Name: H-151
Brand: GlpBio
SKU: GC34610
Availability: InStock
Rating: 5 (10 reviews)

GlpBio Products Cited In Reputable Papers

Nature
610.7931 (2022): 366-372

Nature
618, 1017–1023 (2023)

Cell
183.7 (2020): 1867-1883

Cell Research
31, 1291–1307 (2021)

Cell Research
33, 273–287 (2023)

Cell Research
33, 546–561 (2023)

Molecular Cancer
21.1 (2022): 1-17

Molecular Cancer
21.1 (2022): 1-18

Cancer Cell
39 (2021): 1-16

Cell Host Microbe
30.8 (2022): 1124-1138

Cell Host Microbe
31.5 (2023): 766-780

Cell Host Microbe
31.3 (2023): 418-43

Cell Metabolism
34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
20, 264–276 (2023)

Adv Funct Mater
33.35 (2023): 2214998

Product Documents

Quality Control & SDS

View current batch:

Purity: >99.50%

Protocol

Cell experiment [1]:
Cell lines	THP-1 cells
Preparation Method	Cells were pretreated with H-151 (1 µM) for 6 h, followed by stimulating with 2 ,3 -cGAMP (cGAMP, 10 µg/ml) for 12 h
Reaction Conditions	1 µM; 6 h
Applications	H-151 inhibited the induction of IFN-β mRNA expression triggered by cGAMP in THP-1 cells.
Animal experiment [2]:
Animal models	Female BALB/c mice (model of psoriasis induced by imiquimod)
Preparation Method	Mice were randomly divided into four groups (n = 8): control, model, model with 250 mg/kg H-151 (2.5% H-151 cream) and model with 500 mg/kg H-151 (5% H-151 cream) groups. A topical dose of 62.5 mg of 5% imiquimod cream was applied, once daily, to the shaved back and right ear in a ratio of 4:1 for five consecutive days to induce psoriasis-like skin inflammation. Control group was only treated with control cream (a mixture of wood fat and Vaseline in the ratio of one to one) on the shaved back and right ear in a ratio of 4:1 twice daily, 0.2 g per mice per treatment. The model group was treated with the control cream and imiquimod cream on the shaved back and right ear in a ratio of 4:1. Treatment groups were treated with H-151 creams (2.5% or 5% H-151 creams containing the same components as control cream) and imiquimod cream on the shaved back and right ear in a ratio of 4:1. Before imiquimod administration, the shaved back and right ear were topically treated with control cream or H-151 creams (250 or 500 mg/kg) in a ratio of 4:1, 0.2 g per mice. After imiquimod administration, another treatment with control cream or H-151 creams (250 or 500 mg/kg) was applied in the same manner mentioned above. The interval between all the treatments was 4 h. The body weight was measured every day.
Dosage form	250 /500 mg/kg; on the shaved back and right ear;5days
Applications	H-151 ameliorates IMQ(imiquimod)-induced psoriasis-like dermatitis.
References: [1]. Pan Y, You Y, et,al. The STING antagonist H-151 ameliorates psoriasis via suppression of STING/NF-κB-mediated inflammation. Br J Pharmacol. 2021 Dec;178(24):4907-4922. doi: 10.1111/bph.15673. Epub 2021 Oct 30. PMID: 34460100.

H-151 is a low MW antagonist of STING, which blocks the activation-induced palmitoylation of STING, and exhibits significant inhibitory effects on STING signalling H-151 can be used in the study of autoinflammatory diseases[1-2].

H-151(1 µM; 6 h) exerts anti-psoriasis effect through inhibiting STING/NF-κB signalling[3]. H-151(2.5 µM; 24h) improved the inflammation of peripheral blood mononuclear cells and Coatomer complex I (COPI)-deficient cell lines in patients with COPA syndrome[4].

