Cat. No.: HY-172085

SH514

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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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Pureté: 99.94%
CAS No.: 3099543-90-2
Formule: C₃₂H₃₈N₂O₄
Masse moléculaire:514.66

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SH514 Chemical Structure

CAS No.: 3099543-90-2

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Activité biologique
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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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.

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.

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_0-t	AUC_0-∞	V_z	CL	T_1/2	F
Mice	1 mg/kg	i.v.	0.08 h	174 ng/mL	81 ng·h/mL	86 ng·h/mL	20807 mL/kg	11818 mL/min/kg	1.25 h	/
Mice	10 mg/kg	p.o.	0.53 h	82 ng/mL	285 ng·h/mL	463 ng·h/mL	/	/	6.71 h	53.85 %

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.

Chemical Information

CAS No. 3099543-90-2
Appearance Solid
Masse moléculaire 514.66
Formule C₃₂H₃₈N₂O₄
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9430 mL

9.7152 mL

19.4303 mL

5 mM

0.3886 mL

1.9430 mL

3.8861 mL

10 mM

0.1943 mL

0.9715 mL

1.9430 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Zhang JZ, et al. Design, synthesis and biological evaluation of bisnoralcohol derivatives as novel IRF4 inhibitors for the treatment of multiple myeloma. Eur J Med Chem. 2025 Mar 5;285:117240. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

MCE Bioactive Compound Library

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis

Voir tous les produits spécifiques à Isoform CDK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

SH514 Related Classifications

HY-172085 Related Classifications