RBPJ Inhibitor-1
Based on 10 publication(s) in Google Scholar
RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
For research use only. We do not sell to patients.
- Purity : 99.87%
- CAS No.: 2682114-39-0
- Formula: C17H14FN3O2
- Molecular Weight:311.31
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) RBPJ Inhibitor-1
More- Cell Metab. 2024 Aug 6;36(8):1806-1822.e11. [Abstract]
- Neuro Oncol. 2025 Sep 17;27(8):2006-2022. [Abstract]
- Cell Death Dis. 2022 Apr 2;13(4):295. [Abstract]
- Oncogene. 2026 Aug;45(29):2959-2977. [Abstract]
- Arch Pharm Res. 2025 Dec;48(11-12):1382-1398. [Abstract]
- J Immunol. 2026 Jun 7;215(6):vkag074. [Abstract]
- Genomics. 2024 May;116(3):110838. [Abstract]
- Tissue Cell. 2026 Jun:100:103365. [Abstract]
- Int J Lab Hematol. 2025 Jun 12. [Abstract]
- bioRxiv. 2025 Nov 26:2025.11.23.690056. [Abstract]
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IF
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IF
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WB
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RT-PCR
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WB
Biological Activity
Description
In Vitro
RIN1 inhibits the proliferation of hematologic cancer cell lines and promoted skeletal muscle diferentiation from C2C12 myoblasts[1].
RIN1 (0.6 μM, corresponding to 3 × IC50) decreases the number of MHC+ cells and increased the number of nuclei per cell, indicating that it induces the formation of multinucleated myofbers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:AD-293 cells were transfected with RBPJ-VP16myc.
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Concentration:2 μM.
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Incubation Time:17 hours.
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Result:Inhibited Hes1-Luciferase activity with an IC50 of 0.18 µM and Emax of 82%.
Inhibited NOTCH3 ICD with similar potency and efcacy (0.19 µM and Emax=88%).
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Cell Line:T-cell acute lymphoblastic leukemia (T-ALL) patients (Jurkat and KOPT-K1) and in the mantle cell lymphoma (MCL) line REC-1.
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Concentration:0.1-10 μM.
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Incubation Time:96 h.
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Result:Inhibited NOTCH-dependent tumor cell proliferation.
Was active in both the cancer cell anti-proliferation and myoblast diferentiation assays.
Chemical Information
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CAS No. 2682114-39-0
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Appearance Solid
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Molecular Weight 311.31
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Formula C17H14FN3O2
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Color Off-white to light brown
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SMILES
O=C(N)C1=CC=C(C2=CC=NN2C)C=C1OC3=CC=CC=C3F
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Synonyms
RIN1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Cell Metab
Nicotinamide metabolism face-off between macrophages and fibroblasts manipulates the microenvironment in gastric cancer. [Abstract]2024 Aug 6;36(8):1806-1822.e11. PMID: 38897198
RBPJ Inhibitor-1 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2024 Aug 6;36(8):1806-1822.e11. [Abstract]
After RBPJ Inhibitor-1 (RIN1) (10 mM; 24 h) treatment in human fibroblast cell line HSF, the expression of NNMT and NOTCH signaling target genes (HES1 and HEY1) was detected by western blotting.
RBPJ Inhibitor-1 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2024 Aug 6;36(8):1806-1822.e11. [Abstract]
The expression of NNMT and NOTCH signaling target genes (Hes1, Hey1) in m-CAFs treated with RBPJ Inhibitor-1 (RIN1) (10 mM; 24 h) was detected by qRT-PCR.
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Neuro Oncol
SOX2 commands LIM homeobox transcription factors in choroid plexus development and tumorigenesis. [Abstract]2025 Sep 17;27(8):2006-2022. PMID: 40128799
RBPJ Inhibitor-1 purchased from MedChemExpress. Usage Cited in: Neuro Oncol. 2025 Sep 17;27(8):2006-2022. [Abstract]
RBPJ Inhibitor-1 (RIN1) (10 µM) significantly decreased SOX2 expression in NOTCH-driven CP tumor cells.
RBPJ Inhibitor-1 purchased from MedChemExpress. Usage Cited in: Neuro Oncol. 2025 Sep 17;27(8):2006-2022. [Abstract]
RBPJ Inhibitor-1 (RIN1) (10 µM) significantly decreased LMX1B expression in NOTCH-driven CPP cells.
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Cell Death Dis
The RBPJ/DAPK3/UBE3A signaling axis induces PBRM1 degradation to modulate the sensitivity of renal cell carcinoma to CDK4/6 inhibitors. [Abstract]2022 Apr 2;13(4):295. PMID: 35368029
RBPJ Inhibitor-1 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Apr 2;13(4):295. [Abstract]
RBPJ Inhibitor-1 (RIN1) (1-10 μM) decreased DAPK3 gradually in 786-O cells.
