PH-064

PH-064 (BIM-46187) is an orally active inhibitor of the heterotrimeric G-protein complex. PH-064 inhibits SERT activity and attenuates shear stress-induced Akt phosphorylation. PH-064 has potent anti-hyperalgesia activity. PH-064 inhibits G protein-coupled receptor-dependent tumorigenesis. PH-064 can be used in the study of pain (e.g., inflammatory pain, neuropathic pain), GPCR-dependent tumors, and inflammatory lung injury[1][2][3][4][5][6].

Product Specifications

CAS Number

[892546-37-1]

Product Name Alternative

BIM-46187

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Akt; Serotonin Transporter

Type

Reference compound

Related Pathways

Neuronal Signaling; PI3K/Akt/mTOR

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer; Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/PH-064.html

Purity

99.88

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C([C@H](CSSC[C@@H](C(N1CCN2C([C@@H]1CC3CCCCC3)=NC(C4=CC=CC=C4)=C2)=O)N)N)N([C@H]5CC6CCCCC6)CCN(C5=N7)C=C7C8=CC=CC=C8

Molecular Formula

C44H58N8O2S2

Molecular Weight

795.11

Precautions

H302, H315, H319, H335

References & Citations

[1]Favre-Guilmard C, et al. The novel inhibitor of the heterotrimeric G-protein complex, BIM-46187, elicits anti-hyperalgesic properties and synergizes with morphine. Eur J Pharmacol. 2008 Oct 10;594 (1-3) :70-6.|[2]Dela Paz NG, et al. Rapid flow-induced activation of Gαq/11 is independent of Piezo1 activation. Am J Physiol Cell Physiol. 2019 May 1;316 (5) :C741-C752. |[3]Haase J, et al. Sex and brain region-specific regulation of serotonin transporter activity in synaptosomes in guanine nucleotide-binding protein G (q) alpha knockout mice. J Neurochem. 2021 Oct;159 (1) :156-171.|[4]Auguet M, et al. SYNERGISTIC ANALGESIC INTERACTION BETWEEN MORPHINE AND BIM‐46187. European Journal of Pain, 2006, 10 (S1) : S89-S89. |[5]Silvente-Poirot S, et al. Heterotrimeric G-protein inhibitor BIM-46187 inhibits G-protein coupled receptor dependent tumorigenesis in athymic mice. Cancer Research, 2007, 67 (9_Supplement) : 5603-5603. |[6]Joshi JC, et al. RGS2 is an innate immune checkpoint for suppressing Gαq-mediated IFNγ generation and lung injury. iScience. 2025 Jan 27;28 (2) :111878.