H 151 | CAS#941987-60-6 | STING antagonist

MedKoo Cat#: 584647 | Name: H 151

Description:

WARNING: This product is for research use only, not for human or veterinary use.

H 151 is a STING antagonist that covalently binds STING at Cys91, blocking palmitoylation and preventing assembly of STING clusters.

Chemical Structure

H 151

CAS#941987-60-6

Theoretical Analysis

MedKoo Cat#: 584647

Name: H 151

CAS#: 941987-60-6

Chemical Formula: C17H17N3O

Exact Mass: 279.1372

Molecular Weight: 279.34

Elemental Analysis: C, 73.10; H, 6.13; N, 15.04; O, 5.73

Price and Availability

Size	Price	Availability
50mg	USD 350.00	2 Weeks
100mg	USD 550.00	2 Weeks
200mg	USD 850.00	2 Weeks
500mg	USD 1,650.00	2 Weeks
1g	USD 2,950.00	2 Weeks

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Related CAS #

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Synonym

H 151; H151; H-151; NSC845762; NSC 845762; NSC-845762

IUPAC/Chemical Name

N-(4-Ethylphenyl)-N'-1H-indol-3-yl-urea

InChi Key

UJZDIKVQFMCLBE-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H17N3O/c1-2-12-7-9-13(10-8-12)19-17(21)20-16-11-18-15-6-4-3-5-14(15)16/h3-11,18H,2H2,1H3,(H2,19,20,21)

SMILES Code

O=C(NC1=CNC2=C1C=CC=C2)NC3=CC=C(CC)C=C3

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934999001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

H-151 is a potent, selective and covalent antagonist of STING that has noteworthy inhibitory activity both in cells and in vivo. H-151 reduces TBK1 phosphorylation and suppresses STING palmitoylation.

In vitro activity:

TBD

In vivo activity:

Kidney tissues from cisplatin-treated mice showed obvious apoptotic tubular cells stained with TUNEL, while H151 treatment reduced the number of TUNEL-positive cells (Fig. 4, A and B). These data were consistent with the decreased level of cleaved caspase-3 in kidney tissues from the H151-treated group (Fig. 4, C and D), suggesting that H151 ameliorated cisplatin-induced renal tubular cell death in mice. Reference: Am J Physiol Renal Physiol. 2021 Apr 1;320(4):F608-F616. https://pubmed.ncbi.nlm.nih.gov/33615891/

	Solvent	mg/mL	mM
Solubility
	DMF	30.0	107.39
	DMSO	36.3	129.93
	DMSO:PBS (pH 7.2) (1:2)	0.3	1.07
	Ethanol	10.7	38.15

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 279.34 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Gong W, Lu L, Zhou Y, Liu J, Ma H, Fu L, Huang S, Zhang Y, Zhang A, Jia Z. 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. doi: 10.1152/ajprenal.00554.2020. Epub 2021 Feb 22. PMID: 33615891.

In vitro protocol:

TBD

In vivo protocol:

Haag et al (2018) Targeting STING with covalent small-molecule inhibitors. Nature 559 269 PMID: 29973723