(DEVD)2-R110

Product Name:(DEVD)2-R110

Form:TFA salt

Purity:95%

Storage:2-8 degree Celsius

Cas No:220846-75-3

Molar Mass:1247.2

Chemical Formula:C56H66N10O23

IUPAC Name:(4S)-4-[[(2S)-2-amino-3-carboxypropanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[6'-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-carboxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-3-carboxypropanoyl]amino]-3-oxospiro[2-benzofuran-1,9'-xanthene]-3'-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic acid

SMILES:CC(C)[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)NC1=CC2=C(C=C1)C3(C4=C(O2)C=C(C=C4)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)N)C5=CC=CC=C5C(=O)O3)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)N

InChIKey:NBDFNNHYGGESSN-DFRKUSGVSA-N

InChI:InChI=1S/C56H66N10O23/c1-23(2)45(65-49(81)33(13-15-39(67)68)61-47(79)31(57)19-41(71)72)53(85)63-35(21-43(75)76)51(83)59-25-9-11-29-37(17-25)88-38-18-26(10-12-30(38)56(29)28-8-6-5-7-27(28)55(87)89-56)60-52(84)36(22-44(77)78)64-54(86)46(24(3)4)66-50(82)34(14-16-40(69)70)62-48(80)32(58)20-42(73)74/h5-12,17-18,23-24,31-36,45-46H,13-16,19-22,57-58H2,1-4H3,(H,59,83)(H,60,84)(H,61,79)(H,62,80)(H,63,85)(H,64,86)(H,65,81)(H,66,82)(H,67,68)(H,69,70)(H,71,72)(H,73,74)(H,75,76)(H,77,78)/t31-,32-,33-,34-,35-,36-,45-,46-/m0/s1

Sequence:(Asp-Glu-Val-Asp)2-Rhodamine 110

Application:

(DEVD)₂-R110 is a fluorogenic substrate used to measure caspase-3 and caspase-7 activity in apoptosis research. It consists of two DEVD (Asp-Glu-Val-Asp) sequences linked to Rhodamine 110 (R110), a highly fluorescent dye. Upon cleavage by caspase-3/-7, the non-fluorescent substrate releases R110, producing a strong green fluorescence signal (Ex/Em: ~496/520 nm). This substrate is widely utilized in apoptosis assays, high-throughput drug screening, and studies of programmed cell death in cancer, neurodegeneration, and inflammation research. (DEVD)₂-R110 enables sensitive, real-time monitoring of caspase activation, making it an essential tool for studying cell death mechanisms and evaluating apoptosis-modulating compounds.

Current Research:

Caspases play a crucial role in apoptosis, the programmed cell death process essential for maintaining tissue homeostasis and eliminating damaged or diseased cells. Among them, caspase-3 and caspase-7 are key executioner caspases, responsible for the cleavage of structural and regulatory proteins that drive apoptosis. (DEVD)₂-R110 has become an essential fluorogenic substrate in apoptosis research, allowing real-time and high-throughput detection of caspase-3/-7 activity in various disease models.

1. Application in Cancer Research and Drug Screening
   Dysregulated apoptosis is a hallmark of cancer, with many tumors exhibiting resistance to cell death. Caspase-3 activity is a key indicator of apoptosis induction in response to chemotherapy, radiation, and targeted therapies. Researchers frequently use (DEVD)₂-R110 to evaluate apoptosis levels in tumor cells treated with anti-cancer agents, including small-molecule inhibitors, monoclonal antibodies, and immunotherapies.

High-throughput drug screening programs also employ this substrate to identify novel pro-apoptotic compounds, such as Bcl-2 inhibitors and proteasome inhibitors, which can restore apoptotic signaling in resistant cancer cells.

2. Role in Neurodegenerative Diseases and Neuronal Apoptosis
   Caspase activation is a key feature of neurodegenerative diseases, including Alzheimer’s disease (AD), Parkinson’s disease (PD), and Huntington’s disease (HD). In AD models, (DEVD)₂-R110 has been used to detect neuronal apoptosis triggered by β-amyloid toxicity, confirming the involvement of caspase-3 in neurodegeneration.

Similarly, in PD research, (DEVD)₂-R110 has been utilized to study dopaminergic neuron loss induced by mitochondrial dysfunction and oxidative stress. The substrate helps assess the effectiveness of neuroprotective compounds targeting apoptosis pathways in neurodegenerative conditions.

3. Inflammation and Autoimmune Disease Research
   Apoptotic caspases also regulate inflammation by controlling immune cell survival and activation. Excessive or defective apoptosis has been linked to autoimmune diseases, such as systemic lupus erythematosus (SLE) and rheumatoid arthritis (RA). (DEVD)₂-R110 has been used to measure caspase-3 activation in immune cells undergoing apoptosis, helping researchers understand how defects in apoptotic pathways contribute to chronic inflammation and autoimmunity.
4. Use in Toxicology and Drug Safety Assessment
   Toxicological studies frequently use (DEVD)₂-R110 to assess chemical- or drug-induced apoptosis in various tissues, including liver, kidney, and cardiac cells. This substrate is instrumental in evaluating the cytotoxic effects of new pharmaceuticals, environmental toxins, and industrial chemicals, ensuring drug candidates do not trigger excessive apoptosis in non-target tissues.

Conclusion
(DEVD)₂-R110 is a powerful fluorogenic substrate that has significantly advanced apoptosis research. Its application in cancer, neurodegeneration, autoimmune diseases, and drug toxicity studies underscores its value in biomedical research and drug discovery. By enabling real-time, sensitive caspase detection, it continues to facilitate breakthroughs in understanding cell death mechanisms and identifying novel therapeutic strategies.