Apoptosis Activator

TPP-C8-CO-DSG bromide is a derivative of Diosgenin (HY-N0177) and an anticancer agent. TPP-C8-CO-DSG bromide downregulates Bcl-2 expression and upregulates Bax expression. TPP-C8-CO-DSG bromide promotes the cleavage of Caspase 9, Caspase 3 and PARP-1. TPP-C8-CO-DSG bromide depolarizes mitochondrial membrane potential, reduces intracellular ATP production, and induces intracellular ROS accumulation. TPP-C8-CO-DSG bromide promotes Apoptosis. TPP-C8-CO-DSG bromide exhibits anticancer activity against prostate cancer, breast cancer, lung adenocarcinoma, cervical cancer and colorectal cancer. TPP-C8-CO-DSG bromide can be used in the research of cervical cancer.

Galarubicin hydrochloride (DA 125) is a novel Anthracycline derivative. Galarubicin hydrochloride shows high-affinity DNA binding and topoisomerase II inhibitory activities. Galarubicin hydrochloride induces Apoptosis. Galarubicin hydrochloride exerts cytotoxicity via JNK pathway. Galarubicin hydrochloride can be used in the research of hepatocellular carcinoma.

Estrogen receptor-IN-2 is a potent estrogen receptor inhibitor formed by the conjugation of Tam (HY-13757)-NHC and gold (I). Estrogen receptor-IN-2 significantly downregulates estrogen receptor (ER) levels, inhibits ER-mediated downstream signaling pathways, and induces immunogenic cell death (ICD) mediated by damage-associated molecular patterns (DAMPs). Estrogen receptor-IN-2 can overcome drug resistance in MCF-7^Y537S mutant cells via the RAMP3/CALCR signaling pathway. It is suitable for research on endocrine-resistant breast cancer.

Tubulin polymerization-IN-93 is a β-tubulin polymerization inhibitor. Tubulin polymerization-IN-93 disrupts the microtubule network structure. Tubulin polymerization-IN-93 activates the spindle assembly checkpoint and promotes Mitotic catastrophe. Tubulin polymerization-IN-93 activates the mitochondrial Apoptotic pathway. Tubulin polymerization-IN-93 exhibits anticancer activity against acute myeloid leukemia.

EGFR AUTOTAC-1 is a p62/SQSTM1-directed EGFR AUTOTAC degrader. EGFR AUTOTAC-1 recruits p62 to form a ternary complex, activates the ubiquitin-proteasome system-independent Atg5-dependent autophagy-lysosome pathway, mediates autophagic degradation of EGFR and inhibits the AKT/ERK signaling pathway, thereby promoting apoptosis and activating autophagy. EGFR AUTOTAC-1 can be used for the research of non-small cell lung cancer.(Pink: EGFR ligand (HY-79511); Blue: p62 ligand (HY-187557); Black: Linker)

Tolinapant dihydrochloride (ASTX660 dihydrochloride) is an orally active cIAP1/2 and XIAP antagonist, with an IC₅₀ of < 40 nM against XIAP and an IC₅₀ of <12 nM against cIAP1. Tolinapant dihydrochloride triggers TNFα-dependent Apoptosis in cancer cells. Tolinapant dihydrochloride inhibits tumor growth in mouse xenograft models. Tolinapant dihydrochloride can be used in research related to breast cancer, melanoma, lymphoma, multiple myeloma, acute lymphoblastic leukemia and advanced solid tumors.

NSD-IN-4 (Compound A8) is a potent and an orally active NSD3 inhibitor. NSD-IN-4 induces Apoptosis in a dose-dependent manner. NSD-IN-4 exhibits significant antitumor effects against lung squamous carcinoma.

Lovastatin hydroxy acid (sodium) (Standard) is the analytical standard of Lovastatin hydroxy acid (sodium). This product is intended for research and analytical applications. Lovastatin hydroxy acid sodium (Mevinolinic acid sodium) is a highly potent inhibitor of HMG-CoA reductase with a Ki of 0.6 nM.

