Apoptosis Inducer

CAY10404 (Standard) is the analytical standard of CAY10404. This product is intended for research and analytical applications. CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities.

Apitolisib (Standard) is the analytical standard of Apitolisib. This product is intended for research and analytical applications. Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.

Oxatomide (Standard) (KW-4354 (Standard)) is the analytical standard of Oxatomide (HY-123205). This product is intended for research and analytical applications. Oxatomide (KW-4354) is an orally active dual antagonist of the H1-histamine receptor and the P2X7 receptor, as well as an inhibitor of serotonin. Oxatomide possesses antihistaminic, antiallergic and anti-inflammatory activities. Oxatomide can be used in the research of allergic diseases.

D-Cl-amidine (hydrochloride) (Standard) is the analytical standard of D-Cl-amidine (hydrochloride) (HY-100574D). This product is intended for research and analytical applications. D-Cl-amidine hydrochloride is a potent and highly selective PAD1 inhibitor. D-Cl-amidine is well-torelated with no significant toxicity.

Alisertib (Standard) is the analytical standard of Alisertib. This product is intended for research and analytical applications. Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.

R547 mesylate is a potent, selective and orally active ATP-competitive CDK inhibitor, with K_is of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.

KYP-2047 (Standard) is the analytical standard of KYP-2047 (HY-100475). This product is intended for research and analytical applications. KYP-2047 is a potent and BBB-penetrating prolyl-oligopeptidase (POP) inhibitor, with an Ki value of 0.023 nM. KYP-2047 reduces glioblastoma proliferation through angiogenesis and apoptosis modulation.

Pranoprofen (Standard) is the analytical standard of Pranoprofen. This product is intended for research and analytical applications. Pranoprofen is a non-steroidal anti-inflammatory agent (NSAID) for the research of keratitis or other ophthalmology diseases. Pranoprofen inhibit COX-1 and COX-2 enzymes, thus blocking arachidonic acid converted to eicosanoids and reducing prostaglandins synthesis.

TP-472 (Standard) is the analytical standard of TP-472 (HY-100517). This product is intended for research and analytical applications. TP-472, a chemical probe, is a selective BRD9/7 inhibitor, with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7. TP-472 induces apoptosis of melanoma cells.

Hydroxymethyl dasatinib (M24), a benzylhydroxy metabolite of Dasatinib (HY-10181), exhibits an IC₅₀ of 46.7nM in K562 CML cells.

Nutlin-3a (Standard) is the analytical standard of Nutlin-3a (HY-10029). This product is intended for research and analytical applications. Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas.

Elrelesertib (Standard) (AZD1390 (Standard)) is the analytical standard of Elrelesertib (AZD1390) (HY-109566). This product is intended for research and analytical applications. Elrelesertib (AZD1390) is an orally active, brain-penetrant ATM kinase inhibitor with IC₅₀ values of 0.78 nM. Elrelesertib blocks ATM-dependent DNA damage response, inhibits ATM autophosphorylation and downstream Chk2, Rad50 phosphorylation, and accumulates at DNA breaks. Elrelesertib acts as a radiosensitizer, induces apoptosis, genomic instability, G2-M cell cycle arrest, ROS elevation, and mitochondrial membrane potential alteration. Elrelesertib has low efflux liability against P-gp and BCRP. Elrelesertib can be used for the research of central nervous system malignancies, glioblastoma multiforme, glioma, lung cancer brain metastases, and breast cancer.

Ibulocydine is an isobutyrate prodrug of the Cdk inhibitor BMK-Y101 (HY-188159), with oral activity, and exhibits IC₅₀ values of approximately 50 nM against CDK1/CDK2, 530 nM against CDK7/cyclin H/Mat1, and 85 nM against CDK9/cyclin T. Ibulocydine reduces the phosphorylation levels of Rb, nucleolin, and RNA polymerase II CTD Ser-5 and Ser-2, downregulates the expression of Mcl-1, survivin, and XIAP, decreases MMP-9 expression, and lowers the Bcl-2/Bax ratio, activates calpain-mediated Bax cleavage, cytochrome c release, and caspase activation. Ibulocydine induces apoptosis, inhibits the growth of cancer cells and xenografts, enhances the sensitivity of cancer cells to TRAIL and radiotherapy, and blocks cancer cell metastasis. Ibulocydine can be used in research related to various cancers, including hepatocellular carcinoma, triple-negative breast cancer, lung cancer, and colon cancer.

GL-331 is a potent anti-cancer agent. GL-331 has demonstrated more efficacious anti-cancer activity in both the in vitro and in vivo lymphoma systems.

Glucobrassicin is an indole-based anticancer agent and plant growth-regulating hormone. Glucobrassicin exerts its biological activity by disrupting the integrity of microtubule networks in both plant and mammalian cells. At high concentrations, Glucobrassicin inhibits seed germination and root growth; it can also specifically induce apoptosis in mammalian cancer cells and interfere with the intercellular transmission of viruses that rely on microtubules. In plants, Glucobrassicin can be catalyzed by myrosinase to release growth-regulating substances, exhibiting a concentration-dependent growth-regulating effect.

PF-573228 (Standard) is the analytical standard of PF-573228. This product is intended for research and analytical applications. PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK.

MPT0B214 is a microtubule inhibitor that strongly binds to the colchicine binding site of tubulin, preventing tubulin polymerization. MPT0B214 induces apoptosis through a mitochondrial/caspase 9 dependent pathway and shows cytotoxicity across various human tumor cell lines. MPT0B214 can be used for cancer research.

KX2-361 (Standard) is the analytical standard of KX2-361 (HY-111187). This product is intended for research and analytical applications. KX2-361 (KX-02) is a Src-K_inase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell.

AT9283 (Standard) is the analytical standard of AT9283. This product is intended for research and analytical applications. AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.

Prednisone-¹³C₂,d₂ (Dehydrocortisone-¹³C₂,d₂) is ¹³C labeled Prednisone. Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus.