RK-33

Catalog No.S8246

For research use only.

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

CAS No. 1070773-09-9

Selleck's RK-33 has been cited by 14 publications

Purity & Quality Control

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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

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 MoHPR5l1d3SxeHnjbZR6KGG|c3H5 NXzMV4tKPzJiaILz MkLWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC3NkBpenNiYomgW3NVOSCjc4PhfUwhUUN3MDC9JFIvPSEQvF2u MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTV5MkW0NUc,OjF3N{K1OFE9N2F-
A549 MYTDfZRwfG:6aXPpeJkh[XO|YYm= MoeyO|IhcHK| MnqwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC3NkBpenNiYomgW3NVOSCjc4PhfUwhUUN3MDC9JFIvPTZizszNMi=> Mn7GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{OUCyOVIoRjJ|MkmwNlUzRC:jPh?=
H460 M3GxXmN6fG:2b4jpZ4l1gSCjc4PhfS=> NGDaSGw4OiCqcoO= MXnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIOFYxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDXV3QyKGG|c3H5MEBKSzVyIE2gNk45KM7:TT6= M{jqd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUeyOVQyLz5{MUW3NlU1OTxxYU6=
H460 NWewNHdIS3m2b4TvfIlkcXS7IHHzd4F6 M1HFblczKGi{cx?= M1vTU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGg1PjBiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHdUXDFiYYPzZZktKEmFNUCgQUAzNjh5IN88UU4> NXnPT4dvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyPVAzPTJpPkKzNlkxOjV{PD;hQi=>
MDA-MB-231 M1[2RmN6fG:2b4jpZ4l1gSCjc4PhfS=> MVy3NkBpenN? MmH1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB5MjDodpMh[nliV2PUNUBie3OjeTygTWM2OCB;IESuNFEh|ryPLh?= NFrKc4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3NlU1OSd-MkG1O|I2PDF:L3G+
MDA-MB-231 NXzEUphWS3m2b4TvfIlkcXS7IHHzd4F6 NHfm[HU4OiCqcoO= MlviR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB5MjDodpMh[nliV2PUNUBie3OjeTygTWM2OCB;IESuNFUh|ryPLh?= NXLyV5M2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyPVAzPTJpPkKzNlkxOjV{PD;hQi=>
PC3 M4P2emN6fG:2b4jpZ4l1gSCjc4PhfS=> NEX5PFc4OiCqcoO= NHrTdoZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHdUXDFiYYPzZZktKEmFNUCgQUA1NjhizszNMi=> NFTLcJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3NlU1OSd-MkG1O|I2PDF:L3G+
PC3 NV3OeHhZS3m2b4TvfIlkcXS7IHHzd4F6 MlexO|IhcHK| MWPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGfTWFEh[XO|YYmsJGlEPTBiPTC0Mlkh|ryPLh?= NEfGelI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K5NFI2Oid-MkOyPVAzPTJ:L3G+
MCF7 MnGzR5l1d3SxeHnjbZR6KGG|c3H5 NVPhc4dCPzJiaILz MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDXV3QyKGG|c3H5MEBKSzVyIE2gO{42KM7:TT6= M2PPXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUeyOVQyLz5{MUW3NlU1OTxxYU6=
MCF7 MoLMR5l1d3SxeHnjbZR6KGG|c3H5 NHL1NIY4OiCqcoO= M3LQPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHdUXDFiYYPzZZktKEmFNUCgQUA4NjV7IN88UU4> M2nVdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkmwNlUzLz5{M{K5NFI2OjxxYU6=
OVCAR3 NI\DT2dEgXSxdH;4bYNqfHliYYPzZZk> NFrXe|U4OiCqcoO= M4r4ZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG9XS0GUMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhX1OWMTDhd5NigSxiSVO1NEA:KDF2LkWg{txONg>? MmjQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{K1OFEoRjJzNUeyOVQyRC:jPh?=
OVCAR3 M4qwdmN6fG:2b4jpZ4l1gSCjc4PhfS=> MWi3NkBpenN? NYnwfox4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hV1[FQWKzJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCZU2SxJIF{e2G7LDDJR|UxKD1iMUSuOUDPxE1w M17kWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkmwNlUzLz5{M{K5NFI2OjxxYU6=
Assay
Methods Test Index PMID
Western blot DDX3 ; Cyclin D1 / Cyclin E1 30292066 25820276
Growth inhibition assay Cell viability 27634756
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].

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: SCID mice
  • Dosages: 20 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 428.44
Formula

C23H20N6O3

CAS No. 1070773-09-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=CC=C(C=C1)CN2C=NC3=C2N=CN=C4C3=NC(=O)N4CC5=CC=C(C=C5)OC

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