Home Transmembrane Transporters ATPase inhibitor - p97 inhibitor CB-5083

CB-5083

Catalog No.S8101

For research use only.

CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.

CB-5083 Chemical Structure

CAS No. 1542705-92-9

Selleck's CB-5083 has been cited by 33 publications

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Biological Activity

Description CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.
Targets
p97 AAA ATPase [1]
(Cell-free assay)
11 nM
In vitro

In A549 cells, CB-5083 causes significant K48 poly-ubiquitinated protein and CHOP accumulation as well as p62 reduction, and kills tumor cells with IC50 of 680 nM. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 M1nLdWZ2dmO2aX;uJIF{e2G7 NHfuXow3KGi{cx?= M2fobGlvcGmkaYTpc44hd2ZicEm3JGFVWGG|ZTDpckBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDwOlIheHKxdHXpckBqdmO3YnH0[YQh\m:{IE[gbJJ{KGK7IHntcZVvd2[udX;y[ZNk\W6lZTDhd5NigSxiSVO1NEA:KDBwNEmg{txONg>? NHPiUJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW2OVY3Pid-Mk[1OlU3PjZ:L3G+
A549 M4TKdWN6fG:2b4jpZ4l1gSCjc4PhfS=> MXm3NkBpenN? NEO3OJBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFczKGi{czDifUBE\WyudHn0[ZIuT2yxIHHzd4F6NCCLQ{WwJF0hOC54ODFOwG0v MnXtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkW2OlYoRjJ4NU[1OlY3RC:jPh?=
A549 MXjGeY5kfGmxbjDhd5NigQ>? NV3UPFVLPiCqcoO= Ml\TTY5pcWKrdHnvckBw\iCyOUegRXRR[XOnIHnuJIh2dWGwIFG1OFkh[2WubIOgZZN{\XO|ZXSgZZMh[WOldX31cIF1cW:wIH;mJGs1QCCyb3z5MZVjcXG3aYTpcoF1\WRicILveIVqdnNiaX7jeYJifGWmIH\vdkA3KGi{czDifUBqdW23bn;mcJVwemW|Y3XuZ4Uh[XO|YYmsJGlEPTBiPTCwMlY5KM7:TT6= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4NU[2Okc,OjZ3NkW2OlY9N2F-
A549 M{DidWZ2dmO2aX;uJIF{e2G7 NEDqV5E3KGi{cx?= M2K2PWlvcGmkaYTpc44hd2ZicEm3JGFVWGG|ZTDpckBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGGlY4XteYxifGmxbjDv[kBEUE:SIIDvcJkufWKrcYXpeIlv[XSnZDDwdo91\WmwczDpcoN2[mG2ZXSg[o9zKDZiaILzJIJ6KGmvbYXuc4ZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3MDC9JFEvODNizszNMi=> NUPMTmxXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1OlU3PjZpPkK2OVY2PjZ4PD;hQi=>
Vero E6 Mm\qSpVv[3Srb36gZZN{[Xl? MnfTOFghcHK| MYTJR|UxKG[xcjDhcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDTRXJUNUOxVj2yJIlvKHSqZTDW[ZJwKEV4IHPlcIwhdGmwZTDheEA1QCCqIHL5JIludXWwb3\seY9z\XOlZX7j[U1j[XOnZDDhd5NigSBqZHX0[YN1cW6pIITo[UB3cXKjbDDOVEBxem:2ZXnuJIlvKHSqZTDueYNt\XW|IH;mJJRp\SCYZYLvJGU3KGOnbHzzLU4tKEmFNUCgQUA1Njh7N{e5JO69VS5? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OjN3M{i1PUc,OzJ|NUO4OVk9N2F-
A549 M4nlWWZ2dmO2aX;uJIF{e2G7 M4CwflE2OCCvZz;r[y=> M17QdVIhfG9iMkSgbJJ{ NF[3bI5FenWpIIXweIFs\SCrbjDwcIF{dWFib3[gcY92e2VieHXuc4dz[W[2ZXSge4l1cCCqdX3hckBCPTR7IHPlcIx{KGG2IEG1NEBu\y:tZzygdI8hdWWjc4Xy[YQh[XRiMjD0c{AzPCCqcoO= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4NU[2Okc,OjZ3NkW2OlY9N2F-
A549 NX7SNnJLSW62aYT1cY9zKGG|c3H5 M1\US|ExOCCvZz;r[y=> MkfkRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczD4[Y5w\3KjZoTl[EBqdiCwdXTlJHNEUURiYnXp[4UhdW:3c3WgZZN{\XO|ZXSgZZMhfHWvb4Kg[5Jwf3SqIHnubIljcXSrb36gZZQhOTByIH3nM4toNCCybzDh[I1qdmm|dHXy[YQh[XNicXS0JI9vNzNib3\mJJdm\WuueTDzZ4hm\HWuZR?= MmHjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3NkW2OlYoRjJ4NU[1OlY3RC:jPh?=
A549 M4C0cGZ2dmO2aX;uJIF{e2G7 NUnmfGdyOTVyIH3nM4to MnezNkB1dyB{NDDodpM> MmHySJJ2\yC3cIThb4UhcW5iaIXtZY4hSTV2OTDj[YxteyC6ZX7v[5Ji\nSnZDDpckBud3W|ZTDheEAyPTBibXevb4ctKHCxIH3lZZN2emWmIHH0JFIhfG9iMkSgbJJ{ M2m2S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[1OlY3Lz5{NkW2OVY3PjxxYU6=
MDA-MB231 MX3GeY5kfGmxbjDhd5NigQ>? NHK3S5IyKHWP Mm\BPEBpenN? M1vV[WlvcGmkaYTpc44hd2ZicEm3JIlvKGi3bXHuJG1FSS2PQkKzNUBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCFSF;QJJBzd3SnaX6gcIV3\Wy|IHH0JFEhfU1iYX\0[ZIhQCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF|OUmyPUc,OjhzM{m5Nlk9N2F-
HCT116 MVLBcpRqfHWvb4KgZZN{[Xl? NIfMOJA4PSCvZz;r[y=> MmTlNVIh\GG7cx?= NH;UVVRCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMhgGWwb3fyZYZ1\WRiaX6gcpVl\SCvb4Xz[UBie3Onc4Pl[EBieyC2dX3vdkBoem:5dHigbY5pcWKrdHnvckBifCB5NTDt[{9s\yxicH:gdYQh\m:{IEGyJIRigXN? M3fNclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NU[1OlY3Lz5{NkW2OVY3PjxxYU6=
AMO1 M{GydWFvfGm2dX3vdkBie3OjeR?= MmjjNVAxKG2pL3vn MmTHRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQV3PNUBk\WyuczD4[Y5w\3KjZoTl[EBqdiCwdXTlJHNEUURiYnXp[4UhdW:3c3WgZZN{\XO|ZXSgZZMhfHWvb4Kg[5Jwf3SqIHnubIljcXSrb36gZZQhOTByIH3nM4toNCCybzDh[I1qdmm|dHXy[YQh[XNicXS0JI9vNzNib3\mJJdm\WuueTDzZ4hm\HWuZR?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4NU[2Okc,OjZ3NkW2OlY9N2F-
AMO1 MWHBcpRqfHWvb4KgZZN{[Xl? MlLHNUBu\y:tZx?= NHjNVXhCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBUW8yKGOnbHzzJJhmdm:pcnHmeIVlKGmwIH71[IUhW0OLRDDi[Ylo\SCvb4Xz[UBie3Onc4Pl[EBieyC2dX3vdkBoem:5dHigbY5pcWKrdHnvckBifCBzIH3nM4toNCCrdjDh[I1qdmm|dHXy[YQhfHerY3WgdIVzKHenZXu= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV4NU[2Okc,OjZ3NkW2OlY9N2F-
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot p-IRE1α / IRE1α / p-eIF2α / ATF4 ; p97 ; Bip / XBP1s / PERK / pEIF2α / CHOP 27729194 31316150 26555175
In vivo In mice bearing human HCT 116 colon tumor xenografts, CB-5083 (75 mg/kg, p.o.) significantly inhibits tumor growth. In mice bearing established human AMO-1 multiple myeloma and A549 lung carcinoma tumor xenografts, CB-5083 (100 mg/kg, p.o.) also results in significant tumor growth inhibition. [1]

