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Napabucasin (BBI608)

For research use only.

Catalog No.S7977 Synonyms: BBI608

12 publications

Napabucasin (BBI608) Chemical Structure

CAS No. 83280-65-3

Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor.

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Selleck's Napabucasin (BBI608) has been cited by 12 publications

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Description Napabucasin (BBI608) is an orally available Stat3 and cancer cell stemness inhibitor.
Targets
Stat3 [1]
In vitro

Napabucasin downregulates stemness gene expression driven by Stat3 and cancer stemness properties, and effectively inhibits self-renewal of stemness-high cancer cells with IC50 ranged from 0.291~1.19 μM, on inhibition on normal stem cells. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human DU145 cells MlzySpVv[3Srb36gZZN{[Xl? M4\5c|czKGh? MUPBcpRq[2GwY3XyJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRGWxOFUh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IGjUWEBie3OjeTygTWM2OD1yLkCyN|A1KM7:TR?= Mlf4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh6MkmzNVYoRjF6OEK5N|E3RC:jPh?=
human HaCaT cells MVnGeY5kfGmxbjDhd5NigQ>? NE\qbY41QCCq NVPue5ViSW62aXj5dIVzeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEijQ3HUJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCyaHHz[UBkd262cnHzeEBucWO{b4Pjc5B6NCCLQ{WwQVAvPSEQvF2= NGfHSZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mki0OVAyPCd-MkK4OFUxOTR:L3G+
human HaCaT cells NX61OGZkWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFjhRXpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjhR4FVKGOnbHzzMEBKSzVyPUCuOUDPxE1? M4XU[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFyNEe5N|E6Lz5zMES3PVMyQTxxYU6=
KB cells MoWzR5l1d3SxeHnjbZR6KGG|c3H5 Ml;TSYZn\WO2aY\lJIN6fG:2b4jpZ{Bld3OnIHHnZYlve3RiS1KgZ4VtdHNid3HzJIV3[Wy3YYTl[EwhTUR3ME20MlIh|ryP MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek86QDd|NkG4K|46QDd|NkG4QE9iRg>?
MDA-MB-231 M1e3d2N6fG:2b4jpZ4l1gSCjc4PhfS=> MYe3NkBpenN? M1u1SGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFAvOzRizszNMi=> NXv1clFDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1OVg{OzNpPkK4OVU5OzN|PD;hQi=>
HepG2 M4TJSWN6fG:2b4jpZ4l1gSCjc4PhfS=> NYS4e5h3PzJiaILz NX;NNVJzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuOlYh|ryPLh?= M17hNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NUW4N|M{Lz5{OEW1PFM{OzxxYU6=
A549 NHzkTJJEgXSxdH;4bYNqfHliYYPzZZk> NHvrTm44OiCqcoO= NWjNeo9bS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMD63OEDPxE1w MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV3OEOzN{c,Ojh3NUizN|M9N2F-
K562 Mmi0RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NFi1S3k1QCCqcoO= NVT6doZ3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJI1m[XO3cnXkJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTCxJO69VS5? MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODByM{e3PEc,OzByMEO3O|g9N2F-
MDA-MB-231 M4jGNWZ2dmO2aX;uJIF{e2G7 MofhOEBpenN? MXXJcohq[mm2aX;uJI9nKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDheEB[PzB3IHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKHKjdHnvJI9nKHCqb4PwbI9zgWyjdHXkJHNVSVR|IITvJJRwfGGuIGPURXQ{KGyndnXsJIFnfGW{IESgbJJ{KGK7IFjUVmYh[XO|YYmsJGVEPTBiPTCxMlkh|ryPLh?= M2fJ[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMECzO|c5Lz5|MECwN|c4QDxxYU6=
MDA-MB-231 M1ThSmZ2dmO2aX;uJIF{e2G7 M3zGWFQhcHK| NGjFUW1KdmirYnn0bY9vKG:oIGPURXQ{KHCqb4PwbI9zgWyjdHnvckBifCC\N{C1JIlvKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZYZ1\XJiNDDodpMh[nliSGTSSkBie3OjeTygSWM2OCB;IEKg{txONg>? MoXJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByMEO3O|goRjNyMECzO|c5RC:jPh?=
MDA-MB-231 M3P4XGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mkj4OFghcHK| NX[3SlhTSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IH3lZZN2emWmIHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB{LkGg{txONg>? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODByM{e3PEc,OzByMEO3O|g9N2F-
HepG2 NHizXItCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NH73OG41QCCqcoO= M{CzUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPDT{05KGG|c3H5MEBKSzVyIE2gNVAvOiEQvF2u MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZyNEW0N{c,Ojl4MES1OFM9N2F-
L02 NFnYWHlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Mn\WOFghcHK| M1:w[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTECyJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFQ1utPEBie3OjeTygTWM2OCB;IEG4Mlch|ryPLh?= M1TSeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NkC0OVQ{Lz5{OU[wOFU1OzxxYU6=
MDA-MB-231 NXT3ZVh6TnWwY4Tpc44h[XO|YYm= MlfDNVAxKHWP NIDCNW8yKGi{ NFW0WHFDcW6maX7nJIFn\mmwaYT5JJRwKFOWQWSzJIlvKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZZQhOTByIIXNJJRz\WG2ZXSg[o9zKDFiaIKg[o9tdG:5ZXSgZpkhfGincn3vcJl{cW5iYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOzBibXnud{BjgSCGQWLUV{1Y\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODByM{e3PEc,OzByMEO3O|g9N2F-
MDA-MB-231 NVjtTIVZTnWwY4Tpc44h[XO|YYm= NXqwb2V4PSC3bX;sM2w> NHTCcoQzPCCqcoO= NHjKZYxKdmS3Y4Tpc44hd2Zic4Xw[ZJwgGmmZTDn[Y5memG2aX;uJIlvKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZZQhPSC3bX;sM2whdWWjc4Xy[YQh[W[2ZYKgNlQhcHK|IHL5JGRJTSC|dHHpcolv\yCkYYPl[EBndG:5IHP5eI9u\XS{eR?= Ml\yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzByMEO3O|goRjNyMECzO|c5RC:jPh?=
MDA-MB-231 NFLjVJhHfW6ldHnvckBie3OjeR?= NWj1XYNoPSC3bX;sM2w> NHL3XVUzPCCqcoO= MWXJcoR2[3Srb36gc4Yhe3WyZYLvfIll\SCpZX7ldoF1cW:wIHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYSgOUB2dW:uL1ygcYVie3W{ZXSgZYZ1\XJiMkSgbJJ{KGmwIIDy[ZNmdmOnIH;mJG5SVzFiaX7obYJqfG:{IHTpZ492dWG{b3ygZpkhTEiHIIP0ZYlvcW6pIHLhd4VlKG[ub4egZ5l1d22ndIL5 MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODByM{e3PEc,OzByMEO3O|g9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CDK4 / Cyclin D1; 

