Apoptosis Activator

Sitamaquine (WR 6026) is an orally active Antileishmanial agent and Succinate dehydrogenase inhibitor. Sitamaquine accumulates in the acidocalcisomes of Leishmania, induces organelle alkalization, and crosses the plasma membrane of Leishmania via temperature- and energy-independent diffusion. Sitamaquine disrupts oxidative phosphorylation in Leishmania, induces mitochondrial depolarization, oxidative stress, elevated intracellular calcium, plasma membrane depolarization, and Apoptosis-like cell death. Sitamaquine can be used in the research of leishmaniasis.

1,2-DLPC (Standard) is the analytical standard of 1,2-DLPC (HY-107737). This product is intended for research and analytical applications. 1,2-DLPC (1,2-Dilauroyl-sn-glycero-3-phosphocholine) is a ligand for LRH-1 agonists. 1,2-DLPC is a phospholipid used in the synthesis of liposomes. 1,2-DLPC enhances fat breaK_down and apoptosis in fat cells through a TNFα-dependent pathway, while also inhibiting palmitate-induced insulin resistance through PPARα-mediated inflammation in muscle cells.

Izorlisib (CH5132799) methanesulfonate is an orally active, selective Class I PI3K inhibitor with an IC₅₀ value of 14 nM against PI3Kα. Izorlisib methanesulfonate specifically inhibits Class I PI3K (particularly PI3Kα and its mutants) and blocks the PI3K/Akt/mTOR pathway; this leads to cell cycle arrest at the G1 phase and apoptosis without triggering feedback activation of Akt by competitively binding to the ATP-binding site of PI3K. Izorlisib methanesulfonate can be used in research on cancers harboring PIK3CA mutations or PTEN loss (such as breast, ovarian, prostate, and endometrial cancers).

ML385 (Standard) is the analytical standard of ML385 (HY-100523). This product is intended for research and analytical applications. ML385 is a potent and selective Nrf2 inhibitor with an IC₅₀ of 1.9 μM. ML385 directly binds to the Neh1 domain of NRF2, interferes with the binding of the MAFG-NRF2 protein complex to the antioxidant response element (ARE) DNA sequence, thereby blocking the expression of downstream target genes of NRF2. ML385 can be used in studies related to adult T-cell leukemia, breast cancer, myocardial ischemia/reperfusion injury, non-small cell lung cancer, esophageal squamous cell carcinoma, head and neck squamous cell carcinoma, and lung squamous cell carcinoma.

3-AP-Me is a dimethyl derivative of the nucleotide reductase inhibitor 3-AP (SML0568). 3-AP-Me can activate the endoplasmic reticulum (ER) stress pathway by promoting the phosphorylation of eIF2α and increasing the gene expression of transcription factors ATF4 and ATF6, leading to cell apoptosis. Additionally, 3-AP-Me can activate the stress kinases c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinases. 3-AP-Me also leads to the upregulation of the spliced mRNA variant XBP1, can be used in cancer research.

N6-Cyclopentyladenosine (Standard) is the analytical standard of N6-Cyclopentyladenosine (HY-103181). This product is intended for research and analytical applications. N6-Cyclopentyladenosine (CPA) is a selective Adenosine A1 receptor agonist, with K_i values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively. N6-cyclopentyladenosine increases Apoptosis. N6-Cyclopentyladenosine has antitumor activity against leukemia. N6-cyclopentyladenosine improves 5-fluorouracil (HY-90006)-induced hematopoietic damage, regulates sleep, and delays Aminophylline-induced clonic epileptic seizures.

Fludioxonil-¹³C₃ (CGA-173506-¹³C₃) is ¹³C labeled Fludioxonil. Fludioxonil (CGA-173506) is a phenylpyrrole-type fungicide with oral activity that can inhibit the growth of S. sclerotiorum. Fludioxonil promotes tumor growth and metastasis, and induces cardiac toxicity. Fludioxonil causes cytoskeletal disruption, DNA damage, and apoptosis in mouse glioma cells.

Simmitecan is a potent topoisomerase I (TOP1) inhibitor, which is a 9-substituted lipophilic camptothecin (Camptothecin (HY-16560)) derivative. Simmitecan blocks DNA replication and transcription, thereby inducing tumor cell apoptosis by inhibiting the activity of TOP1. Simmitecan can be used in the research of cancers such as liver cancer.

3-Methylxanthine-d₃ is deuterated labeled 3-Methylxanthine (HY-50723). 3-Methylxanthine is a blood-brain barrier-permeable cyclic GMP phosphodiesterase inhibitor, with an IC₅₀ of 920 μM against guinea pig cyclic GMP phosphodiesterase. 3-Methylxanthine relaxes the spontaneous tension of isolated guinea pig tracheal smooth muscle preparations. Through a DRD1-dependent pathway, 3-Methylxanthine upregulates the expression of γH2AX and activated caspase-3, downregulates the expression of Bcl-2, and enhances Cisplatin-induced apoptosis (apoptosis) in ovarian cancer cells both in vitro and in vivo. 3-Methylxanthine induces clonic convulsions in the central nervous system. 3-Methylxanthine is the major metabolite of Theophylline (HY-B0809). 3-Methylxanthine can be used in studies related to ovarian cancer and neurotoxic convulsions.

