For research use only.

Catalog No.S1575

81 publications

RO4929097 Chemical Structure

CAS No. 847925-91-1

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 238 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's RO4929097 has been cited by 81 publications

Purity & Quality Control

Choose Selective Gamma-secretase Inhibitors

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 M2PjW2NmdGxiVnnhZoltcXS7IFHzd4F6 NWnlO3ZNOzBizszN NUG2RXJ[PCCm NHfTVY1l\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm= NUm3Vm9COjR2OUW5NFc>
U87 R1 MoTzR4VtdCCYaXHibYxqfHliQYPzZZk> M3\rVFMxKM7:TR?= MXS0JIQ> NFm1W3ll\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm= NXvyeWFiOjR2OUW5NFc>
MGG6 M{O5emNmdGxiVnnhZoltcXS7IFHzd4F6 MVuzNEDPxE1? MlLpOEBl M2e4RYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eR?= MV6yOFQ6PTlyNx?=
MGG8 M{TTN2NmdGxiVnnhZoltcXS7IFHzd4F6 MljqN|Ah|ryP NYS5bpdvPCCm NUnJTlJS\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5 NYDxclNzOjR2OUW5NFc>
MGG23 Mn7mR4VtdCCYaXHibYxqfHliQYPzZZk> MXKzNEDPxE1? MXS0JIQ> NX32PGN{\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5 NVXGdodCOjR2OUW5NFc>
SUM149 NGDzdodE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mmf0NE0yOCEQvF2= NULkcFZJPzJiaB?= NXfPdFRNcW6qaXLpeJMh[2WubDDndo94fGhiZH;z[UBl\XCnbnTlcpRtgQ>? NX6xcXVHOjJ3NEexNFk>
Sum190 NY[2e3FCS2WubDDWbYFjcWyrdImgRZN{[Xl? M4j0dVAuOTBizszN NHPPPWs4OiCq NHm3THRqdmirYnn0d{Bk\WyuIHfyc5d1cCCmb4PlJIRmeGWwZHXueIx6 M3PUcVIzPTR5MUC5
WM35 NIfVUY5HfW6ldHnvckBCe3OjeR?= NUjmPW9oOTBidV2= NFjtbJEzPCCq MoXUSG1UVw>? NGTiNo9l\WO{ZXHz[ZMhfGinIHzleoVteyCxZjDOU3REUCCmb4fud5Rz\WGvIIThdodmfCCKRWOx M3vGNVIyQThyNEC4
WM98.1 MnPySpVv[3Srb36gRZN{[Xl? M{PT[lExKHWP MoXNNlQhcA>? NF3aRmpFVVOR NHrZ[mdl\WO{ZXHz[ZMhfGinIHzleoVteyCxZjDOU3REUCCmb4fud5Rz\WGvIIThdodmfCCKRWOx MVeyNVk5ODRyOB?=
WM115 MlrMSpVv[3Srb36gRZN{[Xl? MXqxNEB2VQ>? MYKyOEBp M{XwbWROW09? NF\FWVFl\WO{ZXHz[ZMhfGinIHzleoVteyCxZjDOU3REUCCmb4fud5Rz\WGvIIThdodmfCCKRWOx Mki2NlE6QDB2MEi=
WM3248  MonDSpVv[3Srb36gRZN{[Xl? MXmxNEB2VQ>? M4LJZ|I1KGh? MnWzSG1UVw>? NVj4PFBW\GWlcnXhd4V{KHSqZTDs[ZZmdHNib3[gUm9VS0hiZH;3cpN1emWjbTD0ZZJo\XRiSFXTNS=> MXiyNVk5ODRyOB?=
WM35 NF3xN5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGm2ZXgyOCC3TR?= Mmr4NE0yQCCm MorxSG1UVw>? MkHibY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NFPWTVEzOTl6MESwPC=>
WM98.1 NHTUbZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\tNVAhfU1? MYKwMVE5KGR? NYj3NpFbTE2VTx?= MX;pcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NFy1U28zOTl6MESwPC=>
WM115 M1vSO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXOxNEB2VQ>? M3\SVFAuOThiZB?= M2X6eWROW09? MVfpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MlfjNlE6QDB2MEi=
WM983A NEXFSlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETpUGoyOCC3TR?= M3\nSVAuOThiZB?= Mn;rSG1UVw>? M1;5[4lvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> MnnxNlE6QDB2MEi=
WM3248  NFnDT3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrxepQyOCC3TR?= M3vVPVAuOThiZB?= NFvFZW5FVVOR MXzpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 M2rvUlIyQThyNEC4

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot

PubMed: 29899322     

HeLa and Caski cells treated with RO4929097 and the DMSO control showed downregulation of the Hey1 protein as determined by Western blot analysis;

Snail / N-cadherin / Twist / E-cadherin; 

PubMed: 29899322     

Effect of inhibiting the Notch signaling pathway on the protein expression levels of EMT-associated proteins Snail, N-cadherin, Twist, and E-cadherin in HeLa and Caski cells. 

Akt / p-Akt / Notch / IGF1R / FBXW7 ; 

PubMed: 28507201     

Western blots showing expression of p-Akt, Akt, Notch, IGF1R, and FBXW7 in HCC827/ER cells treated with MK-2206 (an Akt inhibitor) or RO4929097 (a Notch inhibitor). GAPDH served as an internal control. 

NICD / Hes1 / Hes3 / Hes5; 

PubMed: 24038660     

A panel of GICs was treated with the indicated doses of DAPT, BMS-708163 and RO4929097 for 48 hours. γ Secretase inhibitors inhibited expression of NICD, Hes1, Hes3 and Hes5 in a dose-dependent manner.

29899322 28507201 24038660
Growth inhibition assay
Cell viability; 

PubMed: 30669546     

A panel of GIC lines was treated with various concentrations of the RO4929097. Cells were treated in triplicate wells for 72 h, and cell viability was assessed with the CellTiter-Blue assay. Cell viability in the vehicle control was considered to be 100%; 

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]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • Animal Models: Female nude mice bearing Calu-6 cells
  • Dosages: 3 to 60 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 93 mg/mL (198.12 mM)
Water Insoluble
Ethanol ''16 mg/mL
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
Smiles CC(C)(C(=O)NCC(C(F)(F)F)(F)F)C(=O)NC1C2=CC=CC=C2C3=CC=CC=C3NC1=O

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 ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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

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

  • * Indicates a Required Field

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:

Gamma-secretase Signaling Pathway Map

Gamma-secretase Inhibitors with Unique Features

Related Gamma-secretase Products

Tags: buy RO4929097 | RO4929097 supplier | purchase RO4929097 | RO4929097 cost | RO4929097 manufacturer | order RO4929097 | RO4929097 distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID