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Chemical Structure| 2682114-39-0 Chemical Structure| 2682114-39-0

Structure of RBPJ Inhibitor-1
CAS No.: 2682114-39-0

Chemical Structure| 2682114-39-0

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RIN1 is a new class of small molecule inhibitor that disrupts the interaction between NOTCH and RBPJ. It also blocked the functional interaction of RBPJ with SHARP, a scaffold protein that forms a transcriptional repressor complex with RBPJ in the absence of NOTCH signaling.

Synonyms: RIN1

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Product Details of RBPJ Inhibitor-1

CAS No. :2682114-39-0
Formula : C17H14FN3O2
M.W : 311.31
SMILES Code : FC1=CC=CC=C1OC2=C(C(N)=O)C=CC(C3=CC=NN3C)=C2
Synonyms :
RIN1
MDL No. :MFCD32856863
InChI Key :MFSSHRCJKRDIOL-UHFFFAOYSA-N
Pubchem ID :146019721

Safety of RBPJ Inhibitor-1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
C2C12 myoblasts 0.6 µM 4 days RIN1 promoted the differentiation of C2C12 myoblasts into multinucleated myofibers. PMC6658660
Jurkat cells 2 µM 8 h RIN1 suppressed the proliferation of Jurkat cells and induced gene expression changes similar to RBPJ silencing. PMC6658660
T lymphocytes 2 μM 24 h To validate the effect of Notch pathway inactivation on Th cell differentiation and apoptosis in patients with uveitis. Results showed that after RIN1 treatment, the expression of Dll4 and RBPJ was significantly reduced, the proportion of Th17/Treg, CD4+/CD8+, and apoptotic cell levels decreased, while mitochondrial membrane potential levels increased. PMC11987260
Peripheral blood CD8+ T cells 10 µM 96 h To investigate the synergistic regulation of Notch and TGF-β signaling pathways on the differentiation of DP CD8+ TRM cells. Results showed that the addition of DLL4 and TGF-β1 significantly increased CD103 expression, while the addition of RIN1 decreased CD103 expression. PMC11657194
C2C12 myoblasts 0.6 µM 4 days Promoted muscle cell differentiation into multinucleated myofibers PMC6658660
Jurkat cells 2 µM 8 h Compared transcriptomic effects of RIN1, DAPT, and CB-103, RIN1 inhibited cell proliferation PMC6658660
AD-293 cells 10 µM 17 h Primary screen for RBPJ inhibitors, RIN1 inhibited UAS-Luc activity PMC6658660

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice 786-O renal cancer cell xenograft model Intraperitoneal injection 40 mg/kg Not specified Combination of RBPJ inhibitors with CDK4/6 inhibitors showed synergistic effects on renal cancer cells. PMC8976838

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.21mL

0.64mL

0.32mL

16.06mL

3.21mL

1.61mL

32.12mL

6.42mL

3.21mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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