Apoptosis Inducer

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.

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.

Glutathione maleimide (GS-Mal) is a glutathione depletor and oxidative stress inducer that reduces intracellular GSH levels in cancer cells and induces apoptosis. Glutathione maleimide can selectively extract and quantify GSH from complex biological samples, and the polymeric micelles prepared from it also inhibit the growth of cancer cells in a concentration-dependent manner. Glutathione maleimide has broad applications in breast cancer and related fields.

ZINC69391 (Standard) is the analytical standard of ZINC69391 (HY-102078). This product is intended for research and analytical applications. ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects.

Ertabresib (Standard) (INCB-057643 (Standard)) is the analytical standard of Ertabresib (HY-111485). This product is intended for research and analytical applications. Ertabresib (INCB-057643) is an orally active BET protein inhibitor. Ertabresib blocks gene transcription by targeting the BET protein family, induces cell cycle arrest and apoptosis by downregulating proto-oncogenes such as c-MYC, and additionally reduces the expression of FOXP3 and PD-L1 to improve the immune microenvironment. It also exerts synergistic effects and overcomes drug resistance when combined with chemotherapy and XPO1 inhibitors. Ertabresib can be used in research related to high-grade B-cell lymphoma with MYC and BCL2 rearrangements, pancreatic cancer, pancreatitis, and metastatic castration-resistant prostate cancer.

Survivin-IN-1 (Compound II₃) is a potent Survivin (a member of the Inhibitor of Apoptosis Protein family) inhibitor with an IC₅₀ value of 8.1 μM against human lung cancer A549 cells and 9.0 μM against breast cancer MCF-7 cells. Survivin-IN-1 reduces Survivin protein levels and induces tumor cell apoptosis. Survivin-IN-1 is promising for research of malignant tumors such as lung cancer and breast cancer.

PS-1145 (Standard) is the analytical standard of PS-1145. This product is intended for research and analytical applications. PS-1145 is an IκB kinase (IKK) inhibitor with an IC50 of 88 nM.

Ramentaceone (7-Methyljuglon), a naphthoquinone that can be isolated from Drosera sp., inhibits PI3K activity. Ramentaceone (7-Methyljuglon) reduces the expression of the PI3K protein and inhibits the phosphorylation of the Akt protein in breast cancer cells. Ramentaceone (7-Methyljuglon) induces apoptosis.

VAS 3947 (Standard) is the analytical standard of VAS 3947 (HY-111447). This product is intended for research and analytical applications. VAS 3947, a specific NADPH oxidase (NOX) inhibitor, exerts a potent antiplatelet effect. VAS3947 induces apoptosis independently of anti-NOX activity, via UPR activation, mainly due to aggregation and misfolding of proteins.

LYN-1604 dihydrochloride (Standard) is the analytical standard of LYN-1604 dihydrochloride (HY-101923B). This product is intended for research and analytical applications. LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC₅₀=18.94 nM) for the research of triple negative breast cancer (TNBC).

PETCM (Standard) is the analytical standard of PETCM (HY-103349). This product is intended for research and analytical applications. PETCM is an activator of caspase-3 and acts as an cytochrome c (cyto c)-dependent manner. PETCM promotes Apaf-1 oligomerization and induces cell apoptosis in HeLa cells.

GW 5074 (Standard) is the analytical standard of GW 5074 (HY-10542). This product is intended for research and analytical applications. GW 5074 is a potent and selective c-Raf inhibitor with IC₅₀ of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms.