Cytochrome P450 Inhibitor

β-Zearalenol (Standard) is the analytical standard of β-Zearalenol (HY-N6741). This product is intended for research and analytical applications. β-Zearalenol is a zearalenone metabolite and Estrogen receptor binder (K_d = 0.406 nM) that induces apoptosis through activation of p53, JNK, and p38 kinases and the mitochondrial apoptosis pathway, while inhibiting CYP19A1 and inducing autophagy via SIRT1. β-Zearalenol is used in research on cardiotoxicity, mycotoxin-induced reproductive toxicity, and breast cancer.

(S)-Nornicotine (Standard) is the analytical standard of (S)-Nornicotine (HY-W040430). This product is intended for research and analytical applications. (S)-Nornicotine is a nicotine metabolite that crosses the blood-brain barrier. (S)-Nornicotine weakly inhibits human CYP2A6 with a K_i >300 μM. (S)-Nornicotine promotes dopamine release in rat striatal and nucleus accumbens slices and increases endogenous DOPAC overflow through a calcium-dependent nAChR pathway that is sensitive to Mecamylamine (HY-B1395A). (S)-Nornicotine reduces behavioral responses maintained by nicotine or sucrose, exerts analgesic effects in persistent inflammatory pain and neuropathic pain models, and enhances the analgesic effect of morphine. (S)-Nornicotine is useful for research on tobacco dependence and pain.

BM-51 is a selective inhibitor of CYP4Z1, with a human IC₅₀ value of 91.7 nM. BM-51 binds to amino acid residues of CYP4Z1, thereby inhibiting its enzymatic activity. BM-51 downregulates the protein expression of stem cell markers (ALDH1A1, SOX2, OCT3/4 and KLF4) in cancer cells, inhibits cancer cell migration and invasion, and exhibits low toxicity to normal cells/tissues. BM-51 suppresses tumor initiation capacity and enhances the chemotherapeutic efficacy of Doxorubicin (HY-15142A). BM-51 can be used in breast cancer-related research.

Seneciphylline (Standard) is the analytical standard of Seneciphylline. This product is intended for research and analytical applications. Seneciphylline is a toxic pyrrolizidine alkaloid in Gynura japonica. Seneciphylline significantly increases the activities of epoxide hydrase and glutathione-S-transferase but causes reduction of cytochrome P-450 and related monooxygenase activities.

Exemestane-¹³C₃ is the ¹³C-labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC₅₀s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.

Furohyperforin is a natural product isolated from Hypericum perforatum L., possessing neuroprotective and antidepressant activities. Furohyperforin acts as an NLRP3 inflammasome inhibitor and also exhibits inhibitory effects on recombinant CYP3A4. Furohyperforin exerts neuroprotective effects against corticosterone-induced neuronal damage. Furohyperforin inhibits the NLRP3 inflammasome cascade and its downstream IL‑1β and GSDMD signaling pathways, and also reduces serum corticosterone levels in mice, regulating HPA axis function. Furohyperforin is applicable for depression-related research.

ADL-5859 is a selective and orally active δ opioid receptor (DOR) agonist with an K_i and an EC₅₀ value of 0.84 and 20 nM, respectively. ADL-5859 also shows inhibitory activity to hERG channel with an IC₅₀ value of 78 μM. ADL-5859 can be used for the research of pain.

CZx-243 is an orally active broad-spectrum antifungal agent. CZx-243 binds to the active site of fungal CYP51 and interferes with ergosterol biosynthesis by depleting ergosterol and causing the accumulation of upstream sterol intermediates. CZx-243 blocks yeast-to-hypha transition; it inhibits the membrane integrity of fungi such as Candida glabrata and Cryptococcus neoformans. CZx-243 significantly reduces renal fungal burden in a systemic mouse model of invasive fungal infection resistant to Fluconazole (HY-B0101). CZx-243 can be used in the research of fungal infections.

EGFR-IN-137 (Compound 4c) is an inhibitor for aromatase and EGFR with IC₅₀s of 1.67 μg/mL and 0.08 μg/mL. EGFR-IN-137 inhibits the proliferation of cancer cell MCF-7 and MDA-MB-231 with IC₅₀s of 1.62 µM and 4.14 µM. EGFR-IN-137 arrests the cell cycle at G0/G1 phase in MDA-MB-231, and induces apoptosis through caspase-dependent pathway.

(S)-Aminoglutethimide is an aromatase inhibitor. (S)-Aminoglutethimide has an IC₅₀ value of 23.15 μM for rat ovarian microsomal aromatase. (S)-Aminoglutethimide can be used in the research of diseases such as breast cancer.

