MSI-1436

Research use only, not for human use.

An non-competitive, allosteric inhibitor of PTP1B with Ki of 0.6 uM for PTP1B1-405; antagonizes HER2 signaling.

An non-competitive, allosteric inhibitor of PTP1B with Ki of 0.6 uM for PTP1B1-405; antagonizes HER2 signaling, inhibits tumorigenesis in xenografts and abrogates metastasis in the NDL2 mouse model of breast cancer. Breast Cancer Phase 1 Clinical

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. 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. MSI-1436 (0.1-100 μM) blocks PTP1B activity, has insulin-mimetic effects in cultured neuronal cells.

MSI-1436 (10 mg/kg, i.p.) causes obesity-dependent body weight, reduces total body fat content and adipocyte size and lipid content of white adipose tissue of mice. MSI-1436 treatment significantly reduces plasma insulin levels. MSI-1436 (10 mg/kg, i.p.) increases phosphorylation of STAT-3 2.7-fold and, in conjunction with 100 U/kg insulin, p-IRβ increases threefold over insulin alone-treated rats. MSI-1436 (Trodusquemine) exhibits anxiolytic effect through a restoration of endocannabinoid (eCB) signaling within the amygdala. MSI-1436 (5 mg/kg, i.p.) has an anti-diabetic effect on diabetic mice, and is sufficient to suppress food intake and cause weight loss in CD1 mice.

Trodusquemine | Aminosterol-1436 | MSI1436

Metabolic Enzyme/Protease

Protein Phosphatase/PTP

Protein Phosphatase/PTP

Cancer

Breast Cancer

186139-09-3

685.0564

C37H72N4O5S

>98% (HPLC)

10 mM in DMSO

CC(C)C(CCC(C)C1CCC2C1(CCC3C2C(CC4C3(CCC(C4)NCCCNCCCCNCCCN)C)O)C)OS(=O)(=O)O

Cholestane-7,24-diol, 3-[[3-[[4-[(3-aminopropyl)amino]butyl]amino]propyl]amino]-, 24-(hydrogen sulfate), (3β,5α,7α,24R)-

(-20℃)

With Ice Pack

≥ 2 years