1. Epigenetics
  2. Epigenetic Reader Domain Histone Acetyltransferase
  3. SGC-CBP30

SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects.

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SGC-CBP30 Chemical Structure

SGC-CBP30 Chemical Structure

CAS No. : 1613695-14-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 112 In-stock
Solution
10 mM * 1 mL in DMSO USD 112 In-stock
Solid
1 mg USD 77 In-stock
5 mg USD 100 In-stock
10 mg USD 150 In-stock
50 mg USD 450 In-stock
100 mg USD 760 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 13 publication(s) in Google Scholar

Top Publications Citing Use of Products

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects[1][2][3].

IC50 & Target

CBP/p300

 

Cellular Effect
Cell Line Type Value Description References
CWR22R IC50
> 10 μM
Compound: CBP30
Antiproliferative activity against human 22Rv1 cells incubated for 5 days by CCK-8 method
Antiproliferative activity against human 22Rv1 cells incubated for 5 days by CCK-8 method
[PMID: 35569250]
HEK293 IC50
2.8 μM
Compound: 2; SGC-CBP30
Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated CBP (unknown origin) expressed in HEK293 cells after overnight incubation by BRET assay
Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated CBP (unknown origin) expressed in HEK293 cells after overnight incubation by BRET assay
[PMID: 27682507]
MCF7 IC50
2.39 μM
Compound: CBP30
Antiproliferative activity against human MCF7 cells incubated for 5 days by CCK-8 method
Antiproliferative activity against human MCF7 cells incubated for 5 days by CCK-8 method
[PMID: 35569250]
MOLM-13 IC50
1.53 μM
Compound: CBP30
Cytotoxicity against human MOLM-13 cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo luminescence assay
Cytotoxicity against human MOLM-13 cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo luminescence assay
[PMID: 33872011]
OPM-2 IC50
2.64 μM
Compound: CBP30
Antiproliferative activity against human OPM-2 cells incubated for 5 days by CCK-8 method
Antiproliferative activity against human OPM-2 cells incubated for 5 days by CCK-8 method
[PMID: 35569250]
RKO IC50
1.5 μM
Compound: 11; SGC-CBP30
Inhibition of doxorubicin-stimulated p53 (unknown origin) expressed in human RKO cells preincubated for 24 hrs followed by addition of doxorubicin for 16 hrs by luciferase reporter assay
Inhibition of doxorubicin-stimulated p53 (unknown origin) expressed in human RKO cells preincubated for 24 hrs followed by addition of doxorubicin for 16 hrs by luciferase reporter assay
[PMID: 26572217]
SCC-9 IC50
6.42 μM
Compound: CBP30
Antiproliferative activity against human SCC-9 cells incubated for 5 days by CCK-8 method
Antiproliferative activity against human SCC-9 cells incubated for 5 days by CCK-8 method
[PMID: 35569250]
In Vitro

In ankylosing spondylitis and psoriatic arthritis condition, SGC-CBP30 inhibits IL-17A secretion by Th17 cells. Transcriptional profiling of human T cells after SGC-CBP30 treatment shows a much more restricted effect on gene expression than that observed with the pan-BET (bromo and extraterminal domain protein family) bromodomain inhibitor JQ1[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SGC-CBP30 treatment slightly alleviates alveolar bronchial fibrosis induced by NSC-125066. SGC-CBP30 plus CQ-061 dramatically reduces alveolar bronchial fibrosis. The ELISA of cytokines IL-4 and IFN-γ in BALF demonstrates that combination of SGC-CBP300 and CQ-061 suppresses the activation of IL-4 as well as IFN-γ in NSC-125066 induced IPF murine models to nearly normal levels[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (SD) rats (aged 3-4 weeks) injected with NSC-125066[2]
Dosage: 25 mg/kg
Administration: Oral administration; daily; for 14 days
Result: Slightly alleviated alveolar bronchial fibrosis induced by NSC-125066.
Molecular Weight

509.04

Formula

C28H33ClN4O3

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

C[C@H](N1CCOCC1)CN2C(CCC3=CC=C(OC)C(Cl)=C3)=NC4=CC(C5=C(C)ON=C5C)=CC=C42

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 66.67 mg/mL (130.97 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9645 mL 9.8224 mL 19.6448 mL
5 mM 0.3929 mL 1.9645 mL 3.9290 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.83%

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
DMSO 1 mM 1.9645 mL 9.8224 mL 19.6448 mL 49.1121 mL
5 mM 0.3929 mL 1.9645 mL 3.9290 mL 9.8224 mL
10 mM 0.1964 mL 0.9822 mL 1.9645 mL 4.9112 mL
15 mM 0.1310 mL 0.6548 mL 1.3097 mL 3.2741 mL
20 mM 0.0982 mL 0.4911 mL 0.9822 mL 2.4556 mL
25 mM 0.0786 mL 0.3929 mL 0.7858 mL 1.9645 mL
30 mM 0.0655 mL 0.3274 mL 0.6548 mL 1.6371 mL
40 mM 0.0491 mL 0.2456 mL 0.4911 mL 1.2278 mL
50 mM 0.0393 mL 0.1964 mL 0.3929 mL 0.9822 mL
60 mM 0.0327 mL 0.1637 mL 0.3274 mL 0.8185 mL
80 mM 0.0246 mL 0.1228 mL 0.2456 mL 0.6139 mL
100 mM 0.0196 mL 0.0982 mL 0.1964 mL 0.4911 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SGC-CBP30
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