Catalog No.S1575

RO4929097 Chemical Structure

Molecular Weight(MW): 469.4

RO4929097 is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2.

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In DMSO USD 238 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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Cited by 17 Publications

7 Customer Reviews

  • (d,e) Effect of TUG1 overexpression on Nestin activity. Plasmid vectors expressing indicated genes were added to GSC-pE-Nes-222 treated with RO4929097. Phase-contrast and Nestin-EGFP images were shown in (d). Scale bars, 100 μm. (e) Intensity of Nestin-EGFP (left) and number of viable cells (right) compared with the DMSO control were quantified. Viable cells were assessed by trypan blue staining. *P<0.01, Kruskal–Wallis analysis. For all the experimental data, error bars indicate +s.d. (n=3).

    Nat Commun, 2016, 7:13616. RO4929097 purchased from Selleck.

    Western blot analysis of MDA-MB-231 cells treated with CCL2/7/8 or PBS in the presence or absence of a γ-secretase inhibitor (GSI) RO4929097 (10 μmol/L).

    Clin Cancer Res, 2018, 24(10):2370-2382. RO4929097 purchased from Selleck.

  • (F–H) Representative z-projection confocal images of the principal islets in dissected pancreata (post-paraformaldehyde fixation) fromTg(ins:hmgb1-EGFP; β/δ-reporter ) triple transgenic lines treated with DMSO (F), paroxetine (G), or RO4929097 (H). Shown are EGFP+ β-cell nuclei (green) and TagRFP+ δ cells (red); note, PhiYFP in the β/δ-reporter line does not withstand fixation, allowing ‘clean‘ labeling of β-cell nuclei with EGFP. In addition, apparent overlap between the β-cell and δ-cell markers (i.e., occasional ‘yellow‘ cells) is an artifact of z-projection images shown in 2D format. For clarity, the inset panels show a single z-slice image of partial islet showing no co-localization of cell type specific reporters.

    Elife, 2015, doi:10.7554/eLife.08261. RO4929097 purchased from Selleck.

    Stem Cells 2014 32(1), 301-12. RO4929097 purchased from Selleck.

  • Stem Cells 2014 32(1), 301-12. RO4929097 purchased from Selleck.

    left, Increasing doses (0 μmol/L, 3 μmol/L, 30 μmol/L) of GSI RO4929097 inhibits sphere formation in RD and SMS-CTR spheres; right, Expression of YAP5SA in the presence of GSI restores sphere formation.

    Mol Cancer Res, 2017, 15(12):1777-1791. RO4929097 purchased from Selleck.

  • Melanoma growth inhibition by the concomitant treatment with a TKI and the GSI inhibitor RO4929097. WM266-4, K457 and SK-Mel2 human metastatic melanoma cells were treated for four days in culture with a tyrosine kinase inhibitor (TKI at 20 mM), and the GSI RO4929097 (RO at 10 mM), either alone or in combination. All treatments significantly reduced cell growth except for RO4929097 on K457 cells. The highest level of inhibition was observed with TKI in combination with RO4929097. Growth was evaluated by the crystal violet staining.



    2012 Dr. Barbara Bedogni of Case Western Reserve University. RO4929097 purchased from Selleck.

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Biological Activity

Description RO4929097 is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2.
γ secretase [1]
(Cell-free assay)
γ secretase(ICN) [1]
(Cell-free assay)
Aβ40 [1]
(Cell-free assay)
4 nM 5 nM 14 nM
In vitro

