Apoptosis Inducer

Tubulosine is an alkaloid. Tubulosine can be isolated from Pogonopus tubulosus (DC.) Schumann. Tubulosine is an ATP-competitive, selective JAK3 inhibitor with an IC₅₀ value of 9.9 nM. Tubulosine also inhibits the kinase activities of other JAK family members, the extent of inhibition is less than that of JAK3, with IC₅₀ values of 69.5, 84.9 and 76.3 nM for JAK1, JAK2 and TYK2, respectively. Tubulosine selectively inhibits JAK3 signalling by binding to the ATP-binding site of the kinase of JAK3. Tubulosine induces apoptotic and necrotic/autophagic cell death. Tubulosine inhibits the process of peptide chain elongation by eukaryotic polysomes by, specifically preventing the elongation-factor-2-dependent step of translocation. Tubulosine exhibits anticancer activity in breast cancer cells.

Sertaconazole (nitrate) (Standard) is the analytical standard of Sertaconazole (nitrate). This product is intended for research and analytical applications. Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells.

Phanginin D is a cassane-type furanoditerpene found in the seeds of Caesalpinia sappan. Phanginin D induces apoptosis in HL-60 cells by activating Caspase-3 and promoting the cleavage of procaspase-3 and PARP. Phanginin D can be used for research on human promyelocytic leukemia.

FBP is a mitochondria-targeted, selective anticancer agent. FBP induces oxidative stress and mitochondrial dysfunction, leading to Apoptosis. FBP generates ROS and causes double-strand DNA breaks in cancer cells. FBP exhibits cytotoxic efficacy against cancer cells, with cervical cancer cells being the most sensitive. FBP can be used for the research of cervical cancer, lung cancer, melanoma and breast cancer.

Antitumor agent-196 (Compound 6a (β, β, β)) is an artemisinin-based oligomer with anticancer activity, showing an IC₅₀ of 90 nM against MCF-7 breast cancer cells. Antitumor agent-196 promotes Apoptosis by regulating the Bax-caspase 3 signaling pathway, and induces Ferroptosis through the modulation of key signaling molecules, including GPX4. Antitumor agent-196 holds promising potential for further research in the field of cancer therapy.

Dinoprost-¹³C₅ is ¹³C labeled Dinoprost (HY-12956). Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour.

Anticancer agent 195 (Compound 10) is an inhibitor for ELF3-MED23 PPI with K_i of 0.68 μM. Anticancer agent 195 induces apoptosis and exhibits antitumor activity.

PROTAC HDAC8 Degrader-2 is a HDAC6/8 PROTAC degrader, with IC₅₀ values of 0.042 μM and 0.147 μM against human HDAC8 and HDAC6, respectively, and exhibits selectivity over other class I HDAC isozymes. PROTAC HDAC8 Degrader-2 induces apoptosis (apoptosis) in leukemia cells, shows no obvious cytotoxicity to normal cells, and has favorable chemical stability. PROTAC HDAC8 Degrader-2 can be used in research related to acute myeloid leukemia.

SCP-7 is a STAT3 inhibitor with a K_d value of 795 nM. SCP-7 induces mitochondrial dysfunction, increases ROS levels and promotes apoptosis. SCP-7 induces G2/M phase arrest of the cell cycle. SCP-7 inhibits the proliferation, migration and colony formation of colorectal cancer cells. SCP-7 suppresses tumor growth in a mouse xenograft model of colorectal cancer. SCP-7 is applicable to research related to colorectal cancer.

(Rac)-Roscovitine ((Rac)-Seliciclib) is a selective cyclin-dependent kinases (CDKs) inhibitor. (Rac)-Roscovitine binds to the active sites of CDKs competitively with ATP, inhibiting the phosphorylation activity of CDKs. (Rac)-Roscovitine induces apoptosis in cancer cells. (Rac)-Roscovitine is promising for research of cancers or other diseases associated with CDK dysregulation, such as neurodegenerative diseases, cardiac disorders, viral and protozoan infections, glomerulonephritis, and chronic inflammation.

Anticancer agent 211 (AK301) can inhibit tubulin polymerization. Anticancer agent 211 can block the division of human colon cancer cells. Anticancer agent 211 can increase the sensitivity of human colon cancer cells to apoptotic ligands and promote cell apoptosis.

GSK-3484862 GMP is GSK-3484862 (HY-135146) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma.

IDO1-IN-34 is a selective IDO1 inhibitor with an IC₅₀ of 0.093 μM. IDO1-IN-34 exhibits cytotoxicity against various cancer cell lines. IDO1-IN-34 inhibits the kynurenine (kynurenine) pathway and activates IL-2. IDO1-IN-34 induces cell apoptosis via the endogenous mitochondrial pathway, while increasing the levels of cytochrome c, caspase-3, caspase-9 and PARP-1. IDO1-IN-34 can be used for research on liver cancer, lung cancer, breast cancer, prostate cancer, colon cancer and leukemia.

Sodium butyrate (GMP) refers to Sodium butyrate (HY-B0350A) of GMP grade. Small molecules of GMP grade can be used as adjuvants in cell therapy. Sodium Butyrate (sodium butanoate) is an inhibitor of HDAC, possessing anti-tumor activity.

EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual BRAFV600E/EGFR inhibitor with IC₅₀ of 0.048 μM and 0.037 μM, respectively. EGFR/BRAFV600E-IN-5 has significant anti-melanoma activity with IC₅₀ of 3.16 μM and 2.50 μM against MALME-3M and LOX-IMVI cell lines, respectively. EGFR/BRAFV600E-IN-5 exerts anti-tumor effects by inducing G1 arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 can be used for melanoma research, especially for combined inhibition of BRAFV600E mutation and EGFR signaling pathway.

Enzastaurin (LY317615) hydrochloride is a potent and selective PKCβ inhibitor with an IC₅₀ of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.

EGFR-IN-187 (Compound 4d) is a selective EGFR inhibitor with an IC₅₀ of 25.41 μM. EGFR-IN-187 can cause cancer cells S amd G2/M phase arrest and induce apoptosis and autophagy. EGFR-IN-187 upregulates CCNE1, Bax, LC3B-II and P27 expression and downregulates CCNA1 and Bcl-2 levels. EGFR-IN-187 can be used for the research of cancer, such as lung cancer.

HDAC-IN-105 is a histone deacetylase (HDAC) inhibitor with binding to HDAC2 and HDAC4 isoforms. HDAC-IN-105 suppresses HDAC activity via binding within conserved HDAC catalytic pockets. HDAC-IN-105 induces G2/M phase cell cycle arrest. HDAC-IN-105 triggers mitochondrial dysfunction marked by loss of mitochondrial membrane potential. HDAC-IN-105 exhibits growth inhibition in triple-negative breast cancer cells and low toxicity toward normal cells. HDAC-IN-105 can be used for the research of triple-negative breast cancer.

JC-010a is a selective SHP2 allosteric inhibitor. JC-010a inhibits cancer cells proliferation. JC-010a can be used for the research of cancer.

Dobesilate-d₆ (calcium) is deuterium labeled Calcium dobesilate. Calcium dobesilate, a vasoprotective, is widely used in chronic venous disease, diabetic retinopathy and the symptoms of haemorrhoidal attack in many countries.