2. Isotope-Labeled Compounds
  3. Research Area
  4. Stable isotope-labeled inhibitors for use in in vivo cell experiments

Stable isotope-labeled inhibitors for use in in vivo cell experiments

By introducing stable isotope-labeled inhibitors, it becomes possible to trace precise metabolic pathways and metabolites within organisms. This valuable information provides a foundation for studying synthetic biology, understanding disease pathogenesis, and unraveling the mechanisms of drug actions. How do you screen for stable-isotope labeled inhibitors for in vivo experiments? Please refer to the summary provided byProfessor Juan Fernández-Garcí et al as showed below[1]

 

Figure 1. Outline of the different steps involved in an in vivo stable-isotope tracing experiment[1].

 

References:

[1] Trends Biochem Sci. 2020 Mar;45(3):185-201.

Stable isotope-labeled inhibitors for use in in vivo cell experiments (3154):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-13631DS
    Dxd-d5 98.89%
    Dxd-d5 is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) .
    Dxd-d<sub>5</sub>
  • HY-10201S
    Sorafenib-d3 1130115-44-4 99.57%
    Sorafenib-d3 (Donafenib), a deuterated compound of Sorafenib, is the first deuterium-generation tumor suppressor small molecule. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
    Sorafenib-d<sub>3</sub>
  • HY-N0390S2
    L-Glutamine-d5 14341-78-7 99.78%
    L-Glutamine-d5 is the deuterium labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells.
    L-Glutamine-d<sub>5</sub>
  • HY-100807S
    Quinolinic acid-d3 138946-42-6 99.90%
    Quinolinic acid-d3 is the deuterium labeled Quinolinic acid. Quinolinic acid is an endogenous N-methyl-D-aspartate (NMDA) receptor agonist synthesized from L-tryptophan via the kynurenine pathway and thereby has the potential of mediating N-methyl-D-aspartate neuronal damage and dysfunction.
    Quinolinic acid-d<sub>3</sub>
  • HY-B0617S
    S-Adenosyl-L-methionine-d3 68684-40-2 99.80%
    S-Adenosyl-L-methionine-d3 (S-Adenosyl methionine-d3) is the deuterated product of S-Adenosyl-L-methionine (HY-B0617). S-Adenosyl-L-methionine (S-Adenosyl methionine) is an orally active methyl group donor. S-Adenosyl-L-methionine is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine has the potential for, cancer, liver disease and osteoarthritis research.
    S-Adenosyl-L-methionine-d<sub>3</sub>
  • HY-B0228S9
    Adenosine-13C10,15N5 202406-75-5 99.60%
    Adenosine-13C10,15N5 is the 13C and 15N labeled Adenosine (HY-B0228). Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
    Adenosine-<sup>13</sup>C<sub>10</sub>,<sup>15</sup>N<sub>5</sub>
  • HY-111124
    Paroxetine-d2 923932-43-8
    Paroxetine-d2 (CTP 347) is a deuterium labeled Paroxetine (HY-122272). Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches.
    Paroxetine-d<sub>2</sub>
  • HY-B0196S4
    Venlafaxine-d9 940297-30-3
    Venlafaxine-d9 (Wy 45030-d9) is a deuterium labeled Venlafaxine (HY-B0196). Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant.
    Venlafaxine-d<sub>9</sub>
  • HY-N1428S1
    Citric acid-13C6 287389-42-8 99.90%
    Citric acid-13C6 is the 13C-labeled Citric acid (HY-N1428). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries.
    Citric acid-<sup>13</sup>C<sub>6</sub>
  • HY-15550S
    4'-Hydroxy diclofenac-d4 254762-27-1 98.92%
    4'-Hydroxy diclofenac-d4 is the deuterium labeled 4'-Hydroxy diclofenac. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties.
    4'-Hydroxy diclofenac-d<sub>4</sub>
  • HY-100806S
    Kynurenic acid-d5 350820-13-2 99.64%
    Kynurenic acid-d5 is the deuterium labeled Kynurenic acid. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
    Kynurenic acid-d<sub>5</sub>
  • HY-B0228S1
    Adenosine-13C5 159496-13-6 99.9%
    Adenosine-13C5 is the 13C labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
    Adenosine-<sup>13</sup>C<sub>5</sub>
  • HY-78131S
    Ibuprofen-d3 121662-14-4 99.94%
    Ibuprofen-d3 is a deuterium labeled Ibuprofen. Ibuprofen is a COX-1 and COX-2 inhibitor with IC50s of 13 μM and 370 μM.
    Ibuprofen-d<sub>3</sub>
  • HY-15531S
    Venetoclax-d8 1257051-06-1 99.76%
    Venetoclax-d8 is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy.
    Venetoclax-d<sub>8</sub>
  • HY-N0092S2
    Inosine-13C5 99.90%
    Inosine-13C5 is the 13C5 labeled Inosine (HY-N0092). Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors.
    Inosine-<sup>13</sup>C<sub>5</sub>
  • HY-W013636S
    2-Ketoglutaric acid-13C5 161096-83-9 99.1%
    2-Ketoglutaric acid-13C5 (Alpha-Ketoglutaric acid-13C5) is a 13C labeled 2-Ketoglutaric acid (HY-W013636). 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM).
    2-Ketoglutaric acid-<sup>13</sup>C<sub>5</sub>
  • HY-108872S
    Water-18O 14314-42-2 99.99%
    Water-18O is the 18O-labeled Water.
    Water-<sup>18</sup>O
  • HY-13704S
    SN-38-d3 718612-49-8 98.79%
    SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.
    SN-38-d<sub>3</sub>
  • HY-D0843S
    N-Ethylmaleimide-d5 360768-37-2 99.90%
    N-Ethylmaleimide-d5 is the deuterium labeled N-Ethylmaleimide. N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor.
    N-Ethylmaleimide-d<sub>5</sub>
  • HY-101410S
    SDMA-d6 1331888-08-4 98.07%
    SDMA-d6 is the deuterium labeled SDMA. SDMA (Symmetric dimethylarginine) is an endogenous inhibitor of nitric oxide (NO) synthase activity.
    SDMA-d<sub>6</sub>