RO4929097 decreases the amount of Aβ peptides secreted into the culture medium in HEK293 cells with EC50 of 14 nM. RO4929097 strongly inhibits Notch processing with EC50 of 5 nM in the Notch cell-based reporter assay. The potency of RO4929097 in cell-free and cellular assays is in the low nanomolar range with >100-fold selectivity observed with respect to 75 other proteins of various types including receptors, ion channels, and enzymes (CEREP panel). After 5 days of treatment, RO4929097 reduces the production of ICN in the human NSCLC A549 cells inducing a flattened and less transformed tumor cell phenotype in tissue culture. [1] RO4929097 blocks Notch processing in human non-small cell lung carcinoma cells and decreases expression of the Notch transcriptional target gene Hes1. Treatment with RO4929097 reveals a two- to threefold decrease in the expression of direct Notch target genes, Hes1, Hey1, and Heyl in SUM149 and a 3.5- to eightfold decrease in expression in SUM190 cells. RO4929097 modestly inhibits the growth of SUM149 cells in a dose-dependent manner. At a concentration of 1 μM of RO4929097, growth inhibition is 20 % for SUM149 and 10 % for SUM190 cells, relative to vehicle-treated controls. RO4929097 decreases the production of inflammatory cytokines by T-cells. Furthermore, with RO4929097 treatment, there is a shift in favor of TH2 over TH1 cytokines. In addition, T-cell activation induced IL-6 production would be increased with RO4929097. [2] Upon RO4929097 treatment, the selected melanoma cell lines reveals downregulation of NOTCH downstream effector HES1. A decrease in the amount of melanospheres formed upon RO4929097 treatment in primary melanoma cell lines is detected. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U87 NG\ydYdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFnicY0{OCEQvF2= M2f2O|Qh\A>? NG\MdFJl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm= M3W2[VI1PDl3OUC3
U87 R1 M4W0XGNmdGxiVnnhZoltcXS7IFHzd4F6 MW[zNEDPxE1? M{DxS|Qh\A>? MVrk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHl? MXuyOFQ6PTlyNx?=
MGG4 MnX0R4VtdCCYaXHibYxqfHliQYPzZZk> MlzNN|Ah|ryP M4fORlQh\A>? M1vOeIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eR?= NYrUPXBMOjR2OUW5NFc>
MGG6 MVLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4TsdFMxKM7:TR?= MXu0JIQ> NEjrVIdl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm= M2P1SFI1PDl3OUC3
MGG8 Mn;4R4VtdCCYaXHibYxqfHliQYPzZZk> NXnHOIhEOzBizszN M3HuWFQh\A>? NGXLd2ll\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm= NGXM[m8zPDR7NUmwOy=>
MGG23 NYXIZpZqS2WubDDWbYFjcWyrdImgRZN{[Xl? NHnNcIo{OCEQvF2= NVnSN2ZlPCCm M1vL[IRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eR?= NIL5d|AzPDR7NUmwOy=>
SUM149 M3XKOmNmdGxiVnnhZoltcXS7IFHzd4F6 M4P1blAuOTBizszN MknCO|IhcA>? M1\QeIlvcGmkaYTzJINmdGxiZ4Lve5RpKGSxc3Wg[IVx\W6mZX70cJk> NF[4T2wzOjV2N{GwPS=>
Sum190 NV\lT5hFS2WubDDWbYFjcWyrdImgRZN{[Xl? Mni0NE0yOCEQvF2= NELa[Gk4OiCq NX7Ddnh7cW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? Mke5NlI2PDdzMEm=
WM35 MlPSSpVv[3Srb36gRZN{[Xl? NXj5bZlEOTBidV2= NFS1bHMzPCCq MX7EUXNQ M4q3UoRm[3KnYYPld{B1cGVibHX2[Yx{KG:oIF7PWGNJKGSxd37zeJJm[W1idHHy[4V1KEiHU{G= MnjsNlE6QDB2MEi=
WM98.1 M3j3bmZ2dmO2aX;uJGF{e2G7 MmPjNVAhfU1? MkPqNlQhcA>? NYnBW2x{TE2VTx?= Mmjk[IVkemWjc3XzJJRp\SCuZY\lcJMhd2ZiTl;UR2gh\G:5boP0doVidSC2YYLn[ZQhUEWVMR?= NWrFN5AyOjF7OEC0NFg>
WM115 MkGySpVv[3Srb36gRZN{[Xl? MkDZNVAhfU1? NWTUZlloOjRiaB?= MoiwSG1UVw>? MWPk[YNz\WG|ZYOgeIhmKGyndnXsd{Bw\iCQT2TDTEBld3ewc4Ty[YFuKHSjcnfleEBJTVNz NFTXV2UzOTl6MESwPC=>
WM983A NFziVXpHfW6ldHnvckBCe3OjeR?= NEPhfFIyOCC3TR?= MmDGNlQhcA>? MoXwSG1UVw>? M3Tp[IRm[3KnYYPld{B1cGVibHX2[Yx{KG:oIF7PWGNJKGSxd37zeJJm[W1idHHy[4V1KEiHU{G= M{noXFIyQThyNEC4
WM3248  NGXpco1HfW6ldHnvckBCe3OjeR?= Ml6zNVAhfU1? Mkm3NlQhcA>? M4e2NGROW09? NGXvPYdl\WO{ZXHz[ZMhfGinIHzleoVteyCxZjDOU3REUCCmb4fud5Rz\WGvIIThdodmfCCKRWOx NWHmXWhzOjF7OEC0NFg>
WM35 M2jNR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4r5[FExKHWP M{DPWFAuOThiZB?= NIrzd3NFVVOR Ml2wbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MkDmNlE6QDB2MEi=
WM98.1 NXPEO3FDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrpNZgyOCC3TR?= NGHR[ZAxNTF6IHS= NVHJe2JNTE2VTx?= NUW0UGdDcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? NX3Nb2JXOjF7OEC0NFg>
WM115 M2jMOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\hO|ExKHWP NWXYV4pIOC1zODDk M{DPTGROW09? M1;oRYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NHvMcHkzOTl6MESwPC=>
WM983A M2fiTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUCyR3lEOTBidV2= MVGwMVE5KGR? MWTEUXNQ NUewfmhGcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? NWLxR3hwOjF7OEC0NFg>
WM3248  MlHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFi5cGkyOCC3TR?= NI\hdJkxNTF6IHS= MVHEUXNQ Mn71bY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NVjNfXd2OjF7OEC0NFg>

