Apoptosis Activator

RUNX1/ETO-IN-1 is a RUNX1-ETO oncogenic fusion protein inhibitor that specifically targets the NHR2 oligomerization domain. RUNX1/ETO-IN-1 directly interacts with the NHR2 (K_D,app = 39 μM). RUNX1/ETO-IN-1 exhibits anti-leukemic activity by inducing apoptosis and promoting differentiation in RUNX1/ETO-translocated AML cells. RUNX1/ETO-IN-1 remains essentially uncharged at physiological pH, demonstrating superior membrane permeability.

Rocaglaol induces apoptosis and cell cycle arrest in LNCaP cells.

Taurodeoxycholate sodium salt (Standard) is a bile salt (Standard)-related anionic detergent. Taurodeoxycholate sodium salt (Standard) is formed in the liver by conjugation of deoxycholate with Taurine (HY-B0351). Taurodeoxycholate sodium salt (Standard) is used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholate (TDCA) exhibits anti-inflammatory and neuroprotective effects.

MY-943 is a potent tubulin polymerization and LSD1 inhibitor with anticancer activity. MY-943 induces G2/M phase arrest and apoptosis, and inhibits cell migration. MY-943 can be used for gastric cancer research.

Bax activator-1 (compound 106) is a Bax activator that induces Bax-dependent tumor cell apoptosis.

Rotundifuran, a labdane type diterpene, is isolated from Vitex rotundifolia. Rotundifuran can inhibit the cell cycle progression and induce apoptosis in human myeloid leukaemia cells.

Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells.

K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC₅₀ of 4.3 µM and a K_i of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity.

BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a K_i of 7.5 nM and an IC₅₀ of 10 nM. BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.

YH239-EE, ethyl ester of the free carboxylic acid compound YH239, is a potent p53-MDM2 antagonizing and apoptosis-inducing agent.

Uridine 5'-monophosphate-¹⁵N₂ (5'-​Uridylic acid-¹⁵N₂) is the ¹⁵N labeled Uridine 5'-monophosphate (HY-101981). Uridine 5'-monophosphate (5'-Uridylic acid) is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea.

Dibromoacetic acid, a haloacetic acid found in drinking water as a disinfection by-product, can cause many adverse effects, including immunotoxicity and apoptosis.

FF2049 is a selective HDAC1-3 PROTAC degrader (with a DC₅₀ of 257 nM against HDAC1). FF2049 recruits the E3 ligase FEM1B to mediate ubiquitination and proteasomal degradation of HDAC1-3. FF2049 induces cell cycle arrest and Apoptosis in cells. FF2049 can be used in research related to multiple myeloma, acute monocytic leukemia, triple-negative breast cancer and glioblastoma.

PM534 is a potent tubulin inhibitor (K_D = 20 nM). PM534 targets and binds to the entire colchicine-binding domain (CBD) of tubulin, thereby inhibiting tubulin assembly; this leads to cell cycle arrest at the G2-M phase and induces multinucleation and apoptosis. PM534 exhibits microtubule-destabilizing agent (MDA) activity, potent broad-spectrum antitumor activity, and anti-angiogenic effects. PM534 can be used in research concerning human non-small cell lung cancer (NSCLC), breast cancer, ovarian cancer, and prostate cancer.

ZS3-046 is a potent TAF1 PROTAC degrader with a DC₅₀ < 10 nM. ZS3-046 recruits the CRBN E3 ubiquitin ligase, promotes polyubiquitination and proteasomal degradation of TAF1, thereby activating p53 and downregulating c-Myc, and ultimately induces apoptosis of tumor cells. ZS3-046 can be used in research related to acute myeloid leukemia.

AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.

TL02-59 dihydrochloride is an orally active, selective Src-family kinase Fgr inhibitor with an IC₅₀ of 0.03 nM. TL02-59 dihydrochloride inhibits Lyn and Hck with IC₅₀s of 0.1 nM and 160 nM, respectively. TL02-59 dihydrochloride potently suppresses acute myelogenous leukemia (AML) cell growth.

SS28, a SRT501 analog with oral bioavailability, inhibits tubulin polymerization to cause cell cycle arrest at G2/M phase. SS28 results in apoptosis rather than necrosis tubulin.

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

Brusatol (Standard) is the analytical standard of Brusatol (HY-19543). This product is intended for research and analytical applications. Brusatol (NSC 172924) is a unique inhibitor of the Nrf2 pathway that sensitizes a broad spectrum of cancer cells to Cisplatin and other chemotherapeutic agents. Brusatol enhances the efficacy of chemotherapy by inhibiting the Nrf2-mediated defense mechanism. Brusatol can be developed into an adjuvant chemotherapeutic agent. Brusatol increases cellular apoptosis.