Sulfasalazine (Synonyms: NSC 667219)

Name: Sulfasalazine
Brand: MedChemExpress
SKU: HY-14655
Rating: 5.0 (40 reviews)

Cat. No.: HY-14655 Purity: 98.75%: FAQs
Data Sheet SDS COA Handling Instructions

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Sulfasalazine (NSC 667219) is an anti-rheumatic agent for the research of rheumatoid arthritis and ulcerative colitis. Sulfasalazine can suppress NF-κB activity. Sulfasalazine is a type 1 ferroptosis inducer.

For research use only. We do not sell to patients.

Sulfasalazine Chemical Structure

CAS No. : 599-79-1

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10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
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500 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
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Based on 40 publication(s) in Google Scholar

Other Forms of Sulfasalazine:

38 Publications Citing Use of MCE Sulfasalazine

: Sulfasalazine purchased from MedChemExpress. Usage Cited in: Mol Ther. 2021 Mar 17;S1525-0016(21)00142-8. [Abstract]; PD-L1 expression is significantly increased after Sulfasalazine (SAS) treatment at both the protein and mRNA levels.

: Sulfasalazine purchased from MedChemExpress. Usage Cited in: Cell Res. 2018 Dec;28(12):1171-1185. [Abstract]; Melanoma A375 cells are treated with SSZ (Sulfasalazine, 125 μM) with or without FeSO₄ (100 μM) for 6 h to detect the ROS level or 24 h to assess the pyroptotic features (including morphology, GSDME cleavage, and LDH release), unless specifically defined.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

RelA

Autophagy

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.56 μM Compound: Sulfasalazine	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	12 μM Compound: Sulfasalazine	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	3 μM Compound: Sulfasalazine	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
HepG2	IC₅₀	0.9 μM Compound: SFZ	Inhibition of TNF-alpha-induced NFkappaB activation in human HepG2 cells after 1 hr by luciferase reporter assay Inhibition of TNF-alpha-induced NFkappaB activation in human HepG2 cells after 1 hr by luciferase reporter assay	[PMID: 21870831]
HepG2	IC₅₀	0.9 μM Compound: Sulfasalazine	Inhibition of TNF-alpha-induced NF-kappaB transcriptional activation in human HepG2 cells preincubated for 1 hr followed by TNF-alpha challenge measured after 1 hr by luciferase reporter gene assay Inhibition of TNF-alpha-induced NF-kappaB transcriptional activation in human HepG2 cells preincubated for 1 hr followed by TNF-alpha challenge measured after 1 hr by luciferase reporter gene assay	[PMID: 24314396]
HepG2	IC₅₀	0.9 μM Compound: SFZ	Inhibition of NF-kappaB expressed in human HepG2 cells assessed as inhibition of TNFalpha-induced luciferase activity preincubated for 1 hr followed by TNFalpha challenge measured after 1 hr by reporter gene assay Inhibition of NF-kappaB expressed in human HepG2 cells assessed as inhibition of TNFalpha-induced luciferase activity preincubated for 1 hr followed by TNFalpha challenge measured after 1 hr by reporter gene assay	[PMID: 23031596]
HepG2	IC₅₀	0.9 μM Compound: Sulfasalazine	Inhibition of TNFalpha-induced NFkappaB transcriptional activity in human HepG2 cells pretreated for 1 hr before TNFalpha challenge by luciferase reporter gene analysis Inhibition of TNFalpha-induced NFkappaB transcriptional activity in human HepG2 cells pretreated for 1 hr before TNFalpha challenge by luciferase reporter gene analysis	[PMID: 22381047]
HepG2	IC₅₀	0.9 μM Compound: Sulfasalazine	Inhibition of NF-kappaB activation expressed in TNFalpha-stimulated human HepG2 cells co-transfected with PPRE-Luc plasmid pretreated for 1 hr before TNFalpha challenge measured after 24 hrs by luciferase reporter gene assay Inhibition of NF-kappaB activation expressed in TNFalpha-stimulated human HepG2 cells co-transfected with PPRE-Luc plasmid pretreated for 1 hr before TNFalpha challenge measured after 24 hrs by luciferase reporter gene assay	[PMID: 21889336]
T-cell	IC₅₀	> 10 μM Compound: Salazosulfapyridine	Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells	[PMID: 11229767]
U2OS	IC₅₀	9.6 μM Compound: Sulfasalazine	Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method	[PMID: 31439379]
U-87MG ATCC	IC₅₀	30 μM Compound: 2	Inhibition of xc-cystine-glutamate antiporter-mediated cystine uptake in human U87 cells using L-[14C]cystine as substrate after 15 mins by liquid scintillation counting Inhibition of xc-cystine-glutamate antiporter-mediated cystine uptake in human U87 cells using L-[14C]cystine as substrate after 15 mins by liquid scintillation counting	[PMID: 21889337]

In Vitro

Treatment of SW620 colon cells with sulfasalazine inhibits TNFα-, LPS-, or phorbol ester-induced NFκB activation. NFκB-dependent transcription is inhibited by sulfasalazine at micro- to millimolar concentrations. TNFα-induced nuclear translocation of NFκB is prevented by sulfasalazine through inhibition of IκBα degradation^[1]. Pre-incubation with 5 mM of sulfasalazine alone significantly increases basal mRNA expression of all pro-inflammatory cytokines with levels of IL-6 mRNA increased by 80-fold compared with vehicle control^[2]. Once digested, sulfasalazine is cleaved into sulfapyridine and 5-aminosalicylic acid by colonic bacteria, and the latter, too, is reported to suppress NF-kappaB activity^[3].

