Caspase Activator

HDAC-IN-82 (Compound 18b) is a histone deacetylase (HDAC) inhibitor with selective antiplasmodial and anticancer activity. HDAC-IN-82 shows potent antiproliferative activity and caspase 3/7 activation in cancer cells. HDAC-IN-82 causes hyperacetylation of histone H3 and α-tubulin.

Nivitol (UP302) is a natural phenolic compound discovered from Dianella ensifolia and also acts as a Tyrosinase inhibitor. Nivitol competitively and reversibly inhibits tyrosinase, suppressing melanin production. Nivitol inhibits homogentisate 1,2-dioxygenase (HGD). In human leukemia cells, Nivitol inhibits PI3K/AKT pathway phosphorylation, increases ROS, decreases mitochondrial membrane potential, and induces G2/M cell cycle arrest, apoptosis, and PINK1/Parkin-mediated mitophagy. Nivitol exhibits inhibition of tumor growth in the MV411 xenograft mouse model. Nivitol is used for research on exogenous ochronosis, hyperpigmentation, and leukemia.

NCP26 is an ATP-competitive ProRS inhibitor (with a K_D of 271 nM in the absence of proline, and a K_D of 0.35 nM in the presence of 100 μM proline). NCP26 activates AAR, induces G0/G1 phase arrest, Apoptosis, Caspase cleavage, and PARP cleavage. NCP26 downregulates MYC, TCF3, and CCND1. NCP26 inhibits the growth of multiple myeloma cells. NCP26 can be used for the research of multiple myeloma.

TASIN-1 hydrochloride is a selective inhibitor of truncated APC^TR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 hydrochloride specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 hydrochloride exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 hydrochloride can be used to prevent and intervene in APC mutant colorectal cancer.

Neosolaniol (Standard) is the analytical standard of Neosolaniol (HY-N6799). This product is intended for research and analytical applications. Neosolaniol is an orally active type A trichothecene mycotoxin, and it is a metabolite of T-2 Toxin (HY-N6792) in human cancer cells and renal epithelial cells. Neosolaniol targets Bax, Bcl-2, caspase 3, caspase 8, and cytochrome c, thereby inducing apoptosis, emesis and anorexia. Neosolaniol reduces intracellular ATP levels, elevates ROS levels, decreases mitochondrial membrane potential, induces mitochondrial damage, and exerts toxicity on Leydig cells. Neosolaniol downregulates the expression of intestinal tight junction proteins in broilers and increases the load of Salmonella enteritidis in the cecum of broilers. Neosolaniol can be used in research related to anorexia, lymphoma, Fusarium melonis rot, and Salmonella infection.

N1,N11-Diethylnorspermine (tetrahydrochloride) (Standard) is the analytical standard of N1,N11-Diethylnorspermine (tetrahydrochloride). This product is intended for research and analytical applications. N1, N11-Diethylnorspermine tetrahydrochloride (DENSPM tetrahydrochloride) is a potent anticancer agent. N1,N11-Diethylnorspermine tetrahydrochloride activates polyamine catabolism and downregulates mTOR protein. N1,N11-Diethylnorspermine tetrahydrochloride induces the release of cytochrome c from mitochondria, resulting in activation of caspase 3. N1,N11-Diethylnorspermine tetrahydrochloride kills glioblastoma multiforme (GBM) through induction of SSAT (spermidine/spermine N1-acetyltransferase) coupled with H2O2 production.

N-Hydroxyphthalimide (Standard) is the analytical standard of N-Hydroxyphthalimide (HY-Y0396). This product is intended for research and analytical applications. N-Hydroxyphthalimide is a blocking agent and catalyst. N-Hydroxyphthalimide promotes oxidation reactions by generating PINO free radicals and activating hydrogen atom transfer processes. N-Hydroxyphthalimide reduces the expression of anti-apoptotic proteins Survivin and Bcl-xL and activates caspase 9 and caspase 3. N-Hydroxyphthalimide induces Apoptosis. N-Hydroxyphthalimide inhibits the phosphorylation of mTOR (Ser2448, Ser2481) and Akt (Ser473). N-Hydroxyphthalimide has anticancer effects against breast and colon cancer.

STA-1474 sodium is an orally active and highly selective HSP90 inhibitor, as well as a phosphate prodrug of the HSP90 inhibitor STA-9090 (HY-15205). STA-1474 sodium disrupts the chaperone function of HSP90 and promotes the degradation of client proteins. STA-1474 sodium inhibits the phosphorylation of Met, Akt and STAT3, thereby blocking related signaling pathways. STA-1474 sodium induces apoptosis and inhibits proliferation of osteosarcoma cells, and triggers the up-regulation of HSP70 and HSP90. STA-1474 sodium induces tumor regression and caspase-3 activation in mouse osteosarcoma xenograft models. STA-1474 sodium can be used in the research of osteosarcoma.

Almorexant hydrochloride (Standard) is the analytical standard of Almorexant (hydrochloride) (HY-10805A). This product is intended for research and analytical applications. Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with K_d values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.

Diuvaretin is an antimalarial agent and a C-phenylated dihydrochalcone. Diuvaretin can be isolated from the roots of U. acuminata. Diuvaretin increases the activity of Caspase-3 and triggers Apoptosis. Diuvaretin exhibits antiparasitic activity against Plasmodium falciparum. Diuvaretin can be used in the research of promyelocytic leukemia and malaria.

