Home Tools

H-151

Catalog No. T5674 CAS 941987-60-6

H-151 is a highly potent and selective STING antagonist. H-151 covalently binds to Cys91 of STING and inhibits palmitoylation of Cys91, thereby inhibiting STING activity. H-151 can be used in the study of autoinflammatory diseases in vivo and ex vivo.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

H-151, CAS 941987-60-6

Pack Size	Availability	Price/USD
2 mg	In stock	$ 32.00
5 mg	In stock	$ 47.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 148.00
50 mg	In stock	$ 296.00
100 mg	In stock	$ 452.00
500 mg	In stock	$ 987.00
1 g	In stock	$ 1,330.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

Bulk Inquiry

Select Batch

Purity: 99.52%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	H-151 is a highly potent and selective STING antagonist. H-151 covalently binds to Cys91 of STING and inhibits palmitoylation of Cys91, thereby inhibiting STING activity. H-151 can be used in the study of autoinflammatory diseases in vivo and ex vivo.
In vitro	METHODS: Mouse monocyte macrophage RAW264.7 was treated with H-151 (0.25-2 μM) for 1 h, and then stimulated with rmCIRP (1 μg/mL) for 24 h. The level of IFN-β was measured by ELISA. RESULTS: IFN-β was dose-dependently reduced in the culture supernatant of cells pretreated with H-151, which inhibited eCIRP-induced activation of STING in vitro. [1] METHODS: Human monocytes THP-1 were treated with H-151 (0.5 μM) for 2 h, and the expression levels of target proteins were measured by Western Blot. RESULTS: H-151 inhibited the phosphorylation of TBK1, and H-151 effectively inhibited the activation of hsSTING. [2]
In vivo	METHODS: To assay in vivo activity, H-151 (750 nmol, 200 μL) was administered intraperitoneally to Trex1-/- Ifnb1Δβ-luc/Δβ-luc reporter mice once daily for seven days. RESULTS: When administered for one week, H-151 showed significant efficacy in Trex1-/- mice expressing a bioluminescent IFNβ reporter gene. [2] METHODS: To test the role in cisplatin-induced acute kidney injury (AKI), H-151 (7 mg/kg) was administered intraperitoneally to C57BL/6J mice with cisplatin-induced AKI three times a day. RESULTS: H-151 treatment significantly ameliorated cisplatin-induced renal injury, as evidenced by improvement in renal function, renal morphology, and renal inflammation.H-151 may be a potential therapeutic agent for the treatment of AKI, possibly by inhibiting STING-mediated inflammation and mitochondrial damage. [3]

Molecular Weight	279.34
Formula	C17H17N3O
CAS No.	941987-60-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (447.48 mM), Sonification is recommended.

References and Literature

1. Kobritz M, et al. H151, A SMALL MOLECULE INHIBITOR OF STING AS A NOVEL THERAPEUTIC IN INTESTINAL ISCHEMIA-REPERFUSION INJURY. Shock. 2022 Sep 1;58(3):241-250. 2. Haag SM, et al. Targeting STING with covalent small-molecule inhibitors. Nature. 2018 Jul;559(7713):269-273. 3. Gong W, et al. The novel STING antagonist H151 ameliorates cisplatin-induced acute kidney injury and mitochondrial dysfunction. Am J Physiol Renal Physiol. 2021 Apr 1;320(4):F608-F616.

Citations

1. Song P, Yang W, Lou K F, et al. UNC13D inhibits STING signaling by attenuating its oligomerization on the endoplasmic reticulum. EMBO reports. 2022: e55099 2. Chen Q, Tang L, Zhang Y, et al. STING up-regulates VEGF expression in oxidative stress-induced senescence of retinal pigment epithelium via NF-κB/HIF-1α pathway. Life Sciences. 2022: 120089. 3. Qiao W, Hu C, Ma J, et al.Low-dose metronomic chemotherapy triggers oxidized mtDNA sensing inside tumor cells to potentiate CD8+ T anti-tumor immunity.Cancer Letters.2023: 216370. 4. Li J, Sun Y, Zhao X, et al.Radiation induces IRAK1 expression to promote radioresistance by suppressing autophagic cell death via decreasing the ubiquitination of PRDX1 in glioma cells.Cell Death & Disease.2023, 14(4): 1-16. 5. Qiao W, Chen J, Zhou H, et al.A Single‐Atom Manganese Nanozyme Mn‐N/C Promotes Anti‐Tumor Immune Response via Eliciting Type I Interferon Signaling.Advanced Science.2024: 2305979.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Covalent Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Immuno-Oncology Compound Library Immunology/Inflammation Compound Library NO PAINS Compound Library Nonsteroidal Anti-Inflammatory Compound Library

Related Products

Related compounds with same targets

Anti-inflammatory agent 65 Cridanimod CCCP STING activator Compound 53 Vadimezan diABZI STING agonist-1 (Tautomerism) C-178 SN-001

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

H-151 941987-60-6 Immunology/Inflammation STING ERIS phosphorylation Stimulator of Interferon Genes palmitoylatio TMEM173 MPYS H 151 inhibit autoinflammatory TBK1 H151 Inhibitor MITA inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.