Hellebrin is a bufadienolide compound extracted from plants that can inhibit tumor cell growth. Hellebrigenin shows potential in overcoming cancer cells' resistance to apoptosis stimuli and has also demonstrated anti-proliferation effects in multidrug-resistant (MDR) cancer cell models. Hellebrin can act on Na+/K+-ATPase to regulate intracellular signaling pathways.

CDK4/6/HDAC-IN-1 (Compound N14) is a dual-targeting inhibitor of CDK4/6 and HDAC (IC₅₀: CDK4 = 7.23 nM, CDK6 = 13.20 nM, HDAC1 = 55.66 nM, HDAC6 = 48.38 nM). CDK4/6/HDAC-IN-1 induces cell Apoptosis and G0/G1 phase arrest through HDAC-p21-CDK signaling pathway. CDK4/6/HDAC-IN-1 inhibits hepatocellular carcinoma.

CCI-007 is a small molecule with cytotoxic activity against infant leukemia with MLL rearrangements, with IC₅₀ values of 2.5-6.2 μM in sensitive cells.

ALK degrader 1 is a potent, hydrophobic tag (HyT)-based degrader that induces ubiquitin-proteasome system (UPS)-dependent EML4-ALK degradation (DC₅₀ = 0.13 μM). ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research.

Sino-C is a Sinomenine (HY-15122) derivative with anticancer activity. Sino-C broadly disrupts cholesterol homeostasis by upregulating key genes such as SREBF2 and HMGCS1, leading to intracellular cholesterol accumulation and lipid droplet formation. Sino-C-induced metabolic dysregulation further triggers lipid peroxidation and endoplasmic reticulum (ER) stress, initiating a unique form of hybrid cell death including apoptotic (cleaved PARP) and necrotic-like features. Sino-C thus serves as a useful compound for research in colorectal cancer, lung cancer and breast cancer.

TrxR1-IN-3 is a selective TrxR1 inhibitor with an IC₅₀ of 1.19 μM. TrxR1-IN-3 increases intracellular reactive oxygen species (ROS) levels, induces endoplasmic reticulum (ER) stress, and activates Caspase-dependent Apoptosis. TrxR1-IN-3 exhibits anticancer activity against multiple breast cancer subtypes, including triple-negative breast cancer (TNBC). TrxR1-IN-3 can be used in breast cancer-related research.

d-T101 peptide, a human hormone-peptide, is a T1/ST2 receptor ligand. d-T101 peptide binds to the T1/ST2 receptor and activates caspases 8, 9 and 3 mediated apoptosis, together with activation of JNKinase and p38 MAPKinase. d-T101 peptide also changes Golgi structural with function loss and downregulation of the endoplasmic reticulum (ER) stress repair mechanism. d-T101 peptide has immunostimulatory and anticancer activity, selectively induces apoptosis in proliferating cancer cells and increases IL-2 and IFN-γ expression as well as the recruitment of NK cells and M1 macrophages to the tumor site.

BPTQ is a potent inhibitor against VEGFR1 and CHK2 with IC₅₀ values of 0.54 and 1.70 µmol/L, respectively. BPTQ is also an intercalator of DNA with anticancer activities. BPTQ inhibits the proliferation of HL-60 cells by arresting cells at S and G2/M phase with an IC₅₀ value of 12 µmol/L. BPTQ also activates the mitochondria-mediated Apoptosis pathway by a decrease in mitochondrial membrane potential, increase in the Bax:Bcl-2 ratio and activation of caspases.

TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC₅₀ of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo.

Hydrolyzed Fumonisin B1 (Aminopentol) is the backbone and main hydrolysis product of the mycotoxin Fumonisin B1 (HY-N6719). Hydrolyzed Fumonisin B1 can weakly inhibit ceramide synthase.

SKF-83566 hydrochloride is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a K_i value of approximately 0.4-0.56 nM. SKF-83566 hydrochloride modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway. SKF-83566 hydrochloride acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2). SKF-83566 hydrochloride competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation. SKF-83566 hydrochloride is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect").

Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice.