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Chemical Structure| 941987-60-6 Chemical Structure| 941987-60-6

Structure of H-151
CAS No.: 941987-60-6

Chemical Structure| 941987-60-6

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1-(4-Ethylphenyl)-3-(1H-indol-3-yl)urea, also known as H-151, is a irreversible inhibitor of STING that can inhibit the type I interferon (IFN) response and reduce the phosphorylation of TBK1 and palmitoylation of human STING in vitro.

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Product Details of H-151

CAS No. :941987-60-6
Formula : C17H17N3O
M.W : 279.34
SMILES Code : O=C(NC1=CNC2=C1C=CC=C2)NC3=CC=C(CC)C=C3
MDL No. :MFCD08026581
InChI Key :UJZDIKVQFMCLBE-UHFFFAOYSA-N
Pubchem ID :7616033

Safety of H-151

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
HMEC-1 cells 90 μM 1 hour H-151 downregulated the expression levels of adhesion molecules and chemokines in HMEC-1 cells, and reduced the adhesive ability and chemotaxis of iμMunocytes PMC9343420
THP-1 cells 2.5 µM 11 hours H-151 markedly reduced baseline STAT1 phosphorylation and type I IFN-mediated gene transcription, indicating a possible targeted treatment for COPA syndrome patients. PMC9051092
HeLa cells 2.5 µM 11 hours H-151 markedly reduced baseline STAT1 phosphorylation and type I IFN-mediated gene transcription, indicating a possible targeted treatment for COPA syndrome patients. PMC9051092
U251 cells 1 μM 48 hours H-151 significantly decreased IR-induced IRAK1 expression, indicating that the STING signaling pathway is involved in IR-induced IRAK1 expression. PMC10082800
A172 cells 1 μM 48 hours H-151 significantly decreased IR-induced IRAK1 expression, indicating that the STING signaling pathway is involved in IR-induced IRAK1 expression. PMC10082800
OCI-LY1 cells 4 µM 36 hours Inhibit STING activity, reduce BR therapy-induced cell death PMC11551994
SU-DHL2 cells 4 µM 36 hours Inhibit STING activity, reduce BR therapy-induced cell death PMC11551994
OCI-LY1 200 µM 1.5 days To evaluate the direct cytotoxic effect of Bendamustine on DLBCL cells, results showed that Bendamustine significantly reduced cell viability. PMC11551994
SU-DHL2 200 µM 1.5 days To evaluate the direct cytotoxic effect of Bendamustine on DLBCL cells, results showed that Bendamustine significantly reduced cell viability. PMC11551994
KARPAS-422 200 µM 1.5 days To evaluate the direct cytotoxic effect of Bendamustine on DLBCL cells, results showed that Bendamustine significantly reduced cell viability. PMC11551994

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Neonatal anesthesia model Intraperitoneal injection 25 mg/kg single injection, lasting 24 hours To evaluate the effect of neonatal anesthesia on rapid eye movement sleep in adolescent rats. Results showed that anesthetized rats exhibited a significant increase in rapid eye movement sleep time during adolescence. PMC6520183
C57BL/6 mice Diabetic myocardial ischemia-reperfusion injury model Intraperitoneal injection 2 mg/kg Every 4 days for 3 times H-151 significantly ameliorated myocardial injury induced by MFN2 knockdown in both the cell and mouse models, reduced inflammation, and improved cardiac function. PMC10398939

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.58mL

0.72mL

0.36mL

17.90mL

3.58mL

1.79mL

35.80mL

7.16mL

3.58mL

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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