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Oncogene
Enhancing glioma immunotherapy by disrupting RBP-J-mediated NNMT signaling in tumor microenvironment. [Abstract]2026 Aug;45(29):2959-2977. PMID: 42310095 -
Arch Pharm Res
Inhibition of RBPJ transcription complex promotes IL-17 and IFN-γ secretion by CD4⁺ T cells in hepatocellular carcinoma. [Abstract]2025 Dec;48(11-12):1382-1398. PMID: 41284118 -
J Immunol
Sustained antigen-specific CD8+ T cell immunity post-mRNA booster requires notch pathway activation. [Abstract]2026 Jun 7;215(6):vkag074. PMID: 42258807 -
Genomics
Hypoxic environment promotes angiogenesis and bone bridge formation by activating Notch/RBPJ signaling pathway in HUVECs. [Abstract]2024 May;116(3):110838. PMID: 38537807 -
Tissue Cell
Overcoming osimertinib resistance in NSCLC: The role of Notch1 pathway inhibition by berberine. [Abstract]2026 Jun:100:103365. PMID: 41687187 -
Int J Lab Hematol
RBPJ/PAF1 Signaling Axis Promotes Cloning Expansion in Paroxysmal Nocturnal Hemoglobinuria Through NOTCH Signaling. [Abstract]2025 Jun 12. PMID: 40501337 -
bioRxiv
Graded Notch Signaling Functions as a Rheostat of Lineage Plasticity and Therapy Resistance in Prostate Cancer. [Abstract]2025 Nov 26:2025.11.23.690056. PMID: 41394651
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (321.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
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Somatic Cell Culture
A method of simulating the in vivo environment in vitro to maintain the cell growth, differentation and main functions.
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CFSE Dye Dilution Proliferation Assay
The CFSE (carboxyfluorescein diacetate succinimidyl ester) dye dilution proliferation assay is based on the covalent labeling of intracellular proteins by a cell-permeant fluorescent dye that becomes fluorescent upon intracellular ester cleavage and then is stably retained within cells. As labeled cells divide, the dye is partitioned equally between daughter cells, resulting in a stepwise halving of fluorescence intensity that can be quantified by flow cytometry to determine the number of cell divisions undergone by each cell population. This fluorescence dilution approach enables quantitative tracking of lymphocyte proliferation at the single-cell level over multiple rounds of division. CFSE-based proliferation analysis has been widely applied to measure antigen-driven lymphocyte expansion in vitro, where discrete fluorescence peaks correspond to successive cell divisions and allow reconstruction of proliferative history within heterogeneous populations.
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Dye-dilution cell tracking and proliferation staining
Dye-dilution cell tracking assays quantify cell proliferation by covalently labeling intracellular proteins with a stable fluorescent dye that is equally partitioned between daughter cells during mitosis, resulting in stepwise halving of fluorescence intensity with each cell division as measured by flow cytometry histograms. Carboxyfluorescein diacetate succinimidyl ester (CFSE) is a prototypical dye that diffuses into cells, is enzymatically converted into a fluorescent compound, and then covalently binds intracellular amine groups, producing long-lived fluorescence suitable for tracking multiple rounds of division in vitro and in vivo. Successive generations of dividing cells form discrete peaks of decreasing fluorescence intensity, enabling estimation of proliferation history, precursor frequency, and division index within heterogeneous populations. Alternative dyes such as CellTrace Violet (CTV) and far-red membrane dyes (e. g. , PKH26) follow the same dilution principle but differ
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CCK-8/WST-8 Cell Proliferation Assay
The CCK-8/WST-8 assay is based on the reduction of the water-soluble tetrazolium salt WST-8 to a water-soluble formazan product by cellular dehydrogenases in metabolically active cells, where the generated formazan amount is proportional to the number of living cells and is quantified by measuring absorbance in the visible range, providing a colorimetric readout for cell viability and proliferation assessment. This class of tetrazolium-based assays improves upon earlier MTT-based systems by producing a water-soluble formazan, eliminating the need for organic solubilization steps and enabling direct spectrophotometric measurement in culture medium.
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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
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Cell Counting-Based Growth Curve Assay
Cell counting-based growth curve assays quantify cell proliferation by directly measuring changes in viable cell number over time using manual or automated counting methods such as hemocytometer-based counting or instrument-assisted cell enumeration, enabling construction of growth curves that reflect population expansion dynamics in response to culture conditions. A widely used approach is trypan blue exclusion with hemocytometer counting, where membrane-compromised (non-viable) cells take up the dye, allowing discrimination between viable and non-viable cells while simultaneously enabling total cell number quantification. Repeated sampling across time points allows estimation of proliferation rate, growth phases, and comparative growth kinetics between experimental conditions.
