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Chemical Structure| 1613695-14-9 Chemical Structure| 1613695-14-9

Structure of SGC-CBP30
CAS No.: 1613695-14-9

Chemical Structure| 1613695-14-9

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SGC-CBP30 is a potent CREBBP/EP300 bromodomain inhibitor with IC50 of 21-69 and 38 nM for CREBBP and EP300 bromodomains, respectively.

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Product Details of SGC-CBP30

CAS No. :1613695-14-9
Formula : C28H33ClN4O3
M.W : 509.04
SMILES Code : C[C@H](N1CCOCC1)CN2C(CCC3=CC=C(OC)C(Cl)=C3)=NC4=CC(C5=C(C)ON=C5C)=CC=C24
MDL No. :MFCD26792586
InChI Key :GEPYBHCJBORHCE-SFHVURJKSA-N
Pubchem ID :72201027

Safety of SGC-CBP30

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

Related Pathways of SGC-CBP30

epigenetics

Isoform Comparison

Biological Activity

Target
  • p300/CBP

    CREBBP, IC50:21 nM

    EP300, IC50:38 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Myofibroblasts from Dupuytren's disease patients 2.5 µM 3 days To evaluate the effect of SGC-CBP30 on the expression of key profibrotic genes (ACTA2, COL1A1, COL3A1, TGFB1) in myofibroblasts. Results showed that SGC-CBP30 significantly inhibited the expression of these genes. Proc Natl Acad Sci U S A. 2020 Aug 25;117(34):20753-20763.
XG1LenRes cells 0.2 µM and 0.4 µM 3 days Co-treatment with SGC-CBP30 and lenalidomide significantly reduced the viability of XG1LenRes cells and downregulated IRF4 and MYC expression. Blood Cancer J. 2019 Feb 11;9(2):19.
Cardiac progenitor cells 2 mM 48 hours To explore the histone acetylation function of P300 that is responsible for modulation of gata4 transcription; CBP30 suppressed GATA4 mRNA. Genes Dis. 2018 Oct 15;6(3):318-325.
Panc1 cells 1 µM 48 hours To evaluate the effect of SGC-CBP30 on Panc1 cell growth, results showed that SGC-CBP30 alone had a marginal effect on cell growth, but its combination with JQ-1 significantly enhanced the suppression of cell growth. Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119.
MiaPaCa2 cells 1 µM 48 hours To evaluate the effect of SGC-CBP30 on MiaPaCa2 cell viability, results showed that the combination of SGC-CBP30 with JQ-1 significantly reduced cell viability. Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119.
ASPC1 cells 1 µM 48 hours To evaluate the effect of SGC-CBP30 on ASPC1 cell viability, results showed that the combination of SGC-CBP30 with JQ-1 significantly reduced cell viability. Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119.
JJN3 cells 2.5 µM and 5 µM 5 days Co-treatment with SGC-CBP30 and lenalidomide significantly reduced the viability of JJN3 cells. Blood Cancer J. 2019 Feb 11;9(2):19.
KMS11LenRes cells 0.3 µM and 1 µM 5 days Co-treatment with SGC-CBP30 and lenalidomide significantly reduced the viability of KMS11LenRes cells and downregulated IKZF1/IKZF3, IRF4, and MYC expression. Blood Cancer J. 2019 Feb 11;9(2):19.
HiBEC and NHC 10 µM Depletion of ACTA2-AS1 reduced expression of proliferative/fibrogenic markers, reduced LPS-induced cholangiocyte proliferation, and impaired organoid formation J Hepatol. 2022 Apr;76(4):921-933.
Intestinal epithelial cells (IECs) 50 mg/kg To test the hepatoprotective and enteroprotective effect of Ep300 inhibitor Cell Discov. 2023 Jul 25;9(1):77.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Murine cholangiopathy model Intraperitoneal injection 10 μg/g Three times per week for 8 weeks Confirmed the protective role of p300 inhibition in terms of DR and hepatic fibrosis J Hepatol. 2022 Apr;76(4):921-933.
Mice H1975 and H1299 cell lines Intraperitoneal injection 250 mg/kg/d Every other day for a duration of 21 days The study investigated the role of UPP1 in regulating tumor growth and sensitivity to glycolytic inhibitors in a nude mouse model. Aging Dis. 2022 Oct 1;13(5):1488-1503
Mice KPC model Intraperitoneal injection 5 mg/kg Daily for 6 months To evaluate the effect of XP-524 on survival and tumor growth in the KPC model, results showed that XP-524 significantly extended survival and reduced tumor burden and fibrosis. Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119.
Mice D-GALN/LPS-induced acute liver failure model Intraperitoneal injection 50 mg/kg One time 1 h before D/L treatment To investigate the therapeutic potential of Ep300 inhibition in intestinal and liver protection Cell Discov. 2023 Jul 25;9(1):77.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.82mL

1.96mL

0.98mL

19.64mL

3.93mL

1.96mL

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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