d 06

AL 082D06 (D-06), a selective nonsteroidal glucocorticoid receptor (GR) antagonist (Ki: 210 nM), exhibits outstanding selectivity against AR, ER, MR and PR(Ki > 10 uM).

VVD 065 is an NRF2 inhibitor that functions through a covalent allosteric binding mechanism. It promotes the degradation of NRF2 by covalently bonding with C151 on KEAP1, thereby enhancing the formation of the KEAP1-CUL3 ubiquitin ligase complex. With potent target binding affinity (TE50 of 9 nM in KYSE70 cells) and selectivity for unrelated targets, VVD 065 effectively inhibits NRF2-associated cell growth.

(S)-WSD0628 is the S isomer of WSD0628 and serves as an ATM inhibitor, effectively suppressing ATM phosphorylation in MCF-7 cells with an IC50 of less than 100 nM. This compound also demonstrates radiosensitizing activity and is capable of penetrating the blood-brain barrier.

PVD-06 is a selective PROTAC-based degrader of PTPN2 (with a selectivity index of greater than 60-fold over PTP1B) and exhibits anticancer activity. It induces the degradation of PTPN2 through ubiquitination and proteasome-dependent pathways. PVD-06 also enhances T cell activation and amplifies IFN-γ-mediated cytotoxicity.

CYD0682 is an analog of Oridonin. It reduces the activation of STAT3 and the production of ECM in hepatic stellate cells via the HSP90 pathway.

Elvitegravir (JTK-303) is a Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor. The mechanism of action of elvitegravir is as an HIV Integrase Inhibitor, and Cytochrome P450 2C9 Inducer.

Zosuquidar trihydrochloride (LY-335979 trihydrochloride) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.

SD 0006 (SD-06) is a MAPK p38 alpha inhibitor with an IC50 of 110 nM, indicated for the treatment of arthritis.

WSD0628 is a brain-penetrant and potent ATM inhibitor with a significant radiosensitizing effect [1].

SD-066-4 is an orally active acyltransferase inhibitor that can be utilized in cancer research.

BRD0639 is a pioneering inhibitor targeting the interaction between PRMT5 and its substrate adaptor. As a competitive inhibitor of the PRMT5 binding motif (PBM), BRD0639 facilitates the investigation of activities dependent on PBM-associated PRMT5 functions [1].

L-Leucine-1-13C,15N is L-Leucine that is labeled with 13C and 15N. L-Leucine is an essential branched-chain amino acid (BCAA) known to activate the mTOR signaling pathway.

ATP-d14 (Adenosine 5'-triphosphate-d14) dilithium is the deuterium-labeled form of ATP. ATP (Adenosine 5'-triphosphate) is a crucial compound for energy storage and metabolism in the body, providing energy for metabolic processes and functioning as a coenzyme within cells. It also acts as a significant endogenous signaling molecule in immunity and inflammation.

Probenecid-d14 is a deuterated form of Probenecid. Probenecid serves as a potent and selective agonist of the transient receptor potential vanilloid 2 (TRPV2) channel. Additionally, it acts as an inhibitor of pannexin 1 channels.

Acetaminophen-13C2,15N is an isotopically labeled version of Acetaminophen, incorporating both 13C and 15N atoms. Acetaminophen (Paracetamol) serves as a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 25.8 μM. It is also a potent inhibitor of hepatic N-acetyltransferase 2 (NAT2). Acetaminophen is widely utilized as an antipyretic and analgesic agent.

Oseltamivir-d5 is the deuterated form of Oseltamivir, a neuraminidase (NAI) inhibitor targeting influenza viruses. It effectively suppresses influenza A/H3N2, A/H1N2, A/H1N1, and influenza B viruses, with average IC50 values of 0.67, 0.9, 1.34, and 13 nM, respectively.

D-Galactose-13C is a 13C-labeled D-Galactose. D-Galactose is a naturally occurring hexose and is the C-4 epimer of glucose.

N-Nitrosodiethylamine-d4 is the deuterated form of N-Nitrosodiethylamine. N-Nitrosodiethylamine (Diethylnitrosamine) is a potent carcinogenic dialkylnitrosamine. It is commonly found in tobacco smoke, water, cheddar cheese, cured foods, fried foods, and several alcoholic beverages. N-Nitrosodiethylamine is known to affect enzymatic processes related to DNA repair and replication, leading to various tumors in animals. The primary target organs are the nasal cavity, trachea, lungs, esophagus, and liver.

4-Hydroxyphenylacetic acid-d4 is the deuterated form of 4-Hydroxyphenylacetic acid. 4-Hydroxyphenylacetic acid, primarily derived from the microbial metabolism of polyphenols, exhibits antioxidant properties and induces the expression of Nrf2.

Metoprolol-d5 is a deuterated form of Metoprolol. Metoprolol is an orally active, selective β1-adrenoceptor antagonist with anti-inflammatory, anti-tumor, and anti-angiogenic properties.

Hypoxanthine-13C2,15N is a DL-Cystine compound labeled with both 15N and 13C isotopes.

Uridine-13C5 (β-Uridine-13C5) is a variant of uridine labeled with carbon-13. It is a nucleoside compound composed of uracil attached to a ribose ring, linked through a β-N1-glycosidic bond.

Choline-13C2(chloride) is the 13C-labeled version of Choline chloride. As an essential nutrient, Choline chloride activates α7 nicotinic receptors (alpha7 nicotinic receptors) and exhibits analgesic and anti-inflammatory properties. It may influence conditions such as liver diseases, atherosclerosis, and neurological disorders.

L-Glutathione reduced-13C2,15N is an isotopically labeled variant of L-Glutathione reduced, incorporating both 13C and 15N. L-Glutathione reduced (GSH; γ-L-Glutamyl-L-cysteinyl-glycine) functions as an endogenous antioxidant, capable of scavenging oxygen free radicals.