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H-151 STING inhibitor

Name: H-151
Brand: Selleck Chemicals
SKU: S6652
Availability: InStock
Rating: 5 (36 reviews)

Cat.No.S6652

H-151 is a highly potent and covalent inhibitor of STING that has noteworthy inhibitory activity both in human cells and in vivo.

Chemical Structure

Molecular Weight: 279.34

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.94%

99.94

Products Often Used Together with H-151

Pevonedistat (MLN4924)

It and MLN4924 reduce cytokine production by inhibiting NF-κB and STING pathways by delivering anti-inflammatory agents to macrophages.

Related Targets	Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor TNF-alpha ROS Parasite PD-1/PD-L1 TLR Prostaglandin Receptor IFN CXCR Nrf2 NOS CCR NLRP3 eIF AhR IL Receptor NADPH-oxidase Complement System IRAK β-lactamase IDO/TDO PGES FKBP LTR
Related Products	C-176 CCCP diABZI STING agonist-1 (tautomerism) STING inhibitor C-178 C-171 G10 (STING agonist-1) MSA-2 SN-001 ZSA-51 NVS-STG2 diABZI STING agonist-1 trihydrochloride 2',3'-cGAMP Sodium Salt 3',3'-cGAMP STING Antibody [N23J24] SN-011 Cridanimod C-170 STING Antibody [F1N19]

Chemical Information, Storage & Stability

Molecular Weight	279.34	Formula	C₁₇H₁₇N₃O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	941987-60-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCC1=CC=C(C=C1)NC(=O)NC2=CNC3=CC=CC=C32

Solubility

In vitro
Batch:

DMSO : 56 mg/mL (200.47 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (8.95mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (2.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (17.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (14.32mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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.

Mechanism of Action

Targets/IC₅₀/Ki	STING ^[1]
In vivo	After intraperitoneal administration, H-151 reachs effective systemic levels, displays a short half-life in the serum and formed an adduct to mmSTING. Notably, pretreatment of this compound markedly reduces systemic cytokine responses in CMA-treated mice. Moreover, it exhibits notable efficacy in Trex1−/− mice that expressed a bioluminescent IFNβ reporter, when administered for one week.^[1]
References	[1] https://www.ncbi.nlm.nih.gov/pubmed/?term=Targeting+STING+with+covalent+small-molecule+inhibitors [2] https://pubmed.ncbi.nlm.nih.gov/36198273/

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