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Product details:
CAS
287403-39-8
Purity
95%
TMI 1 is an inhibitor of disintegrin and metalloproteinase domain-containing protein 17 (ADAM17/TACE). It inhibits matrix metalloproteinase-1 (MMP-1), -2, -7, -9, -13, and -14, as well as ADAM-TS-4 in vitro.
Properties
Name
TMI 1
Smiles
CC#CCOC=1C=CC(=CC1)S(=O)(=O)N2CCSC(C)(C)[C@@H]2C(=O)NO
Targets
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Sold for research purposes under agreement from Pfizer Inc.
TMI 1 (CAS 287403-39-8) is a potent dual inhibitor of ADAM17 (TACE) and matrix metalloproteases, also known as WAY-171318 and PF-05312062. The compound demonstrates nanomolar inhibitory activity across multiple metalloprotease targets and is orally bioavailable, making it a versatile tool for inflammation and oncology research. Enamine offers TMI 1 as a high-purity screening sample for in vitro and in vivo experimental models.
TMI 1 is a hydroxamate-based thiomorpholine compound with molecular formula C₁₇H₂₂N₂O₅S₂ and TMI 1 molecular weight of 398.49 g/mol. The TMI 1 chemical structure incorporates a sulfonyl-linked phenyl group with a butynyloxy substituent and an N-hydroxy carboxamide moiety responsible for zinc ion coordination at the active site. Researchers study the TMI 1 structure to understand its binding geometry within MMP and ADAM17 catalytic domains. The compound is registered under CAS 287403-39-8 and sold under agreement from Pfizer Inc.
TMI 1 is applied in research targeting TNF-α–driven inflammatory pathways, metalloprotease-mediated tissue remodeling, and tumor biology. It is particularly relevant for studies on rheumatoid arthritis, cancer progression, and neuroinflammation. WAY-171318 is used in screening workflows requiring well-characterized reference inhibitors and in mechanistic studies exploring ADAM17 substrate shedding and downstream cytokine regulation.
TMI 1 inhibits ADAM17 and a broad panel of MMPs with IC₅₀ values of 3–26 nM across MMP-13, MMP-2, MMP-1, ADAM17, MMP-9, MMP-7, and MMP-14. The compound potently suppresses LPS-induced TNF-α secretion in human primary monocytes and whole blood, and selectively induces caspase-dependent apoptosis in triple-negative and ERBB2-overexpressing breast tumor cell lines.
In vivo, TMI 1 suppresses TNF-α production in an acute LPS mouse model and reduces severity scores in a rheumatoid arthritis model. PF-05312062 induces tumor apoptosis in a breast cancer model and demonstrates oral bioavailability, supporting its use in dose-response and translational research studies.
TMI 1 acts by coordinating the catalytic zinc ion within the ADAM17 and MMP active sites through its hydroxamate moiety, blocking substrate access and proteolytic processing. This reduces ectodomain shedding of TNF-α and attenuates downstream inflammatory signaling. At the cellular level, WAY-171318 triggers caspase-dependent apoptosis selectively in tumor cells, with limited toxicity toward normal cells.
TMI 1 (WAY-171318, CAS 287403-39-8) offers a well-documented activity profile across multiple research areas:
When sourced as EBC-114027, TMI 1 is provided with analytical quality control data for consistent use in pharmacological and biochemical studies.
SDS
TMI-1
No data available
The compound has purity validated by NMR and/or LCMS methods.
1 mg
$80
2 mg
$90
5 mg
$100
10 mg
$149
15 mg
$180
20 mg
$211
25 mg
$257
30 mg
$302
35 mg
$348
40 mg
$394
45 mg
$422
50 mg
$450
75 mg
$599
100 mg
$POA
Quantity
1
Total amount
$ 100
TMI-1
No data available
The compound has purity validated by NMR and/or LCMS methods.
Target activity features
It should be emphasized that the product may be active against a larger number of targets than shown on the card. The information represented here refers to the targets with the largest value of pX or the targets with ΔpX less than 1.5 from the largest pX value.