PubMed: 31277685     


U87MG and LN229 cells were treated with the vehicle or 5 μM Napabucasin for 48 h. Then, cell lysates were analyzed by western blotting.

STAT3 / β-catenin / c-Myc; 

PubMed: 31277685     


GSCs (glioma stem cells) under the indicated conditions were harvested and subjected to western blotting. 

c-Myc / Nanog / Bmi-1 / Axl / Sox2 / Klf4 / β-catenin / Survivin; 

PubMed: 25605917     


FaDu cancer stem cells were treated for 3, 6, or 24 h with BBI608 at either 1 or 2 μM or with DMSO (0). Cell lysates from these treated cells were then analyzed by Western blotting. BBI608 down-regulates a number of stemness related proteins involved in t䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ瑖堘𢡄빢᎒

31277685 25605917
Immunofluorescence
STAT3; 

PubMed: 31277685     


IF was used to estimate the expression of STAT3 in U87MG and LN229 cells after treatment with Napabucasin (scale bar: 50 μm).

Cleaved caspase-3 ; 

PubMed: 31277685     


Immunofluorescence staining of glioma cells treated with the vehicle or Napabucasin. Nuclei were stained with DAPI (blue). Scale bar = 50 μm.

31277685
Growth inhibition assay
Cell viability ; 

PubMed: 31277685     


Proliferation of glioma cells treated with Napabucasin and detected by CCK-8 assays. Half maximal inhibitory concentrations (IC50) of Napabucasin in U87MG and LN229 cells were 6.4 and 5.6 μM respectively. 

31277685
In vivo In mice bearing PaCa-2 xenografts, Napabucasin (20 mg/kg, i.p.) significantly inhibits tumor growth, relapse and metastasis. [1]

Protocol

Cell Research:

[1]

- Collapse
  • Cell lines: Cancer stem cells U87-MG, U118, COLO205, DLD1, SW480, HCT116, FaDu, ACHN, SNU-475, Huh7, HepG2, H1975, A549, H460, CAOV-3, SW-626, PaCa2.
  • Concentrations: ~2 μM
  • Incubation Time: 72 h
  • Method:

    For cancer stem cells, spheres are dissociated and plated under cancer stem cell culture conditions on coated 96-well plates. After 72 h of culture, wells are dosed with the indicated compounds. Seventy-two hours or 24 h after dosing, CellTiter-Glo 2.0 is added to each well, and the luminescence is measured as described by the manufacturer. IC50 values are calculated by fitting a four parameter dose–response curve to normalized data using GraphPad Prism software. For bulk cells, cells are plated at 5,000 cells per well on 96-well plates. Twenty-four hours after plating, cells are treated with the indicated compounds. Viability is determined at 72 h as described above.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: Mice bearing PaCa-2 xenografts
  • Dosages: 20 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 10 mg/mL (41.63 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
1mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 240.21
Formula

C14H8O4

CAS No. 83280-65-3
Storage powder
in solvent
Synonyms BBI608
Smiles CC(=O)C1=CC2=C(O1)C(=O)C3=CC=CC=C3C2=O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID