN2C=NC3=C2N=CN=C4C3=NC(=O)N4CC5=CC=C(C=C5)OC

Solubility

In vitro
Batch:

DMSO : 40 mg/mL (93.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (4.67mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.700mg/ml (1.63mM)	Taking the 1 mL working solution as an example, add 50 μL of 14 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	DDX3 ^[1]
In vitro	RK-33 binds specifically to DDX3, but not to the closely related proteins DDX5 and DDX17. This compound inhibits cancer growth and radiosensitizes lung cancer cells in a DDX3-dependent manner. It has no effect on either mitochondrial respiration or ATP generation. This chemical curbs proliferation and induces apoptosis in a DDX3-dependent fashion. Wnt signaling is mediated by DDX3 and inhibited by RK-33. It impairs radiation-induced DNA damage repair by inhibiting NHEJ activity^[1].
In vivo	RK-33 in combination with radiation induces tumor regression in multiple mouse models of lung cancer. This compound, at the dose used, is non-toxic in SCID mice. This chemical-treated mice do not exhibit any discernable morphological changes^[1].
References	[1] https://pubmed.ncbi.nlm.nih.gov/25820276/

Applications

Methods	Biomarkers	Images	PMID
Western blot	DDX3 Cyclin D1 / Cyclin E1		30292066
Growth inhibition assay	Cell viability		27634756

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):