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 (3089):

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-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-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-B0617S
    S-Adenosyl-L-methionine-d3 68684-40-2 99.55%
    S-Adenosyl-L-methionine-d3 is the deuterated product of S-Adenosyl-L-methionine. S-Adenosyl-L-methionine is endogenously produced from methionine and ATP through the action of methionine adenosyltransferase and is an important orally active methyl donor.
    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-144162S
    (Rac)-Selegiline-d5 hydrochloride
    (Rac)-Selegiline-d5 (hydrochloride) is the deuterium labeled (Rac)-Selegiline hydrochloride[1].
    (Rac)-Selegiline-d<sub>5</sub> hydrochloride
  • HY-A0069AS
    Doxylamine-d5 1173020-59-1
    Doxylamine-d5 is deuterium labeled Doxylamine.
    Doxylamine-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[1][2].
    SDMA-d<sub>6</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-<sup>13</sup>C<sub>5</sub>
  • 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-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-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[1][2].
    Kynurenic acid-d<sub>5</sub>
  • HY-108872S
    Water-18O 14314-42-2 99.99%
    Water-18O is the 18O-labeled Water[1].
    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-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-78131S
    Ibuprofen-d3 121662-14-4 99.18%
    Ibuprofen-d3 is a deuterium labeled Ibuprofen. Ibuprofen is a COX-1 and COX-2 inhibitor with IC50s of 13 μM and 370 μM[1].
    Ibuprofen-d<sub>3</sub>
  • HY-W015967S
    Glycolic acid-d2 75502-10-2 98.54%
    Glycolic acid-d2 is the deuterium labeled Glycolic acid. Glycolic acid is an inhibitor of tyrosinase, suppressing melanin formation and lead to a lightening of skin colour.
    Glycolic acid-d<sub>2</sub>