Apoptosis

Tubulin polymerization-IN-79 (Compound C20) acts as an inhibitor of microtubule polymerization. It exhibits significant antiproliferative activity against esophageal cancer cells, such as KYSE450 (IC50=0.36 μM) and EC-109 (IC50=0.63 μM). In esophageal cancer cells, Tubulin polymerization-IN-79 occupies the colchicine binding site, disrupting the microtubule network's integrity, activating the Hippo signaling pathway, downregulating the oncogenic protein YAP, and inducing G2/M phase arrest and apoptosis. This compound shows promise for esophageal cancer research.

HSP90-IN-18 inhibits Hsp90 with 0.39 μM IC50, useful for viral, neurodegenerative, and inflammatory research.

LSD1-IN-26 (12u) is a potent LSD1 inhibitor (IC50=25.3 nM), also inhibits MAO-A/B, induces apoptosis in MGC-803, for gastric cancer research.

Chaetoglobosin A, the active compound extracted of Penicillium aquamarinium, is a member of the cytochalasan family. It preferentially induces apoptosis.

Thalidomide-O-PEG4-NHS ester is a polyethylene glycol (PEG)-based linker, commonly employed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].

Arisostatin A is a secondary metabolite produced by microorganisms, recognized as an antibiotic (antibiotic) with activity against Gram-positive bacteria. This compound also exhibits potent antitumor properties. It induces apoptosis (apoptosis) by activating caspase-3 and generating reactive oxygen species (ROS) in AMC-HN-4 cells.

F1324 acetate is an efficient, high-affinity b-cell lymphoma inhibitor with IC50 of 1 nM.

Ganglioside GD3 disodium salt is a melanoma-associated antigen often targeted in immune therapy for melanomas.

Halleridone, a natural product, is identified in Teuanchum decipiens and Abeliophyllum distichum.

Gal-ARV-771 is a PROTAC prodrug, modified with galactose, based on ARV-771. It is activated in senescent cancer cells that express SA-β-Gal, thereby releasing ARV-771. Through the ubiquitin-proteasome pathway, Gal-ARV-771 induces selective degradation of the BRD4 protein in senescent cells and promotes apoptosis (apoptosis) of these cancer cells.

FHD-286 is an inhibitor of BRM/BRG1 ATPase and can be used for studies on the treatment of BAF-related disorders such as acute myeloid leukemia.

Compound 25b, an FPR1 antagonist, exhibits potent inhibition of the formyl peptide receptor 1 with an IC50 of 70 nM.

Ch282-5, an orally active inhibitor targeting the Bcl-2 protein, promotes mitochondria-dependent apoptosis (Apoptosis) by disrupting mitophagy and the mTOR pathway. It demonstrates antiproliferative effects on colorectal cancer cells, effective both in vitro and in vivo, while also inhibiting metastasis. Further, Ch282-5 augments Oxaliplatin-induced autophagy (Autophagy) by downregulating Mcl-1 protein and raising platelet count, which helps mitigate the adverse effects of Navitoclax.

PROTACRIPK1Degrader-1 is a selective RIPK1 PROTAC degrader. This compound degrades RIPK1 in various cancer cell lines, such as A375 and B16F10 cells. It enhances the anticancer effects of radiotherapy in both syngeneic and humanized mouse models. PROTACRIPK1Degrader-1 is applicable for research in cancers like melanoma.

BRD4/FKBP12 degrader-2 (a1d) is a BRD4/FKBP12 degrader with anticancer activity.

S-Acetyl-L-glutathione boosts intracellular GSH, induces lymphoma cell apoptosis, and inhibits HSV-1 replication, improving survival in HSV-1 mice.

Perfluorodecanoic acid is a biochemical.

Eldecalcitol, orally active vitamin D analog, boosts bone density and treats osteoporosis.

HDAC-IN-77 (HL-5s), an HDAC inhibitor, has the capability to induce ferroptosis and suppress the Nrf2/HO-1 signaling pathway. This compound is utilized in cancer research.

Pexelizumab is a humanized antibody targeting C5 to inhibit apoptosis and treat cerebral IR injury and myocardial infarction.

Rat form of the beta-Amyloid (1-40) peptide

BAD (103-127) human peptide from BH3 domain, blocks Bcl-xL, 800x more binding than 16-mer.

HMGB1-IN-2 (compound 15) is a selective inhibitor of the highly conserved nuclear protein HMGB1, demonstrating no inhibitory effect at an IC50 of 20.2 μM in

Thujopsene, a sesquiterpene found in T. dolabrata, exhibits a wide range of biological activities. It inhibits Na+/K+-ATPase and cytochrome P450 (CYP) isoform CYP2B6 with IC50 values of 25.9 µg/ml and Ki of 0.8 µM, respectively. Additionally, thujopsene demonstrates antimicrobial efficacy against both Gram-positive and Gram-negative bacteria, such as S. aureus, M. luteus, and S. typhimurium, with MICs ranging from 25-50 µg/ml. It also suppresses antigen-induced β-hexosaminidase release in IgE-sensitized RBL-2H3 mast cells (IC50= 25.1 µM) and shows cytotoxicity against A549 non-small cell lung cancer cells with an LC50 of 35.27 µg/ml. Furthermore, thujopsene causes mortality in mites D. farinae and T. putrescentiae, with LC50s of 9.82 and 10.92 µg/cm2, respectively.

PRDX1-IN-2 (compound 15) is a selective inhibitor of the antioxidant enzyme Peroxiredoxin 1 (PRDX1) with an IC50 of 0.35 μM. It reduces mitochondrial membrane potential in SW620 cells, potentially due to increased ROS resulting from PRDX1 inhibition, leading to apoptosis. PRDX1-IN-2 is applicable in colorectal cancer research.

AMG-7209 is an effective and selective MDM2-p53 interaction inhibitor.

Caspase-3/7 activator 1 is an effective activator of Caspase-3/7 that exhibits tumor-selective, antiproliferative activity and high apoptosis (Apoptosis) induction capability.

Diafenthiuron is a widely utilized thiourea-based pesticide that effectively hinders mitochondrial activity in insect pests.

L-Glutamic-5-14C acid is a bioactive chemical.

dASK1-VHL is an orally active PROTAC degrader targeting ASK1. It effectively binds to VHL, promoting the selective degradation of ASK1. By reducing ASK1 protein levels, dASK1-VHL inhibits the activation of p38 MAPK and decreases liver lipid content, offering new insights for MASH research.

VPC-70063 (Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)-) is an inhibitor of c-Myc-MAX.

SB-T-1214 (SBT) is a taxane-based drug known for its ability to effectively suppress the expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induce apoptosis in drug-resistant tumorigenic CD133+/CD44+ colon cancer spheroids. In Pgp+ DLD-1 human colon tumor xenograft mouse models, SB-T-1214 successfully inhibits tumor growth. This compound is relevant for anti-tumor research, particularly against drug-resistant tumors such as colon, pancreatic, and renal cancers.

CDK4/6/HDAC-IN-1 (Compound N14) is a dual-target inhibitor of CDK4/6 and HDAC, with IC50 values of 7.23 nM for CDK4, 13.20 nM for CDK6, 55.66 nM for HDAC1, and 48.38 nM for HDAC6. It induces apoptosis and G0/G1 phase arrest through the HDAC-p21-CDK signaling pathway and can inhibit hepatocellular carcinoma.

HDAC6-IN-16 (compound 5c), a quinazolin-4(3H)-one-based inhibitor of histone deacetylase 6 (HDAC6), demonstrates an anticancer effect by inhibiting colony

GSNOR-IN-1 is a prodrug of GSNOR-IN-2 and functions as an S-nitrosoglutathione reductase (GSNOR) inhibitor capable of crossing the blood-brain barrier. GSNOR-IN-1 offers significant protective effects against damage induced by oxygen-glucose deprivation/reoxygenation (OGD/R). It regulates calcium signaling and synaptic function through Clstn1 S-nitrosylation and inhibits neuronal apoptosis. Additionally, GSNOR-IN-1 markedly reduces infarct volume in rat models of ischemic stroke while enhancing neurological function. With its neuroprotective properties, GSNOR-IN-1 holds potential for ischemic stroke research.

Eps8 peptide 327 is an HLA-A*2402-restricted peptide antigen derived from the Eps8 protein. It exhibits potent antitumor activity and significant cytotoxicity. Eps8 peptide 327 effectively inhibits cancer cell proliferation, induces apoptosis, and disrupts the EGFR signaling pathway by inhibiting the expression of downstream signals such as IL-2, TNF-α, and IFN-γ, as well as impeding the Eps8/EGFR interaction. It significantly suppresses tumor growth in HT-29 xenograft models.

PDE4-IN-28 (Compound G1) is an inhibitor of PDE4D, with an IC50 of 29 nM. It suppresses the production of TNF-α and NO, with IC50 values of 13.32 μM and 2.32 μM, respectively. In a rat pressure ulcer (PU) model, PDE4-IN-28 exhibits anti-inflammatory, antibacterial, and analgesic properties, while promoting HUVEC cell migration to enhance wound healing.

TopoisomeraseIIα-IN-10 (Compound 13r) is a topoisomerase IIα inhibitor that binds to the active site of DNA when complexed with topoisomerase IIα. This binding is stabilized through interactions with DNA base pairs and amino acid residues. By intercalating into DNA, TopoisomeraseIIα-IN-10 induces apoptosis and disrupts the mitochondrial membrane potential in HCT116 cells, effectively inhibiting their growth with an IC50 of 4.37 μM. It is applicable for cancer research studies.

FTI 277, a FTI 276 prodrug, blocks farnesyltransferase (IC50 = 0.5 nM), H-Ras/K-Ras processing, and fights tumor cell growth.

WH244 is a second-generation dual degrader (PROTAC) targeting BCL-2 and BCL-xL proteins. It effectively degrades these proteins with high specificity, exhibiting a DC50 of 0.6 nM for BCL-xL and 7.4 nM for BCL-2. By promoting ubiquitination and subsequent proteasomal degradation of these proteins, WH244 restores apoptotic pathways in cells. The compound shows strong antitumor activity.

SRE-II, an amide derivative, serves as an activatable photosensitizer tailored for photodynamic cancer research, exhibiting diminished fluorescence and

dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF of FKBP12, the Thalidomide based cereblon ligand and a linker[1].

EGFR-PK/JNK-2-IN-1 (Compound 6c) is a dual inhibitor of EGFR-PK and JNK-2, with IC50 values of 2.7 and 3.0 μM, respectively. It can induce apoptosis and cause cell cycle arrest at various stages. This compound is applicable in cancer research.

DefNEtTrp is an iron bis-chelating ligand composed of Def and Trp groups. It demonstrates potent broad-spectrum antiproliferative and cytotoxic effects in cancer cell lines. DefNEtTrp induces apoptosis and ferroptosis, exhibiting cytotoxicity with an IC50 value of 0.77 μM.

TTQ-SA is a near-infrared spiraling aggregation-induced emitter capable of converting near-infrared light (NIR) into thermal energy, resulting in thermal damage and death of tumor cells. In cancer cells MF-7, TTQ-SA shows cell uptake and targeting capabilities. TTQ-SA binds with DNAzyme to inhibit the expression of the survivin gene, enhancing the sensitivity of tumor cells to photothermal therapy.

MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).

YTHu78 is a KDM5B PROTAC-based degrader. It induces the degradation of KDM5B through the ubiquitin-proteasome system and triggers apoptosis in MV-4-11 and MM.1S cell lines. YTHu78 demonstrates significant antiproliferative activity against various hematologic tumor cell lines and is useful for studying hematological malignancies.

CGP-74514,CDK1 inhibitor (IC50=25 nM). Induces G2/M arrest, apoptosis. Used in bladder cancer research.