Apoptosis Inducer

SD-36 is a potent STAT3 PROTAC degrader with a K_d of 44.4 nM and a K_i of 11 nM. SD-36 recruits the cereblon/culin 4A E3 ligase complex to mediate ubiquitination and proteasomal degradation of STAT3, inducing G1 phase cell cycle arrest and apoptosis. SD-36 is useful for research on acute myeloid leukemia, anaplastic large cell lymphoma, and hematopoietic and lymphoid malignancies.

PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC₅₀ of < 10 μM, with little activity at E2 and E3.

SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC₅₀s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.

Hydroxysafflor yellow A (Safflomin A) is a natural product of flavonoids isolated from safflower. Hydroxysafflor yellow A can inhibit cell proliferation and promote apoptosis through the autophagy pathway. Hydroxysafflor yellow A has anti-inflammatory, antioxidant and antitumor effects. Hydroxysafflor yellow A can be used in the study of cardiovascular disease.

Brassinolide is a predominant plant growth modulator that regulate plant cell elongation.

RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation.

Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride is a blocker of polycystin-2 (PC2; TRPP2) channel.

Cidofovir (GS 0504) is an acyclic monophosphate nucleotide analogue and CMV inhibitor with antiviral activity. Cidofovir inhibits cytomegalovirus (CMV) replication by selectively inhibiting viral DNA polymerase. Cidofovir induces apoptosis and can be used in studies of AIDS cytomegalovirus retinitis, herpes, and cancer. Cidofovir also has anti-orthopoxvirus and anti-variola activities.

Afimetoran (BMS-986256) is an orally active, selective, and highly bioavailable TLR7/8 antagonist. Afimetoran (BMS-986256) can inhibit TLR7/8 activation of the NF-κB pathway and reverse TLR7 mediated resistance to steroid induced apoptosis in plasma cell like dendritic cells (pDCs). Afimetoran (BMS-986256) can be used for research on inflammation and autoimmune diseases (systemic lupus erythematosus).

NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with an IC₅₀ of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC₅₀ values of 0.584 μM, 0.706 μM, and 0.605 μM, respectively. NVP-2 induces cell apoptosis.

AMXT-1501 tetrahydrochloride is a Bacterial agent and polyamine transport system inhibitor. AMXT-1501 tetrahydrochloride targets membrane phospholipids and exhibits antibacterial activity against a variety of Gram-positive and Gram-negative multidrug-resistant bacteria. AMXT-1501 tetrahydrochloride inhibits capsular biosynthesis in Streptococcus pneumoniae. AMXT-1501 tetrahydrochloride targets ornithine decarboxylase and polyamines to inhibit the proliferation of neuroblastoma cells. AMXT-1501 tetrahydrochloride in combination with DFMO (HY-B0744) induces Apoptosis in neuroblastoma cells. AMXT-1501 tetrahydrochloride is applicable to research related to multidrug-resistant bacterial infections, pneumococcal infections, Streptococcus pneumoniae infections, and neuroblastoma.

Carnosic acid is an orally active lipid absorption inhibitor. Carnosic acid has demonstrated inhibition of oxidative stress and inflammation, suppression of cell proliferation, and antibacterial activity.

Vandetanib (D6474) is a potent, orally active, and blood-brain-barrier penetrate inhibitor of VEGFR2/KDR tyrosine kinase activity (IC₅₀=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC₅₀=110 nM) and EGFR/HER1 (IC₅₀=500 nM).

α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1.

3-Hydroxykynurenine, a metabolite of tryptophan, is a potential endogenous neurotoxin whose increased levels have been described in several neurodegenerative disorders. 3-Hydroxykynurenine induces neuronal apoptosis.

Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC₅₀ of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.

AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC₅₀s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.

SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC₅₀=99 nM, K_d=98 nM; CDK13: K_d=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death.

S-Adenosyl-L-methionine (Ademetionine) disulfate tosylate is the disulfate tosylate form of S-Adenosyl-L-methionine (HY-B0617). S-Adenosyl-L-methionine disulfate tosylate is an orally active methyl group donor. S-Adenosyl-L-methionine disulfate tosylate is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine disulfate tosylate also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine disulfate tosylate has the potential for, cancer, liver disease and osteoarthritis research.

Epibrassinolide (24-Epibrassinolide) is a ubiquitously occurring plant growth hormone which shows great potential to alleviate heavy metals and pesticide stress in plants. Epibrassinolide is a potential apoptotic inducer in various cancer cells without affecting the non-tumor cell growth.