H-151 is a highly potent, selective and covalent antagonist of STING, reduces TBK1 phosphorylation and suppresses human STING palmitoylation. H-151 (0.02-2 μM) reduces IFNβ luciferase reporter measurements of HEK293T cells. H-151 (0.5 μM; 2 h) inhibits the phosphorylation of TBK1 in THP-1 cells.
Molecular Weight | 279.34 |
Formula | C17H17N3O |
CAS Number | 941987-60-6 |
Solubility (25°C) | DMSO ≥ 100 mg/mL |
Storage | -20°C, dry, sealed |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Simone M Haag, et al. Nature. Targeting STING with covalent small-molecule inhibitors
Related STING Products |
---|
STING agonist-30
STING agonist-30 is a potent STING agonist. |
F-CRI1
F-CRI1 is a potent STING agonist with a Kd value of 40.62 nM. |
STING agonist-31
STING agonist-31 is a STING agonist, with EC50 values of 0.24 and 39.51 μM for h-STING and m-STING. |
BI 7446
BI 7446 is a cyclic dinucleotide (CDN)-based potent and selective stimulator of interferon genes (STING) agonist. |
STING agonist-8 dihydrochloride
STING agonist-8 dihydrochloride is a potent STING agonist with an EC50 of 27 nM in THP1-Dual KI-hSTING-R232 cells. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.