Pyroptosis Inducer

Prosapogenin A (Standard) is the analytical standard of Prosapogenin A. This product is intended for research and analytical applications. Prosapogenin A, a natural product from Veratrum, induces apoptosis in human cancer cells in vitro via inhibition of the STAT3 signaling pathway and glycolysis.

PARP1/EZH2-IN-1 is a selective PARP1 and EZH2 dual inhibitor. PARP1/EZH2-IN-1 has IC₅₀s of 28 nM, 414 nM and 74 nM for PARP1, PARP2 and EZH2, respectively. PARP1/EZH2-IN-1 inhibits the proliferation and migration of TNBC cells (triple-negative breast Cancer cells). PARP1/EZH2-IN-1 induces PANoptosis (Apoptosis, Pyroptosis and Necroptosis), increases the level of reactive oxygen species (ROS), and activates related inflammatory pathways. PARP1/EZH2-IN-1 can be used in triple-negative breast cancer research.

WYJ-2 is a selective agonist for toll-like receptor 2/1 (TLR2/1) with EC₅₀ of 18.57 nM in human TLR2 and TLR1 transient-cotransfected HEK 293T cells. WYJ-2 induces pyroptosis and exhibits anticancer activity against non-small cell lung cancer (NSCLC).

TNI-97 is a selective and orally active HDAC6 inhibitor, with an IC₅₀ of 0.2 nM. TNI-97 potently inhibited TNBC cell MDA-MB-453 growth and clonogenicity. TNI-97 induces PANoptosis including apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells. TNI-97 shows antitumor activity in the mice carrying the MDA-MB-453 xenograft or carrying murine-derived TNBC cell allografts. TNI-97 can be used for the study of triple-negative breast cancer.

Spiroplatin is a Cisplatin (HY-17394) congener and has antitumor activity.

Clemastine (HS-592; Meclastine) fumarate (Standard) is the analytical standard of Clemastine fumarate. This product is intended for research and analytical applications. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .

DdBIC is a pyroptosis inducer. DdBIC binds to Nur77 and triggers its translocation to mitochondria, activates SDHA to deplete succinyl-CoA, disrupts heme homeostasis, induces electron leakage, and elicits mitochondrial ROS production. DdBIC induces mitochondrial ROS that oxidatively activates OMA1, promotes OPA1 cleavage and its release into the cytoplasm, activates the integrated stress response via PERK, and ultimately activates granzyme B to cleave GSDMC. DdBIC can be used for the study of melanoma.

TRBP-IN-1 (Compound 13j) is an orally active TAR RNA binding protein 2 (TRBP) inhibitor (IC₅₀: 12.72 μM). TRBP-IN-1 has significant anti-hepatocellular carcinoma (HCC) activity and can inhibit the proliferation and metastasis of HCC cells (HCCLM3 cells (IC₅₀: 18.96 μM); SK-Hep-1 cells (IC₅₀: 16.45 μM)). TRBP-IN-1 regulates miRNA biogenesis and inhibits oncogenic miRNA expression by targeting TRBP. TRBP-IN-1 induces apoptosis and pyroptosis in HCC cells by inhibiting the level of miRNA. TRBP-IN-1 can be used for targeted therapy research of HCC.

JLJ648 is a Gag-Pol dimerizer with antiviral activity. JLJ648 can inhibit HIV replication and induce infected cell pyroptosis. JLJ648 can be used for the research of infection, such as HIV (human immunodeficiency virus).

4,4′-Secalonic acid D (Compound 12) is a PARP1 inhibitor. 4,4′-Secalonic acid D induces the accumulation of ROS and DNA damage, activates the caspase-3/GSDME pathway, and triggers apoptosis and pyroptosis of tumor cells by inhibiting PARP1. 4,4′-Secalonic acid D has anti-tumor activity.

Ac-DEVDD-TPP is a porphyrin derivative that can be converted into D-TPP by caspase-3 cleavage and laser irradiation. The formed porphyrin nanofibers can effectively induce Apoptosis and Pyroptosis. Ac-DEVDD-TPP has antitumor activity.

HDAC1/6-IN-3 is a potent HDAC inhibitor. HDAC1/6-IN-3 shows excellent inhibitory activities against HDAC1 (IC₅₀ = 1.1 nM) and HDAC6 (IC₅₀ = 2.7 nM). HDAC1/6-IN-3 significantly arrests HepG2 cells at the G0/G1 phase and induces apoptosis and pyroptosis. HDAC1/6-IN-3 exhibits significant antitumor activity in the HepG2 xenograft mode. HDAC1/6-IN-3 can be used for the study of cancers such as liver cancer, lung cancer, colon cancer and breast cancer.

BTK-IN-15 (compound 42) is a potent Bruton's tyrosine kinase (BTK) inhibitor with high oral absorption. BTK-IN-15 inhibits BTK with an IC₅₀ value of 0.7 nM. BTK-IN-15 displays excellent kinase selectivity, antitumor activity, and induces apoptosis.

Apoptosis inducer 36 (Compound 42) exhibits anti-leukemic activity through reduction of leukemia stem cells (LSCs) and induction of differentiation. Apoptosis inducer 36 inhibits the proliferation of AML cells, arrests cell cycle at G1 phase, and induces PANoptosis including apoptosis, pyroptosis and necrosis. Prodrug of apoptosis inducer 36 exhibits orally active antitumor efficacy in mouse model.

YTB53 is a MNK1 and MNK2 inhibitor with IC₅₀s of 37 nM and 9 nM, respectively. YTB53 inhibits PDGFRα, TRKB and FLT3 in leukemia cells. YTB53 induces cell cycle arrest, apoptosis, pyroptosis, and mitochondrial dysfunction. YTB53 exhibits antiangiogenic effects. YTB53 can be used for the study of acute myeloid leukemia (AML).

Nigericin (sodium salt) (Standard) is the analytical standard of Nigericin (sodium salt). This product is intended for research and analytical applications. Nigericin sodium salt is an antibiotic derived from Streptomyces hygroscopicus that act as a K⁺/H⁺ ionophore, promoting K⁺/H⁺ exchange across mitochondrial membranes. Nigericin sodium salt is a NLRP3 activator. Nigericin sodium salt shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin sodium salt induces pyroptosis through caspase 1/GSDMD in TNBC.

NLRP3-IN-81 (N102) is a BBB-penetrable inhibitor against NLRP3 inflammasome-dependent pyroptosis with an EC₅₀ of 0.029 μM against cell pyroptosis induced by Nigericin (HY-127019). NLRP3-IN-81 potently inhibits NLRP3-dependent activation of caspase-1 and the release of IL-1β. NLRP3-IN-81 disturbs the interaction of NLRP3 with the adaptor protein ASC and inhibits ASC oligomerization. NLRP3-IN-81 can be used for pyroptosis-related diseases research, such as inflammatory bowel diseases and type 2 diabetes.

ICy-OH, an iodinated photosensitizer, is an effective anticancer agent. ICy-OH can be used not only for deep tissue imaging (λ_ex=640 nm，λ_em=690-740 nm) but also to selectively induce cell death in pancreatic cancer cells via cell pyroptosis pathway.

ICy-Q is a quinone oxidoreductase 1 (NQO-1)-activated near-infrared (NIR) reagent which can react with NQO-1 to release the reduction product ICy-OH. ICy-OH selectively induces pancreatic cancer cell death through the pyroptosis pathway. ICy-Q can be used as an effective tool for rapid and accurate diagnosis of intraoperative pathological sections.

BTF-DNBS is a glutathione (GSH)-responsive small-molecule photosensitizer (PS). BTF-DNBS disrupts mitochondrial function and triggers Golgi-mediated pyroptosis, serving as a reactive oxygen species (ROS) generator. BTF-DNBS is promising for research of cancers.