IG-105 is an orally active and potent tubulin inhibitor that competitively inhibits [³H] colchicine binding to tubulin with an IC₅₀ of 0.6 μM and inhibits tubulin polymerization with an IC₅₀ of 3 μM. IG-105 inhibits microtubule polymerization by binding to the colchicine pocket of tubulin, induces G2-M phase arrest, and subsequently activates the caspase cascade through Bcl-2 inactivation and p53 upregulation, inducing apoptosis. IG-105 effectively overcomes multidrug resistance as a non-Pgp substrate. IG-105 can be used for research on leukemia, breast cancer, liver cancer, prostate cancer, lung cancer, melanoma, pancreatic cancer, and colon cancer.

Alternariol-d₂ is deuterium labeled Alternariol. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects.

AB8939 is an effective small moleculeMicrotubule/Tubulin polymerization inhibitor with anti-tumor activity (it inhibits tumor cell proliferation with an IC₅₀ of less than 10 nM). AB8939 can effectively evade resistance mechanisms mediated by things like P-glycoprotein and myeloperoxidase. AB8939 can induce G2/M phase cell cycle arrest and apoptosis in cells.

Erioflorin is a sesquiterpene lactone compound originally isolated from plants of the Asteraceae family (such as Eriophyllum confertiflorum and species of the Podanthus genus). Erioflorin acts as a selective β-TrCP1 modulator. Erioflorin induces cell apoptosis by increasing intracellular reactive oxygen species (ROS) production and decreasing mitochondrial membrane potential, inhibits the NF-κB signaling pathway by blocking the phosphorylation of IκBα, and prevents the ubiquitination and degradation of the tumor suppressor Pdcd4 by inhibiting the interaction between Pdcd4 and the E3 ubiquitin ligase β-TrCP1. Erioflorin can be used in research related to breast cancer, colon cancer, advanced prostate cancer, and Chagas disease.

VJ115 is a potent ENOX1 inhibitor with an EC₅₀ of 50 μM. By inhibiting ENOX1, VJ115 elevates NADH, which in turn downregulates the phosphorylation of p70S6K1/S6, alters the expression of c-Jun and cytoskeletal proteins, induces endothelial cells to lose polarization and migration ability, and increases caspase-3-dependent apoptosis under radiation. VJ115 can be used in studies related to solid tumors.

HX531 (Standard) is the analytical standard of HX531 (HY-108521). This product is intended for research and analytical applications. HX531 is an orally active RXR antagonist with an IC₅₀ of 18 nM. HX531 upregulates the p53-p21Cip1 pathway. HX531 abrogates the anti-apoptotic effect of t-RA. HX531 exerts anti-obesity, anti-diabetic and anti-melanoma activities.

CX-5461 (Standard) is the analytical standard of CX-5461 (HY-13323). This product is intended for research and analytical applications. CX-5461 is a selective, orally active RNA polymerase I inhibitor. CX-5461 disrupts the formation of the SL1-rDNA complex, thereby blocking the transcription initiation of ribosomal RNA without altering the activity of RNA polymerase II, DNA replication, or protein translation processes. CX-5461 upregulates the expression of p21, MDM2, Sestrin1/2, and phosphorylated AMPKα, and reduces the level of phosphorylated Akt. CX-5461 induces G2/G2/M cell cycle arrest, Autophagy, Apoptosis, and cellular senescence, and activates CHK1, CHK2, and RPA. CX-5461 can be used in research related to osteosarcoma, cervical cancer, hematologic malignancies, high-grade serous ovarian cancer, and solid tumors.

Aceanthrenequinone is a polycyclic aromatic hydrocarbon quinone organic compound that belongs to the category of free radical photoinitiators. Aceanthrenequinone serves as an intermediate for dyes and pigments, and also acts as a substrate for organic synthesis and polymer materials. Aceanthrenequinone activates the Aryl Hydrocarbon Receptor pathway, induces the expression of CYP1A protein in the vascular system of zebrafish embryos, and causes the death of embryos at 120 hpf. Aceanthrenequinone is applicable to research related to industrial or biomedical applications.

BV02 (Standard) is the analytical standard of BV02 (HY-101985). This product is intended for research and analytical applications. BV02 is a 14-3-3 inhibitor and an antibacterial agent. BV02 enhances the cleavage of PARP and caspase-3. BV02 induces Apoptosis, Autophagy, and enhances Akt activation. BV02 has anti-B. melitensis infection and epilepsy-promoting effects. BV02 can also be used in colitis research.

Tamsulosin (hydrochloride) (Standard) is the analytical standard of Tamsulosin hydrochloride (HY-B0661A). Tamsulosin hydrochloride ((R)-(-)-YM12617 free base) is an orally active antagonist of α₁-adrenergic receptor. Tamsulosin hydrochloride induces Apoptosis. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models.

Imifoplatin (Standard) is the analytical standard of Imifoplatin (HY-109146). This product is intended for research and analytical applications. Imifoplatin (PT-112) is a platinum-based active molecule and a member of the phosphaplatins family. Imifoplatin can induce Apoptosis and exhibits antitumor activity.