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response to stress

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Histamine H1 receptor

315

Dopamine D2 receptor

297

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Bacterial penicillin-binding protein

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Dordaviprone

9U35A31JAI

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

TRAIL-activated apoptotic signaling pathway

response to stress

D2-like dopamine receptor

Serine/threonine-protein kinase AKT

Mitogen-activated protein kinase; ERK1/ERK2

Conditions:

Non-Hodgkin's lymphoma

Multiple myeloma

Triple-negative breast cancer

TIC10 (TIC10 isomer or ONC201 isomer) is a potent, orally active, and stable small molecule and is an efficacious antitumor therapeutic agent that acts on tumor cells and their microenvironment to enhance the concentrations of the endogenous tumor ne...

crosis factor-related apoptosis-inducing ligand (TRAIL). The isomeric structure of TIC10/ONC201 is critical to its activity: anti-cancer activity is associated with the angular structure and not the linear TIC10 isomer. TIC10 transcriptionally induces a sustained up-regulation TRAIL in tumors and normal cells in a p53-independent manner. TIC10 inactivates kinases Akt and extracellular signal-regulated kinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoter to up-regulate gene transcription. TIC10 crosses the blood-brain barrier. TIC10 treatment caused tumor regression in the HCT116 p53−/− xenograft, RKO human colon cancer xenograft–bearing mice and human triple-negative breast cancer xenografts and significantly prolonged the survival of Eμ-myc transgenic mice, which spontaneously develop metastatic lymphoma from weeks 9 to 12 of age by 4 weeks.

ISRIB

S6SZR97SBZ

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Status:

Other

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

response to stress

Translation initiation factor eIF-2B subunit delta

Dordaviprone Hydrochloride

53VG71J90J

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Search for Structure

Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

TRAIL-activated apoptotic signaling pathway

response to stress

D2-like dopamine receptor

Serine/threonine-protein kinase AKT

Mitogen-activated protein kinase; ERK1/ERK2

Conditions:

Non-Hodgkin's lymphoma

Multiple myeloma

Triple-negative breast cancer

TIC10 (TIC10 isomer or ONC201 isomer) is a potent, orally active, and stable small molecule and is an efficacious antitumor therapeutic agent that acts on tumor cells and their microenvironment to enhance the concentrations of the endogenous tumor ne...

crosis factor-related apoptosis-inducing ligand (TRAIL). The isomeric structure of TIC10/ONC201 is critical to its activity: anti-cancer activity is associated with the angular structure and not the linear TIC10 isomer. TIC10 transcriptionally induces a sustained up-regulation TRAIL in tumors and normal cells in a p53-independent manner. TIC10 inactivates kinases Akt and extracellular signal-regulated kinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoter to up-regulate gene transcription. TIC10 crosses the blood-brain barrier. TIC10 treatment caused tumor regression in the HCT116 p53−/− xenograft, RKO human colon cancer xenograft–bearing mice and human triple-negative breast cancer xenografts and significantly prolonged the survival of Eμ-myc transgenic mice, which spontaneously develop metastatic lymphoma from weeks 9 to 12 of age by 4 weeks.

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