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Merck
CN

SML0702

MRT67307 hydrochloride

≥98% (HPLC), IKKe and TBK-1 inhibitor, powder

Synonym(s):

N-[3-[[5-Cyclopropyl-2-[[3-(4-morpholinylmethyl)phenyl]amino]-4-pyrimidinyl]amino]propyl]-cyclobutanecarboxamide hydrochloride

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About This Item

Empirical Formula (Hill Notation):
C26H36N6O2 · xHCl
CAS Number:
1190378-57-4
Molecular Weight:
464.60 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77

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Product Name

MRT67307 hydrochloride, ≥98% (HPLC)

Quality Level

100

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to light brown

solubility

H2O: 15 mg/mL, clear

storage temp.

2-8°C

SMILES string

N5(CCOCC5)Cc1cc(ccc1)Nc2nc(c(cn2)C4CC4)NCCCNC(=O)C3CCC3

InChI

1S/C26H36N6O2/c33-25(21-5-2-6-21)28-11-3-10-27-24-23(20-8-9-20)17-29-26(31-24)30-22-7-1-4-19(16-22)18-32-12-14-34-15-13-32/h1,4,7,16-17,20-21H,2-3,5-6,8-15,18H2,(H,28,33)(H2,27,29,30,31)

InChI key

UKBGBACORPRCGG-UHFFFAOYSA-N

Related Categories

Application

MRT67307 hydrochloride has been used to study its effect on LPS (lipopolysaccharide) -induced lysosome tubulation.

Biochem/physiol Actions

MRT67307 is a dual inhibitor of the IKKe and TBK-1.
MRT67307 is a dual inhibitor of the IKKe and TBK-1. IKKe and TBK-1 mediate the phosphorylation of interferon regulatory factor 3 (IRF3).
MRT67307 is an amino-pyrimidine derivative and has an IC50 value of 19. It is known to induce TLR (toll like receptor) mediated anti inflammatory cytokine generation. Also, MRT67307 prevents the secretion of cytokines associated with proinflammation.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000399515
0000399515
0000213794
0000213793
0000213793

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Daniel P.
The Inhibitor Index: A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads (2017)
Therapeutic potential of targeting TBK1 in autoimmune diseases and interferonopathies.
Hasan M and Nan Y
Pharmacological Research, 111, 336-342 (2016)
Zachary P Guinn et al.
Immunobiology, 224(4), 565-574 (2019-05-11)
IFN-γ produced during viral infections activates the IFN-γ receptor (IFNGR) complex for STAT1 transcriptional activity leading to expression of Interferon Regulatory Factors (IRF). Simultaneous activation of TBK/IKKε via TLR3 during viral infections activates the transcription factor IRF3. Together these transcription factors
mTOR controls lysosome tubulation and antigen presentation in macrophages and dendritic cells.
Saric A, et al.
Molecular Biology of the Cell, 27(2), 321-333 (2016)
Olga Bondareva et al.
Nature metabolism, 4(11), 1591-1610 (2022-11-19)
Obesity promotes diverse pathologies, including atherosclerosis and dementia, which frequently involve vascular defects and endothelial cell (EC) dysfunction. Each organ has distinct EC subtypes, but whether ECs are differentially affected by obesity is unknown. Here we use single-cell RNA sequencing
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