Protocol (from reference)

Kinase Assay:[1]
  • ATPase assay:

    Compounds are diluted in DMSO with a 3-fold 10-point serial dilution starting at 10 μM. The assay is done in a 384-well plate with each row as a single dilution series with duplicate of each compound concentration point. In 5 μL total volume, 20 nM p97 hexameric enzyme and 20 μM ATP are added to start the reaction. The plate is sealed and incubated at 37 °C for 15 min after mixing thoroughly in an orbital shaker. Compound dilution, ATP and enzymes addition are conducted with automated liquid handling using the Freedom Evo. ADP Glo reagents 1 and 2 are added according to the manufacturer’s protocol. The luminescence is measured by Envision plate reader as the end point of the reaction. The IC50 of each compound is derived by fitting the luminescence values to a four-parameter sigmoidal curve.
Cell Research:[1]
  • Cell lines: A549 cells
  • Concentrations: ~40.0 μM
  • Incubation Time: 72 h
  • Method: A549 and other tumor cell lines are cultured according to ATCC guidelines. Cells are cultured in black or white, clear-bottomed, tissue culture-treated 384-well plates. Cells are treated with 10-point dose titration of the compound in well duplicates. After a 72 h treatment, CellTiter-Glo is added to the white plates to measure cell viability. Luminescence values are fit to a four-parameter sigmoidal curve to determine IC50 concentrations.
Animal Research:[1]
  • Animal Models: Nu/Nu nude female mice bearing human HCT 116 colon tumor xenografts
  • Dosages: 75 mg/kg, qd
  • Administration: p.o.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% CMC Na+5% Tween 80
For best results, use promptly after mixing.

 30mg/mL

Chemical Information

Molecular Weight 413.47
Formula

C24H23N5O2
CAS No. 1542705-92-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC2=C(C=CC=C2N1C3=NC4=C(COCC4)C(=N3)NCC5=CC=CC=C5)C(=O)N

In vivo Formulation Calculator (Clear solution)

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

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% DMSO % % Tween 80 % ddH2O
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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02243917 Terminated Drug: CB-5083 Advanced Solid Tumors Cleave Biosciences Inc. October 11 2014 Phase 1
NCT02223598 Terminated Drug: CB-5083|Drug: Dexamethasone Lymphoid Hematological Malignancies|Relapsed and Refractory Multiple Myeloma Cleave Biosciences Inc. August 25 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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Frequently Asked Questions

Question 1:
I am trying to administrate the compound to mice. Does this compound ever dissolve completely?

Answer:
S8101 CB-5083 can be dissolved in 0.5% CMC Na+5% Tween 80 at 30 mg/ml as a suspension for oral gavage.

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