H 151
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MedKoo CAT#: 584647

CAS#: 941987-60-6

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


Chemical Structure

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H 151
CAS# 941987-60-6

Theoretical Analysis

MedKoo Cat#: 584647
Name: H 151
CAS#: 941987-60-6
Chemical Formula: C17H17N3O
Exact Mass: 279.14
Molecular Weight: 279.343
Elemental Analysis: C, 73.10; H, 6.13; N, 15.04; O, 5.73

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 Weeks
100mg USD 800 2 Weeks
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Synonym: H 151; H-151; H151;

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:
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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. 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

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.

Recalculate based on batch purity %
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: 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.

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