Linichlorin A is a p27^Kip1 ubiquitination inhibitor that blocks p27^Kip1 degradation by inhibiting the Skp2-Cks1–p27^Kip1 interaction. Linichlorin A shows selective antiproliferative activity against tumor cells. Linichlorin A induces apoptosis in leukemia cells via cytochrome c release, caspase activation and PARP cleavage. Linichlorin A can be used in the study of leukemia, melanoma, cervical cancer and breast cancer.

Amsacrine lactate (m-AMSA lactate) is a Topoisomerase II inhibitor. Amsacrine lactate intercalates into DNA. Amsacrine lactate induces Ca²⁺-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine lactate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine lactate blocks HERG potassium channels in the open/inactivated state. Amsacrine lactate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine lactate exhibits anti-leukemic activity. Amsacrine lactate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine lactate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies.

2-HBA (Standard) is the analytical standard of 2-HBA (HY-103667). This product is intended for research and analytical applications. 2-HBA is a potent inducer of NAD(P)H:quinone acceptor oxidoreductase 1 (NQO1) which can also activate caspase-3 and caspase-10.

Acanthoic acid (NP1302) is an orally active pimarane-type diterpenoid. Acanthoic acid is isolated from the root bark of Araliaceae family plant Eleutherococcus senticosus (Siberian ginseng). Acanthoic acid activates LXR and FXR. Acanthoic acid activates the AMPK-LKB1, SIRT1, and p38 MAPK signaling pathways and increases the phosphorylation level of ACC. Acanthoic acid downregulates the expression of SREBP-1, CYP2E1, HIF-1α, and PPARγ, and upregulates the expression of PPARα. Acanthoic acid induces Apoptosis by activating Caspase-3, promoting PARP cleavage, and downregulating Bcl-xL. Acanthoic acid exhibits antioxidant, anti-fibrotic, and hepatoprotective effects. It reduces lipid accumulation and lipogenesis. Acanthoic acid is used in studies on non-alcoholic fatty liver disease, alcoholic liver disease, acute promyelocytic leukemia, and Acetaminophen-induced hepatotoxicity.

Anticancer agent 340 is an orally active antitumor agent. Anticancer agent 340 can bind to both the androgen receptor (AR) and BRD4 protein simultaneously, dose-dependently inducing the formation of the AR-BRD4 ternary complex, inhibiting the expression of the downstream target gene HEXIM1 (Gene X), and activating the Caspase 3/7 pathway to initiate apoptosis. Its proliferation inhibition and apoptosis activities are both significantly AR expression-dependent. Anticancer agent 340 can be used to study AR/BRD4 driven malignancies such as castration-resistant prostate cancer (CRPC).

GNE-140 racemate (Standard) is the analytical standard of GNE-140 racemate (HY-100742). This product is intended for research and analytical applications. GNE-140 racemate is a racemic mixture of (R)-GNE-140 (HY-100742A) and (S)-GNE-140 (HY-100742B), and also a tautomer of GNE-140 (HY-118241). GNE-140 racemate is an orally active lactate dehydrogenase inhibitor, with an IC₅₀ of 3 nM against human LDHA and an IC₅₀ of 5 nM against LDHB. GNE-140 racemate reduces the phosphorylation level and total protein expression of p38 MAPK, and inhibits EGF-induced AKT phosphorylation. GNE-140 racemate decreases lactate production, regulates glycolysis, the pentose phosphate pathway and nucleotide biosynthesis, increases extracellular pH, inhibits cell proliferation, migration and invasion, and induces caspase-3 activation and ROS accumulation. GNE-140 racemate can be used in research related to breast cancer, cystic fibrosis and pancreatic cancer.

GO-Y078 is a curcumin (HY-N0005) analog. GO-Y078 activates p38/JNK1/2. GO-Y078 activates the MAPK pathway, Caspase 3/8/9, PARP, AP-1, DR5, and TP53, while inhibiting cIAP-1, XIAP, and NF-κB. GO-Y078 induces sub-G₁/G₂/M phase arrest and Apoptosis. GO-Y078 impairs angiogenesis. GO-Y078 can be used in research related to osteosarcoma, cervical cancer, oral squamous cell carcinoma, and peritoneal metastasis of gastric cancer.

ARRY-380 analog (Standard) is the analytical standard of ARRY-380 analog (HY-10531). This product is intended for research and analytical applications. ARRY-380 analog (Compound PCM-0095494) is an ARRY-380 (HY-16069) analog. ARRY-380 analog activates caspases 3 and caspases 8. ARRY-380 analog inhibits Salmonella replication in cells.

Phlorizin (Floridzin) (Standard) is the analytical standard of Phlorizin. This product is intended for research and analytical applications. Phlorizin is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC₅₀ of 0.04 μM and a K_i of 39 nM against hSGLT2, and an IC₅₀ of 0.17 μM and a K_i of 0.31 μM against hSGLT1. Phlorizin promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin also exhibits antibacterial, anti-inflammatory and neuroprotective activities.

Myrothecine A is a trichothecene mycotoxin found in M. roridum. Myrothecine A induces apoptosis, promotes the cytochrome c release, PARP-cleavage and phosphorylation of JNK, increases Bax and cleaved caspase-3, -5, and -8 levels. Myrothecine A has anticancer activities and promotes the maturation of DC cells in the microenvironment. Myrothecine A inhibits proliferation of A549, MCF-7, HepG2, and SMMC-7721 cancer cells with IC₅₀s of 95, 70, 60, and 25 µM, respectively.