MSI-1436
Based on 8 publication(s) in Google Scholar
MSI-1436 is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of appr 1 μM, 200-fold preference over TCPTP (IC50, 224 μM).
For research use only. We do not sell to patients.
- CAS No.: 186139-09-3
- Formula: C37H72N4O5S
- Molecular Weight:685.06
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) MSI-1436
More- Nature. 2024 Jul;631(8020):415-423. [Abstract]
- Biomed Pharmacother. 2026 Jan:194:118951. [Abstract]
- J Ginseng Res. 2025 Nov;49(6):652-662. [Abstract]
- Commun Biol. 2021 Feb 24;4(1):248. [Abstract]
- Spectrochim Acta A Mol Biomol Spectrosc. 2024 Nov 3:327:125394. [Abstract]
- Exp Neurol. 2025 Mar:385:115115. [Abstract]
- Oncol Rep. 2024 Nov;52(5):149. [Abstract]
- J Leukoc Biol. 2024 Jul 16:qiae159. [Abstract]
Biological Activity
IC50: 1 μM (PTB1B), 224 μM (TCPTP)[1]
In HepG2, MSI-1436 (10 μM, 30 min) alone has no effect on phosphorylation of IRβ, but in conjunction with 100 nM insulin, MSI-1436 increases p-IRβ 18-fold over untreated cells and by approximately threefold over cells treated with insulin alone. MSI-1436's inhibition of TCPTP is approximately two logs less than the effect on PTP1B activity, with a resulting IC50 value of 224 μM[1]. MSI-1436 (Trodusquemine, 10 μM) restores ERK phosphorylation in response to mGluR1/5 agonist DHPG in F11 neuronal cells. MSI-1436 (10 uM) rescues DHPG-induced holding currents and restores DSI in LMO4KO BLA neurons[2]. MSI-1436 (0.1-100 μM) blocks PTP1B activity, has insulin-mimetic effects in cultured neuronal cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 186139-09-3
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Appearance Solid
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Molecular Weight 685.06
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Formula C37H72N4O5S
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Color White to yellow
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SMILES
NCCCNCCCCNCCCN[C@@H]1C[C@@](C[C@@H](O)[C@]2([H])[C@]3([H])CC[C@@]4(C)[C@@]2([H])CC[C@@]4([C@H](C)CC[C@@H](OS(=O)(O)=O)C(C)C)[H])([H])[C@]3(C)CC1
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Synonyms
Trodusquemine; Aminosterol-1436
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (8)
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Journal Impact Factor
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Most Recent
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Nature
2024 Jul;631(8020):415-423. PMID: 38867038 -
Biomed Pharmacother
Multi-target mechanisms of glabrone in ulcerative colitis: Synergistic restoration of mucosal barrier and inhibition of inflammation through SRC/HSP90 Co-modulation. [Abstract]2026 Jan:194:118951. PMID: 41496348 -
J Ginseng Res
(20S)-protopanaxatriol attenuates Ang II-induced renal injury via PTPN1-mediated AMPK/mTOR signaling pathway. [Abstract]2025 Nov;49(6):652-662. PMID: 41268307 -
Commun Biol
βA1-crystallin regulates glucose metabolism and mitochondrial function in mouse retinal astrocytes by modulating PTP1B activity. [Abstract]2021 Feb 24;4(1):248. PMID: 33627831 -
Spectrochim Acta A Mol Biomol Spectrosc
A novel fluorescent probe with Aggregation-Induced emission characteristics for PTP1B activity sensing and inhibitor screening. [Abstract]2024 Nov 3:327:125394. PMID: 39520822 -
Exp Neurol
Pharmacological PTP1B inhibition rescues motor learning, neuroinflammation, and hyperglycaemia in a mouse model of Alzheimer's disease. [Abstract]2025 Mar:385:115115. PMID: 39672227 -
Oncol Rep
The combination of a PTP1B inhibitor, TNFR2 blocker, and PD‑1 antibody suppresses the progression of non‑small cell lung cancer tumors by enhancing immunocompetence. [Abstract]2024 Nov;52(5):149. PMID: 39301655 -
J Leukoc Biol
Combination of microparticles vaccine with MSI-1436 exerts a strong immune response for hepatocellular carcinoma. [Abstract]2024 Jul 16:qiae159. PMID: 39012079
Protocol
Mice
Male AKR/J mice are randomLy placed on ad libitum 10, 45, or 60% fat kcal diets. After -14 weeks, mice are randomly assigned to three treatment groups (n=5-8 mice/group); MSI-1436 (initial dose of 10 mg/kg with three subsequent weekly doses of 5 mg/kg, intraperitoneally), vehicle (saline, 10 mL/kg, weekly 4×), or pair-fed (PF). PF animals are injected with saline (weekly 4×) and allotted the amount of food consumed daily by MSI-1436-treated animals. On day 23, mice are anesthetized and euthanized for blood and tissue collection, respectively. Plasma is obtained following centrifugation of blood 14,000 rpm for 10 min at 4°C.
Rats
Nine-week-old male Sprague-Dawley rats (225-260 g) with ad libitum access to normal rodent chow are dosed intraperitoneally with MSI-1436 (10 mg/kg, IP) or saline. After an overnight fast, the rats are dosed intraperitoneally with saline or 100 U/kg of insulin. At 30 min after dose, animals are killed, and hypothalami are harvested and homogenized in 1 mL of tissue extraction reagent plus phosphatase and protease inhibitors. Samples are centrifuged (14,000 rpm for 10 min at 4°C), and the protein content of the supernatants are quantitated via BCA kit.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lantz KA, et al. Inhibition of PTP1B by trodusquemine (MSI-1436) causes fat-specific weight loss in diet-induced obese mice. Obesity (Silver Spring). 2010 Aug;18(8):1516-1523. [Content Brief]
[2]. Qin Z, et al. Chronic stress induces anxiety via an amygdalar intracellular cascade that impairs endocannabinoid signaling. Neuron. 2015 Mar 18;85(6):1319-31. [Content Brief]
[3]. Qin Z, et al. Functional properties of Claramine: a novel PTP1B inhibitor and insulin-mimetic compound. Biochem Biophys Res Commun. 2015 Feb 27;458(1):21-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)