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Colony Formation (Clonogenic) Assay
The clonogenic (colony formation) assay measures the ability of a single cell to retain reproductive viability and form a macroscopic colony, typically defined as a cluster derived from one progenitor cell after a defined growth period. This assay is widely used to evaluate cell survival after exposure to ionizing radiation or cytotoxic treatments and is considered a standard method in radiation biology for generating dose-response relationships of reproductive cell death. Colony formation reflects long-term proliferative capacity rather than short-term metabolic activity, and survival is quantified by comparing treated versus untreated conditions based on colony number and derived survival fractions.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
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EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
The EdU incorporation assay measures DNA synthesis by adding the thymidine analog 5-ethynyl-2′-deoxyuridine to cells or tissues, where it is incorporated into newly synthesized DNA during S phase. Incorporated EdU is detected by copper-catalyzed azide-alkyne cycloaddition, in which a fluorescent azide covalently reacts with the ethynyl group on EdU, allowing S-phase cells to be detected by fluorescence microscopy, flow cytometry, or high-content imaging. EdU detection does not require DNA denaturation or anti-BrdU antibody access, which preserves sample structure and improves compatibility with immunostaining and multiparameter cytometry compared with BrdU-based detection. EdU can be cytotoxic in a cell-type- and exposure-dependent manner, so pulse duration, concentration, and continuous-labeling designs should be validated for each cell type.
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Ki-67 Immunostaining Proliferation Assay
Ki-67 immunostaining measures the growth fraction of a cell population by detecting Ki-67, a nuclear antigen present in proliferating cells and absent in quiescent G0 cells. The readout is the percentage of Ki-67-positive nuclei among total counted cells, commonly called the Ki-67 labeling index or proliferation index.
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PCNA Immunodetection Proliferation Assay
PCNA immunodetection measures proliferative activity by detecting proliferating cell nuclear antigen, a nuclear protein associated with DNA polymerase δ function and DNA replication. The assay readout is the proportion of PCNA-positive nuclei among total counted cells, but PCNA labeling is not identical to BrdU labeling because PCNA can mark late G1/early S-associated replication competence and may persist beyond active DNA synthesis depending on fixation and extraction conditions.
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Protocol for Cell Counting and Cell Density Analysis
Cell counting and cell-density analysis estimate the number of cells in a known volume or field area. Manual hemocytometer counting uses a chamber of defined geometry to convert counted cells into cells/mL, while automated counters and image-analysis workflows detect cell objects from optical, brightfield, fluorescence, impedance, or digital-image features. Trypan blue viability counting is based on dye exclusion: viable cells with intact membranes exclude dye, while non-viable cells with compromised membranes stain blue. The readout is total cell density, viable-cell density, dead-cell density, and percent viability. Cell density can also be estimated from microscopy images by counting objects per image area, from flow cytometry using calibrated volume or reference particles, or from in situ microscopy in bioreactors after calibration against reference methods such as hemocytometer or flow cytometry.
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Notch Pathway Solutions
The Notch pathway is a contact-dependent signaling pathway that controls cell-fate decisions, differentiation, proliferation, and tissue patterning through interactions between membrane-bound Notch receptors and membrane-bound ligands on neighboring cells. Canonical Notch signaling is activated when ligand engagement triggers proteolytic release of the Notch intracellular domain, which enters the nucleus and regulates transcription together with DNA-binding transcriptional complexes. In the canonical mechanism, ligand-dependent Notch activation leads to release of the intracellular Notch domain, and presenilin-dependent γ-secretase activity is required for production of the active intracellular signaling fragment. The released intracellular domain functions as a nuclear signal that converts Notch receptor activation at the membrane into transcriptional regulation of target programs such as HES/HEY-family genes and other context-dependent downstream targets. The literature links Notch p
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MTT Cell Proliferation Assay
The MTT assay is a colorimetric endpoint assay for estimating viable cell number, cell growth, cytotoxicity, or cell activation in cultured mammalian cells. Living cells reduce the yellow tetrazolium salt MTT into purple/blue formazan, while dead cells do not generate the same signal; the resulting color can be quantified with a multiwell spectrophotometer. MTT reduction is commonly interpreted as a readout of metabolic activity that often correlates with viable cell number, but it should not be treated as a direct cell-counting method unless the assay is optimized for the cell type and experimental condition. Studies show that MTT reduction can involve mitochondrial and non-mitochondrial reducing systems, and formazan may accumulate in intracellular lipid droplets rather than simply marking mitochondria.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.2122 mL | 16.0612 mL | 32.1223 mL | 80.3058 mL |
| 5 mM | 0.6424 mL | 3.2122 mL | 6.4245 mL | 16.0612 mL | |
| 10 mM | 0.3212 mL | 1.6061 mL | 3.2122 mL | 8.0306 mL | |
| 15 mM | 0.2141 mL | 1.0707 mL | 2.1415 mL | 5.3537 mL | |
| 20 mM | 0.1606 mL | 0.8031 mL | 1.6061 mL | 4.0153 mL | |
| 25 mM | 0.1285 mL | 0.6424 mL | 1.2849 mL | 3.2122 mL | |
| 30 mM | 0.1071 mL | 0.5354 mL | 1.0707 mL | 2.6769 mL | |
| 40 mM | 0.0803 mL | 0.4015 mL | 0.8031 mL | 2.0076 mL | |
| 50 mM | 0.0642 mL | 0.3212 mL | 0.6424 mL | 1.6061 mL | |
| 60 mM | 0.0535 mL | 0.2677 mL | 0.5354 mL | 1.3384 mL | |
| 80 mM | 0.0402 mL | 0.2008 mL | 0.4015 mL | 1.0038 mL | |
| 100 mM | 0.0321 mL | 0.1606 mL | 0.3212 mL | 0.8031 mL |