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Bioymifi, TRAIL Receptor DR5 Activator

Bioymifi, TRAIL Receptor DR5 Activator

$109.00
A potent and selective small molecule agonist of DR5.
Catalog No. Unit Price Qty
M60088-2s 2mg solid $109.00
M60088-2 10 mM DMSO (0.405 mL) $109.00

Details

Product Information
Molecular Weight: 494.32
Formula: C22H12BrN3O4S
Purity: ≥ 97%
CAS#: 1420071-30-2
Solubility: DMSO up to 50 mM
Chemical Name: (Z)-5-(5-((3-(4-bromophenyl)-2-imino-4-oxothiazolidin-5-ylidene)methyl)furan-2-yl)isoindoline-1,3-dione
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.


Biological Activity:

Bioymifi is a potent and selective small molecule agonist of DR5, identified by a high-throughput chemical screening for compounds that promote cell death in synergy with a small-molecule mimetic of Smac. Bioymifi directly targets DR5, specifically binds the ECD of DR5 (Kd ~1.2 μM), and induces the formation of DR5 aggregates and DR5 activation. Bioymifi induces caspase-8–dependent apoptosis, which occurs through a DR5-dependent extrinsic pathway but independent of TRAIL. Bioymifi is capable of acting as a single agent to induce DR5 clustering and aggregation, leading to apoptosis without the need for a Smac mimetic in a variety of cancer cell lines, even in U2OS and HT29 cell lines. Bioymifi could be a potential lead compound for the development of small-molecule TRAIL mimics targeting DR5 for cancer therapy.

 

How to Use:

In vitro:  Bioymifi was used at 5-10 µM final concentration in vitro and in cellular assays.

In vivo:  n/a

 

Reference:

  1. 1. Wang G, et al. Small-molecule activation of the TRAIL receptor DR5 in human cancer cells. (2012) Nat Chem Biol. 9(2):84-89.


   Bioymifi_spec.pdf

   Bioymifi_MSDS.pdf



Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 494.32
Formula: C22H12BrN3O4S
Purity: ≥ 97%
CAS#: 1420071-30-2
Solubility: DMSO up to 50 mM
Chemical Name: (Z)-5-(5-((3-(4-bromophenyl)-2-imino-4-oxothiazolidin-5-ylidene)methyl)furan-2-yl)isoindoline-1,3-dione
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.


Biological Activity:

Bioymifi is a potent and selective small molecule agonist of DR5, identified by a high-throughput chemical screening for compounds that promote cell death in synergy with a small-molecule mimetic of Smac. Bioymifi directly targets DR5, specifically binds the ECD of DR5 (Kd ~1.2 μM), and induces the formation of DR5 aggregates and DR5 activation. Bioymifi induces caspase-8–dependent apoptosis, which occurs through a DR5-dependent extrinsic pathway but independent of TRAIL. Bioymifi is capable of acting as a single agent to induce DR5 clustering and aggregation, leading to apoptosis without the need for a Smac mimetic in a variety of cancer cell lines, even in U2OS and HT29 cell lines. Bioymifi could be a potential lead compound for the development of small-molecule TRAIL mimics targeting DR5 for cancer therapy.

 

How to Use:

In vitro:  Bioymifi was used at 5-10 µM final concentration in vitro and in cellular assays.

In vivo:  n/a

 

Reference:

  1. 1. Wang G, et al. Small-molecule activation of the TRAIL receptor DR5 in human cancer cells. (2012) Nat Chem Biol. 9(2):84-89.


   Bioymifi_spec.pdf

   Bioymifi_MSDS.pdf



Products are for research use only. Not for human use.

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