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Chemical Structure| 48208-26-0 Chemical Structure| 48208-26-0

Structure of RG108
CAS No.: 48208-26-0

Chemical Structure| 48208-26-0

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RG108 is a DNA methyltransferase inhibitor with IC50 of 115 nM.

Synonyms: N-Phthalyl-L-tryptophan

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Product Details of RG108

CAS No. :48208-26-0
Formula : C19H14N2O4
M.W : 334.33
SMILES Code : O=C(O)[C@H](CC1=CNC2=CC=CC=C12)N3C(C4=CC=CC=C4C3=O)=O
Synonyms :
N-Phthalyl-L-tryptophan
MDL No. :MFCD08705332
InChI Key :HPTXLHAHLXOAKV-INIZCTEOSA-N
Pubchem ID :702558

Safety of RG108

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H317
Precautionary Statements:P280

Related Pathways of RG108

epigenetics

Isoform Comparison

Biological Activity

Target
  • DNA Methyltransferase

    DNA methyltransferase, IC50:115 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HL-60 cells 50 µM 48 hours RG108, at a non-toxic dose, enhanced the maturation and differentiation of HL-60 cells into granulocytes when combined with all-trans retinoic acid (RA), and significantly accelerated cell maturation when used in combination with HDAC inhibitors (such as sodium phenyl butyrate or BML-210). PMC6275587

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice cisplatin-induced hearing loss model Intraperitoneal injection 10 mg/kg single dose administration RG108 protects against cisplatin-induced hearing loss. PMC9069410
Mice Transient middle cerebral artery occlusion model (tMCAO) Tail vein injection 10 mg/kg Once daily for 3 days, and once again at the onset of reperfusion RG108 significantly increased infarct volume and exacerbated neurobehavioral deficits. RG108 also promoted neutrophil proliferation in the blood and infiltration into the ischemic brain hemisphere, leading to exacerbated inflammation. PMC11246610
Rat Spontaneously hypertensive rats (SHR) Microinjection into PVN 25 μg Five consecutive days, once daily RG108 increased Agtr1a and Slc12a2 mRNA levels and elevated blood pressure by inhibiting DNMT activity in the PVN. PMC10830874
C57BL/6J mice noise-induced hearing loss model Intraperitoneal injection 1 mg/kg or 10 mg/kg single dose, lasting 2 hours Evaluate the protective effect of RG108 on noise-induced hearing loss, results showed that RG108 significantly attenuated noise-induced ABR threshold elevation and hair cell loss. PMC8490244

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.99mL

0.60mL

0.30mL

14.96mL

2.99mL

1.50mL

29.91mL

5.98mL

2.99mL

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
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. 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

References

 

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