Isosilybin (Standard) is the analytical standard of Isosilybin. This product is intended for research and analytical applications. Isosilybin (Isosilybinin) is a flavonoid from Silybum marianum; inhibits CYP3A4 induction with an IC50 of 74 μM.

CYP51/PD-L1-IN-2 (compound L20) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-2 is a dual inhibitor of CYP51 (IC₅₀: 0.263 μM) and PD-L1 (IC₅₀: 0.017 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-2 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death.

CYP1B1-IN-14 TFA is a metabolically stable hCYP1B1 competitive inhibitor with an IC₅₀ of 1.32 nM and a K_i of 0.72 μM. CYP1B1-IN-14 TFA reverses the resistance of cancer cells to Paclitaxel (HY-B0015). CYP1B1-IN-14 TFA acts synergistically with Paclitaxel (HY-B0015) to inhibit tumor growth in xenograft models without obvious toxicity. CYP1B1-IN-14 TFA can be used for the research of cancers such as paclitaxel-resistant lung cancer.

CYP11A1-IN-3 (Compound II-4) is a selective CYP11A1 inhibitor with an IC₅₀ of 26.7 nM. CYP11A1-IN-3 shows selectivity towards CYP1A2, 2C9 and 2D6. CYP11A1-IN-3 can be used for the research of castration-resistant prostate cancer.

Ticlopidine-d₆ hydrochloride is the deuterium labeled Ticlopidine hydrochloride. Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively.

PAIB-SOs-12 is a CYP1A1-activated antimitotic prodrug with affinity for human CYP1A1, with a K_i value of 1.2 μM. PAIB-SOs-12 exhibits nanomolar antiproliferative activity in cancer cells expressing CYP1A1, with a selectivity ratio of over 100 against cancer cells that do not express CYP1A1. PAIB-SOs-12 undergoes CYP1A1-mediated N-dealkylation to form the active metabolite PIB-SO, which induces G₂/M cell cycle arrest and microtubule disruption, and shows significantly improved stability in rodent liver microsomes compared to its n-butyl analog. PAIB-SOs-12 can be used in breast cancer-related research.

Paroxetine-d₂ (BRL29060-d₂) is the deuterated-labeled Paroxetine (HY-122272). Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.

ETX1975-3 is an orally active inhibitor and bactericide targeting the bd cytochrome oxidase of Mycobacterium tuberculosis. ETX1975-3 disrupts electron transfer between the b-heme centers of the target enzyme, and in combination with Q203 (HY-101040), exerts bactericidal activity against both replicating and non-replicating Mycobacterium tuberculosis, and reduces bacterial loads in acute mouse models. ETX1975-3 retains activity against clinical isolates of multidrug-resistant/extensively drug-resistant Mycobacterium tuberculosis and non-tuberculous mycobacteria, while possessing favorable preclinical ADMET properties. ETX1975-3 can be used in studies related to tuberculosis and non-tuberculous mycobacterial infections.

FGFR2/3-IN-3 is a dual-target FGFR2/3 inhibitor with IC₅₀s of 2.7 nM (TEL-FGFR2) and 3.9 nM (TEL-FGFR3), respectively. FGFR2/3-IN-3 has effective activity against both wild-type and mutant FGFR3. FGFR2/3-IN-3 has low CYP3A4 inhibitory effect and hERG toxicity. FGFR2/3-IN-3 improves the imbalance between chondrocyte proliferation and differentiation and promotes bone growth by inhibiting the signaling pathway mediated by mutant FGFR3. FGFR2/3-IN-3 shows a growth-promoting effect in a dwarfism mouse model and has the potential to study bone development disorder-related diseases such as achondroplasia (ACH).

Gestodene-d₇ (SHB 331-d₇; WL 70-d₇) is the deuterated-labeled Gestodene (HY-B0110). Gestodene is an orally active synthetic progestogen compound of the 19-nortestosterone class. Gestodene binds with high affinity to the progesterone receptor, inhibits 5α-reductase, binds to androgen and aldosterone receptors, and inactivates CYP3A. Gestodene acts as a positive allosteric modulator of PAR1, enhances PAR1-mediated signaling pathways, and is capable of increasing the activation potency of PAR1-AP toward PAR1, thereby promoting ERK1/2 phosphorylation, receptor internalization, cell morphological changes, and human platelet aggregation. Gestodene and its A-ring reduced metabolites promote the proliferation, differentiation, and mineralization of neonatal rat osteoblasts. Gestodene itself has no binding capacity for estrogen receptors, and this osteogenic activity depends on intracellular metabolism to generate A-ring reduced products with estrogen-like agonistic activity. Gestodene is useful for research on diseases related to progesterone secretion and diseases related to thrombosis.