... Click to View More Cell Line Experimental Data

In vivo Oral injection of 3 to 60 mg/kg RO4929097 once daily or twice daily to nude mice bearing A549 NSCLC xenografts for either 7, 14, or 21 days of a 21-day schedule results in significant tumor growth inhibition compared with vehicle-treated animals. The tumor growth inhibition values ranges from 66% to 91%. When mice are treated with 60 mg/kg RO4929097 twice daily with the 7+/14- schedule, treatment initially arouses regression of established A549 tumors. At the end of the 21-day cycle (day 47), tumor growth prevention is still 91% compared with vehicle control mice. Inhibition of tumor growth remains prolonged and sustained up to 34 days post-treatment (day 67). On day 67, these mice are retreated with the same dose of RO4929097 for a second cycle (7 days) until day 74. Importantly, the antitumor effects are sustained after dosing is completed. [1] RO4929097 leads to reduced expression of genes associated with angiogenesis in A549 xenograft model. In contrast, the RO4929097-resistant H460a xenograft displays little change in expression of these genes, underscoring the in vivo anti-angiogenesis mechanism of action of RO4929097.[2] For IL6 and IL8 overexpressing tumors, RO4929097 no longer impacts angiogenesis or the infiltration of tumor associated fibroblasts. [4]


Kinase Assay:[5]
+ Expand

In vitro potency assays:

After RO4929097 is used, the Aβ peptides are measured by ECL assays using a variety of anti-Aβ antibodies and an Origen 1.5 Analyzer. The 4G8 murine mAb binds an epitope in the Aβ peptide (within amino acids 18–21) that is immediately distal to the α-secretase cleavage site. The G2–10 murine mAb binds the C terminus that is exposed after γ-secretase-mediated cleavage to generate amino acid 40 of the Aβ40 peptide. The FCA3542 rabbit antibody binds the C terminus that is exposed after γ-secretase-mediated cleavage to generate amino acid 42 of the Aβ42 peptide. The 4G8 mAb is biotinylated with biotin-LC-sulfo-N-hydroxysuccinimide-ester. The G2–10 and FCA3542 antibodies are ruthenylated with TAG-N-hydroxysuccinimide ester. Aβ(x-40) is detected with biotinylated 4G8 and ruthenylated G2–10. Aβ(x-42) is detected with biotinylated 4G8 and ruthenylated FCA3542.
Cell Research:[3]
+ Expand
  • Cell lines: WM35 and WM98.1 cell lines
  • Concentrations: 10 μM
  • Incubation Time: DMSO
  • Method: Primary melanoma cell lines, including WM35 and WM98.1, are seeded at 2.5 × 103 cells per well on a 12-well dish in triplicate. The day after (day 0), the medium is replaced, and DMSO or 10 μM RO4929097 is added and changed every 3-4 days. At the indicated time points, cells are fixed in 10% formalin solution and stored in PBS at 4 °C. At day 18-24, all the plates are stained with crystal violet. After color elution with 10% acetic acid, optical density is read at 590 nm.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Female nude mice bearing Calu-6 cells
  • Formulation: 1.0% Klucel in water with 0.2% Tween 80
  • Dosages: 3 to 60 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 93 mg/mL (198.12 mM)
Ethanol 16 mg/mL (34.08 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween+ddH2O
For best results, use promptly after mixing.

* 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 469.4


CAS No. 847925-91-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01269411 Terminated Adult Anaplastic Oligodendroglioma|Adult Brain Stem Glioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Recurrent Adult Brain Tumor National Cancer Institute (NCI) July 2011 Phase 1
NCT01269411 Terminated Adult Anaplastic Oligodendroglioma|Adult Brain Stem Glioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Recurrent Adult Brain Tumor National Cancer Institute (NCI) July 2011 Phase 1
NCT01238133 Terminated Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Stage IIA Breast Cancer|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Triple-Negative Breast Carcinoma National Cancer Institute (NCI) December 2010 Phase 1
NCT01122901 Terminated Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Tumor National Cancer Institute (NCI) December 2010 Phase 2
NCT01251172 Withdrawn DS Stage I Plasma Cell Myeloma|DS Stage II Plasma Cell Myeloma|DS Stage III Plasma Cell Myeloma|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) December 2010 Phase 2
NCT01270438 Withdrawn Adenocarcinoma of the Colon|Adenocarcinoma of the Rectum|Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer National Cancer Institute (NCI) December 2010 Phase 2

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.

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Frequently Asked Questions

  • Question 1:

    How about the half-life of RO4929097(S1575)?

  • Answer:

    For S1575, the half-life is about 20 hours based on the following paper:

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID