2. Immunology/Inflammation Cell Cycle/DNA Damage Apoptosis
  3. IFNAR DNA/RNA Synthesis c-Myc CDK
  4. SH514

SH514 is an orally active IRF4 inhibitor (IC50 = 2.63 μM). SH514 binds to the IRF4-DBD domain, thereby inhibiting the interaction of IRF4 protein with DNA (KD = 1.28 μM). SH514 can inhibit the proliferation of IRF4-high-expressing NCI-H929 and MM.1R cells, and displays no cytotoxicity for normal cells. SH514 significantly downregulates the expression of IRF4 downstream target genes concentration-dependently. SH514 inhibits the expression of cell cycle-related proteins CDC2, Cyclin B1, Cyclin D1, Cyclin E1, and CMYC in Multiple Myeloma cells. SH514 can induce DNA damage and increase the expression of γH2AX. SH514 effectively inhibits the proliferation of multiple myeloma tumors .

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SH514

SH514 Chemical Structure

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Based on 1 publication(s) in Google Scholar

SH514 Related Antibodies

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Description

SH514 is an orally active IRF4 inhibitor (IC50 = 2.63 μM). SH514 binds to the IRF4-DBD domain, thereby inhibiting the interaction of IRF4 protein with DNA (KD = 1.28 μM). SH514 can inhibit the proliferation of IRF4-high-expressing NCI-H929 and MM.1R cells, and displays no cytotoxicity for normal cells. SH514 significantly downregulates the expression of IRF4 downstream target genes concentration-dependently. SH514 inhibits the expression of cell cycle-related proteins CDC2, Cyclin B1, Cyclin D1, Cyclin E1, and CMYC in Multiple Myeloma cells. SH514 can induce DNA damage and increase the expression of γH2AX. SH514 effectively inhibits the proliferation of multiple myeloma tumors [1].

In Vitro

SH514 (Compound 41) (0-50 μM, 72 h) targets IRF4 at the cellular level, can selectively inhibit the proliferation of MM cell lines with high IRF4 expression, and displays no cytotoxicity for normal cells[1].
SH514 (100 μM, 1 h) can target IRF4 and reduce its thermal stability, while having almost no effect on the stability of IRF3, a member of the IRF family[1].
SH514 (0.125-1 μM, 24 h) significantly downregulates the expression of IRF4 downstream target genes in NCI-H929 and MM.1R cells, and the inhibitory effect was concentration-dependent in MM cells[1].
SH514 (0-0.5 μM, 24 h) leads to a significant increase in the proportion of cells in the G1 phase and a decrease in cells in the S and G2 phases in NCI-H929 cells[1].
SH514 (0.1-1 μM, 24 h) suppresses the expression of p-AKT, p-ERK, CDC2, Cyclin B1, Cyclin D1, Cyclin E1, and CMYC, and increase γH2AX in NCI-H929 cells and MM.1R cells, suggesting that SH514 could induce DNA damage[1].

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

SH514 Related Antibodies

Cell Viability Assay[1]

Cell Line: NCI-H929, MM.1R, RPMI-8226, HAF, HACAT
Concentration: 0-50 μM
Incubation Time: 72 h
Result: Demonstrated potent inhibition against IRF4-high expressing cells NCI-H929 (IC50 = 0.08 μM) and MM.1R (IC50 = 0.11 μM).
Showed weaker inhibitory effects on IRF4-low expressing cells RPMI-8226 (IC50 = 1.19 μM).
Exhibited no toxicity towards normal cells, HAF and HACAT (IC50 > 100 μM).

Real Time qPCR[1]

Cell Line: NCI-H929, MM.1R
Concentration: 0.125 μM, 0.25 μM, 0.5 μM, 1 μM
Incubation Time: 24 h
Result: Concentration-dependently downregulated the mRNA expression of IRF4 downstream target genes, including CCNC, CANX, E2F5, CMYC, HK2, and Blimp1.

Cell Cycle Analysis[1]

Cell Line: NCI-H929
Concentration: 0.125 μM, 0.25 μM, 0.5 μM
Incubation Time: 24 h
Result: Induced cell cycle arrest at the G1 phase in NCI–H929 cells in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: NCI-H929, MM.1R
Concentration: 0.1 μM, 0.3 μM, 0.5 μM, 1 μM
Incubation Time: 24 h
Result: Concentration gradients inhibited the expression of the cell cycle-related proteins CDC2, Cyclin B1, Cyclin D1, Cyclin E1, and CMYC in NCI–H929 cells and MM.1R cells.
In Vivo

SH514 (12.5-25 mg/kg, oral gavage, once daily for 34 days) can effectively inhibit the proliferation of multiple myeloma tumors in mice without causing toxic effects[1].

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

Animal Model: 1 × 107 of H929 cells were injected subcutaneously into BALB/c nude mice by mixing 1:1 with matrix gel[1].
Dosage: 12.5 mg/kg, 25 mg/kg
Administration: Oral gavage, once daily for 34 days
Result: Significantly inhibited the tumor volume in mice in a dose-dependent manner.
The body weight of mice showed an overall increasing trend, indicating that the compound had no toxic effect on mice.
Significantly reduced the expression of Ki67.
Effectively inhibited the proliferation of MM tumors in mice without causing toxic effects.
Molecular Weight

514.66

Formula

C32H38N2O4
Appearance

Solid

Color

White to off-white

SMILES

C[C@]12CC[C@@]3([H])[C@@]([H])(C(C=C4C(C)(C(C(C#N)=C[C@@]43C)=O)C)=O)[C@]1([H])CC[C@@H]2[C@@H](C(NC5=CC=C(C=C5)OC)=O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (194.30 mM; Need ultrasonic; 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 1.9430 mL 9.7152 mL 19.4303 mL
5 mM 0.3886 mL 1.9430 mL 3.8861 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Volume
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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

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.86 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
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%
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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9430 mL 9.7152 mL 19.4303 mL 48.5758 mL
5 mM 0.3886 mL 1.9430 mL 3.8861 mL 9.7152 mL
10 mM 0.1943 mL 0.9715 mL 1.9430 mL 4.8576 mL
15 mM 0.1295 mL 0.6477 mL 1.2954 mL 3.2384 mL
20 mM 0.0972 mL 0.4858 mL 0.9715 mL 2.4288 mL
25 mM 0.0777 mL 0.3886 mL 0.7772 mL 1.9430 mL
30 mM 0.0648 mL 0.3238 mL 0.6477 mL 1.6192 mL
40 mM 0.0486 mL 0.2429 mL 0.4858 mL 1.2144 mL
50 mM 0.0389 mL 0.1943 mL 0.3886 mL 0.9715 mL
60 mM 0.0324 mL 0.1619 mL 0.3238 mL 0.8096 mL
80 mM 0.0243 mL 0.1214 mL 0.2429 mL 0.6072 mL
100 mM 0.0194 mL 0.0972 mL 0.1943 mL 0.4858 mL
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SH514 Related Classifications

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.

Keywords:

SH514SH 514SH-514IFNARDNA/RNA Synthesisc-MycCDKInterferon-α/β receptorInterferon-alpha/beta receptor MycCyclin dependent kinaseIRF4Multiple MyelomaDNA DamageNCI–H929MM.1RInhibitorinhibitorinhibit

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