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

In Vivo

At low doses (0.25 mM), SAS is able to suppress glioma growth by over 60% compared to untreated controls^[3].

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

Clinical Trial

Molecular Weight

398.39

Formula

C₁₈H₁₄N₄O₅S

CAS No.

599-79-1

Appearance

Solid

Color

Light yellow to orange

SMILES

OC(C1=C(O)C=CC(/N=N/C2=CC=C(S(=O)(NC3=NC=CC=C3)=O)C=C2)=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

NH4OH : 150 mg/mL (376.52 mM; ultrasonic and adjust pH to 9 with NH4OH)

1 M NaOH : ≥ 100 mg/mL (251.01 mM)

DMSO : 80 mg/mL (200.81 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5101 mL	12.5505 mL	25.1010 mL
5 mM	0.5020 mL	2.5101 mL	5.0202 mL
10 mM	0.2510 mL	1.2551 mL	2.5101 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (6.28 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.28 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 10 mg/mL (25.10 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.04%

Select Batch:

Data Sheet (279 KB) SDS (419 KB)

COA (249 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[1]. Wahl C, et al. Sulfasalazine: a potent and specific inhibitor of nuclear factor kappa B. J Clin Invest. 1998 Mar 1;101(5):1163-74. [Content Brief]

[2]. Sykes L, et al. Sulfasalazine augments a pro-inflammatory response in interleukin-1β-stimulated amniocytes and myocytes. Immunology. 2015 Dec;146(4):630-44. [Content Brief]

[3]. Chung WJ, et al. Sulfasalazine inhibits the growth of primary brain tumors independent of nuclear factor-kappaB. J Neurochem. 2009 Jul;110(1):182-93. [Content Brief]

[4]. Mao C, et al. DHODH-mediated ferroptosis defence is a targetable vulnerability in cancer. Nature. 2021;593(7860):586-590. [Content Brief]

Kinase Assay	MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Sulfasalazine is dissolved in culture medium. SW620 cells are grown in Dulbecco’s modified Eagle medium, supplemented with 10% heat-inactivated FCS, 2 mmol/liter glutamine, and 1% (wt/vol) penicillin/streptomycin. SW620 cells are transfected with the 3xIgkBLuc reporter construct. After 18 h, cells are incubated with either medium alone or with sulfasalazine (0.1, 0.2, 0.5, 1, 2, 5 mM) before stimulation with TNFα, LPS, or PMA. Luciferase assay is performed^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice: Sulfasalazine is dissolved in 0.1 M NaOH, and then neutralized by titrating with 0.1 M HCl. U-87MG glioma cells are implanted into the cranium of a SCID mouse. After 7 days, animals are randomized into three groups of five animals each. One group receives 1 mL i.p. saline injections twice daily for 3 weeks. The two test groups receives 8 mg of sulfasalazine in 1 mL saline twice daily for 3 weeks. Tumor growth and animal health were monitored. After perfusion with 4% paraformaldehyde, mouse brains were collected, rinsed, and placed in 30% sucrose^[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Wahl C, et al. Sulfasalazine: a potent and specific inhibitor of nuclear factor kappa B. J Clin Invest. 1998 Mar 1;101(5):1163-74. [Content Brief] [2]. Sykes L, et al. Sulfasalazine augments a pro-inflammatory response in interleukin-1β-stimulated amniocytes and myocytes. Immunology. 2015 Dec;146(4):630-44. [Content Brief] [3]. Chung WJ, et al. Sulfasalazine inhibits the growth of primary brain tumors independent of nuclear factor-kappaB. J Neurochem. 2009 Jul;110(1):182-93. [Content Brief] [4]. Mao C, et al. DHODH-mediated ferroptosis defence is a targetable vulnerability in cancer. Nature. 2021;593(7860):586-590. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / 1 M NaOH / NH4OH	1 mM	2.5101 mL	12.5505 mL	25.1010 mL	62.7526 mL
	5 mM	0.5020 mL	2.5101 mL	5.0202 mL	12.5505 mL
	10 mM	0.2510 mL	1.2551 mL	2.5101 mL	6.2753 mL
	15 mM	0.1673 mL	0.8367 mL	1.6734 mL	4.1835 mL
	20 mM	0.1255 mL	0.6275 mL	1.2551 mL	3.1376 mL
	25 mM	0.1004 mL	0.5020 mL	1.0040 mL	2.5101 mL
	30 mM	0.0837 mL	0.4184 mL	0.8367 mL	2.0918 mL
	40 mM	0.0628 mL	0.3138 mL	0.6275 mL	1.5688 mL
	50 mM	0.0502 mL	0.2510 mL	0.5020 mL	1.2551 mL
	60 mM	0.0418 mL	0.2092 mL	0.4184 mL	1.0459 mL
	80 mM	0.0314 mL	0.1569 mL	0.3138 mL	0.7844 mL
	100 mM	0.0251 mL	0.1255 mL	0.2510 mL	0.6275 mL

Sulfasalazine 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:

Sulfasalazine599-79-1NSC 667219NSC667219NSC-667219NF-κBAutophagyApoptosisFerroptosisBacterialAntibioticNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

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Sulfasalazine (Synonyms: NSC 667219)

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Other Forms of Sulfasalazine:

Sulfasalazine Related Antibodies

38 Publications Citing Use of MCE Sulfasalazine

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Sulfasalazine Related Antibodies

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Complete Stock Solution Preparation Table

Sulfasalazine Related Classifications

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