H-151(250 /500 mg/kg; on the shaved back and right ear;5days) displayed anti-inflammatory activity in both keratinocytes and immune cells, and decreased the severity of psoriatic response in vivo[3]. H-151 downregulated the expression of granzymes and the pro-inflammatory cytokines IL-1β, IL-6, IL-15, IL-23A, and IFN-γ, and induced a pro-resolution macrophage phenotypes in ALS patients [5]. Administration of H-151 alleviated pulmonary edema, hemorrhage, thickening of the alveolar septum and infiltration of inflammatory cells; DNA damage in pulmonary tissue; and disruption of intercellular junctions in LPS-induced ALI [6]. H-151(750 nmol; i.p) treatment preserves myocardial function 28 days after myocardial infarction (MI)[7].

References:
[1]. Haag SM, Gulen MF, et,al. Targeting STING with covalent small-molecule inhibitors. Nature. 2018 Jul;559(7713):269-273. doi: 10.1038/s41586-018-0287-8. Epub 2018 Jul 4. PMID: 29973723.
[2]. Li J, Lu Y, et,al. Blocking cGAS/STING signaling protects against sepsis-associated acute liver injury. Int Immunopharmacol. 2022 Dec;113(Pt A):109276. doi: 10.1016/j.intimp.2022.109276. Epub 2022 Oct 15. PMID: 36252490.
[3]. Pan Y, You Y, et,al. The STING antagonist H-151 ameliorates psoriasis via suppression of STING/NF-κB-mediated inflammation. Br J Pharmacol. 2021 Dec;178(24):4907-4922. doi: 10.1111/bph.15673. Epub 2021 Oct 30. PMID: 34460100.
[4]. Steiner A, Hrovat-Schaale K, et,al. Deficiency in coatomer complex I causes aberrant activation of STING signalling. Nat Commun. 2022 Apr 28;13(1):2321. doi: 10.1038/s41467-022-29946-6. PMID: 35484149; PMCID: PMC9051092.
[5]. Zamiri K, Kesari S, et,al. Therapy of autoimmune inflammation in sporadic amyotrophic lateral sclerosis: Dimethyl fumarate and H-151 downregulate inflammatory cytokines in the cGAS-STING pathway. FASEB J. 2023 Aug;37(8):e23068. doi: 10.1096/fj.202300573R. PMID: 37436778; PMCID: PMC10619685.
[6]. Zhao J, Zhen N, et,al. NETs Promote Inflammatory Injury by Activating cGAS-STING Pathway in Acute Lung Injury. Int J Mol Sci. 2023 Mar 7;24(6):5125. doi: 10.3390/ijms24065125. PMID: 36982193; PMCID: PMC10049640.
[7]. Hu S, Gao Y, et,al. The selective STING inhibitor H-151 preserves myocardial function and ameliorates cardiac fibrosis in murine myocardial infarction. Int Immunopharmacol. 2022 Jun;107:108658. doi: 10.1016/j.intimp.2022.108658. Epub 2022 Mar 9. PMID: 35278833.

Cas No.	941987-60-6	SDF
Canonical SMILES	O=C(NC1=CNC2=C1C=CC=C2)NC3=CC=C(CC)C=C3
Formula	C₁₇H₁₇N₃O	M.Wt	279.34
Solubility	DMSO : 125 mg/mL (447.48 mM);Water : < 0.1 mg/mL (insoluble)	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	3.5799 mL	17.8993 mL	35.7987 mL
	5 mM	0.716 mL	3.5799 mL	7.1597 mL
	10 mM	0.358 mL	1.7899 mL	3.5799 mL

Molarity Calculator
Dilution Calculator

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal:μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Related Products

Reviews

Review for H-151

Average Rating: 5 ★★★★★ (Based on Reviews and 10 reference(s) in Google Scholar.)

5 Star

100%

4 Star

0%

3 Star

0%

2 Star

0%

1 Star

0%

Review for H-151

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

Overall Rating

★

Review Title

Review

Nickname

Email

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.

H-151

Customer Reviews

GlpBio Citations

Bioactive Compounds Premium Provider