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 (3157):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-13631DS
    Dxd-d5 98.84%
    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) [1].
    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 98.5%
    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[1][2].
    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[1][2].
    Quinolinic acid-d<sub>3</sub>
  • HY-B0617S
    S-Adenosyl-L-methionine-d3 68684-40-2 99.55%
    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-118645S
    1'-Hydroxymidazolam-d4 1781843-10-4 99.12%
    1'-Hydroxymidazolam-d4 is the deuterium labeled 1'-Hydroxymidazolam. 1'-Hydroxymidazolam is a primary active metabolite of Midazolam, and it is a neuronal depressant agent. 1'-Hydroxymidazolam could inhibit neuronal activity add to the effects of Midazolam[1][2].
    1'-Hydroxymidazolam-d<sub>4</sub>
  • HY-D0844S
    Glutathione oxidized-13C4,15N2 1416898-83-3 ≥98.0%
    Glutathione oxidized-13C4,15N2 is the 13C and 15N labeled Glutathione oxidized (HY-D0844). Glutathione oxidized is produced by the oxidation of glutathione. Detoxification of reactive oxygen species is accompanied by production of glutathione oxidized. Glutathione oxidized can be used for the research of sickle cells and erythrocytes.
    Glutathione oxidized-<sup>13</sup>C<sub>4</sub>,<sup>15</sup>N<sub>2</sub>
  • HY-100806S
    Kynurenic acid-d5 350820-13-2 98.35%
    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-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[1][2][3].
    Venetoclax-d<sub>8</sub>
  • HY-D0843S
    N-Ethylmaleimide-d5 360768-37-2 99.49%
    N-Ethylmaleimide-d5 is the deuterium labeled N-Ethylmaleimide. N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor[1]. N-ethylmaleimide specific inhibits phosphate transport in mitochondria[2]. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor[3].
    N-Ethylmaleimide-d<sub>5</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-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[1][2].
    4'-Hydroxy diclofenac-d<sub>4</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[1][2].
    SDMA-d<sub>6</sub>
  • HY-108872S
    Water-18O 14314-42-2 99.99%
    Water-18O is the 18O-labeled Water.
    Water-<sup>18</sup>O
  • HY-19939S
    VX-984 1476074-39-1 98.86%
    VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium.
    VX-984
  • HY-131968
    BMS-986202 1771691-34-9 99.92%
    BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 value of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 value of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research. BMS-986202 is a de novo deuterium.
    BMS-986202
  • HY-13704S
    SN-38-d3 718612-49-8 99.07%
    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[1][2][3][4].
    SN-38-d<sub>3</sub>
  • HY-N1428S1
    Citric acid-13C6 287389-42-8 ≥99.0%
    Citric acid-13C6 is the 13C-labeled Citric acid. Citric acid is a weak organic tricarboxylic acid found in citrus fruits. Citric acid is a natural preservative and food tartness enhancer.
    Citric acid-<sup>13</sup>C<sub>6</sub>
  • HY-W013636S
    2-Ketoglutaric acid-13C5 161096-83-9 98.6%
    2-Ketoglutaric acid-13C5 is the 13C labeled 2-Ketoglutaric acid[1]. 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].
    2-Ketoglutaric acid-<sup>13</sup>C<sub>5</sub>
  • HY-W008772S
    4-Hydroxymephenytoin-d3 1173022-56-4 99.05%
    4-Hydroxymephenytoin-d3 is the deuterium labeled 4-Hydroxymephenytoin. 4-Hydroxymephenytoin is a metabolism of an antiepileptic agent mephenytoin, which is used as a CYP2C19 substrate[1][2].
    4-Hydroxymephenytoin-d<sub>3</sub>