Apoptosis

<p>Moracin N, a ferroptosis inhibitor derived from mulberry leaves, exhibits neuroprotective activity by mitigating oxidative stress [1].</p>

<p>Thalidomide-O-PEG2-propargyl is a cereblon-based E3 ligase ligand with a PEG linker for PROTAC-induced protein degradation.</p>

<p>TNF-α-IN-6 is an orally efficacious allosteric inhibitor of TNFα ( K D = 6.8 nM).</p>

<p>Calcimycin (A-23187) is an antibiotic calcium ionophore that raises intracellular Ca2+ to induce cell death.</p>

<p>AMXT-1501 tetrahydrochloride is an inhibitor of polyamine transport.</p>

<p>NCA029 is a potent activator of human caseinolytic protease P (HsClpP) with an EC50 of 0.15 μM. It targets HsClpPP and triggers an ATF3-dependent integrated stress response, resulting in the death of colon cancer cells.</p>

<p>BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL)</p>

<p>Estradiol cypionate (Depofemin), the 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor.</p>

<p>LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). In mouse models, LC-1-40 selectively inhibits tumor growth induced by MYCN and induces nucleotide damage and apoptosis (cell death) in MYCN-associated tumors. It is applicable for cancer research.</p>

<p>dMCL1-2 is a PROTAC-based MCL1 degrader, binding at 30 nM, and induces apoptosis in leukemia.</p>

<p>HDAC6-IN-28 (compound 10C) is a potent inhibitor of HDAC6 with an IC50 of 261 nM. It significantly induces apoptosis in B16-F10 cells and causes S phase arrest. Additionally, HDAC6-IN-28 effectively increases the expression of acetylated-α-tubulin both in vitro and in vivo.</p>

<p>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.</p>

<p>ILS-920, a Rapamycin analog, has reduced immunosuppression, enhanced neuroprotection, and preferentially binds FKBP52 and L-type VGCC β1.</p>

<p>Antitumor agent-170 (Compound C6) inhibits PD-1/PD-L1 interaction and PARP7 with IC50 values of 0.342 μM and 7.05 nM, respectively. It shows high affinity for human PD-L1, with a Ki of 9.31 nM, and can restore T cell function while increasing IFN-γ secretion. In mouse models, Antitumor agent-170 exhibits antitumor effects against melanoma and demonstrates favorable pharmacokinetic properties.</p>

ECDD-S16 is a potent inhibitor of pyroptosis. It effectively suppresses pyroptosis in Raw264.7 cells activated by surface and endosomal TLR ligands.

<p>PROTACPD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with significant PD-L1 protein degradation capacity. It demonstrates strong PD-L1 degradation activity in 4T1 cells, with a DC50 of 0.609 μM. This compound is applicable to breast cancer research.</p>

<p>UZH1a: METTL3 inhibitor, IC50 280 nM, used for epitranscriptomic modulation and has antitumor properties.</p>

<p>RIP1 kinase inhibitor 9 (compound SY-1) is a selective inhibitor of RIP kinase. It effectively reduces central inflammatory responses caused by seizures. RIP1 kinase inhibitor 9 also obstructs Z-VAD-FMK-induced necroptosis in HT-29 cells, with an EC50 of 7.04 nM.</p>

<p>OPBP-1 is a D-peptide developed through phage display screening, molecular docking, and molecular dynamics simulations. It exhibits high stability, strong antitumor activity, and oral bioavailability. OPBP-1 selectively binds to the PD-L1 protein, significantly blocking the interaction between PD-1 and PD-L1, which helps restore and enhance T lymphocyte function while reducing the proportion of myeloid-derived suppressor cells (MDSCs), counteracting tumor-induced immune evasion. OPBP-1 is applicable for research in cancer immunotherapy.</p>

<p>Minocycline is a useful organic compound for research related to life sciences. The catalog number is T131626 and the CAS number is 10118-90-8.</p>

S2/IAPinh is a conjugate composed of an inhibitor of apoptosis proteins inhibitor (IAPinh) and a ligand of sigma 2 SW43. It demonstrates anti-proliferative and apoptosis-inducing activity by degrading inhibitor of apoptosis proteins (clAP-1).

RIPK1-IN-13 (compound 28) is a selective inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK1), showing a pKi of 7.66 as measured by the ADP-Glo kinase assay. It exhibits inhibitory effects in human leukemia U937 cells with a pIC50 of 7.2.

NAE-IN-1 (compound X-10) is a potent inhibitor of NAE1. It induces apoptosis and causes cell cycle arrest in the G2/M phase. Furthermore, NAE-IN-1 increases ROS levels and inhibits cell migration, demonstrating antiproliferative activity.

<p>PROTACEGFRdegrader 9 (Compound C6) is an orally active, CRBN-based PROTAC EGFR degrader. It has a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFRL858R/T790M/C797S. PROTACEGFRdegrader 9 demonstrates effective degradation activity against various EGFR mutants while not affecting EGFRWT.</p>

<p>YX-02-030M is a PROTACMDM2 degrader. It inhibits the binding of MDM2 to p53 and VHL to HIF1α, with IC50 values of 63 nM and 1.35 μM, respectively. YX-02-030M binds to MDM2 and recruits the VHL E3 ubiquitin ligase to initiate MDM2 degradation, effectively killing p53 mutant or deficient triple-negative breast cancer (TNBC) cells.</p>

N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, a dasatinib-based molecule that degrades ABL by binding to the IAP

<p>C-Peptide 1 (rat) is a polypeptide isolated from proinsulin. C-Peptide acts as a β-catenin/GSK-3β activator, influences Na/K-ATPase, regulates apoptosis.</p>

<p>KB02-SLF, a molecular glue, degrades nuclear FKBP12 by modifying E3 ligase DCAF16 and extends protein degradation.</p>

<p>Fosbretabulin is a natural cis-stilbene that interferes with cellular tubulin dynamics and selectively destroys tumor blood vessels.</p>

<p>MS105 is an orally active, selective protein tyrosine kinase 6 (PTK6) PROTAC degrader. It recruits the VHL E3 ligase through a VHL ligand fragment, facilitating ubiquitination and proteasomal degradation of PTK6, thereby inhibiting the proliferation and migration of breast cancer cells and inducing apoptosis (apoptosis). MS105 is a promising compound for breast cancer research.</p>

<p>MKC-1 (Ro-31-7453) is an oral bisindolylmaleimide inhibitor that disrupts tubulin polymerization, potentially halting cancer cell division.</p>

Vinepidine (LY-119863) sulfate, a derivative of vincristine, exhibits antitumor activity .

<p>Tubulin polymerization-IN-67 (Compound 5h) serves as an inhibitor of microtubule protein polymerization at the colchicine binding site, exhibiting an IC50 value of 2.92 μM. It effectively inhibits the proliferation of various cancer cell lines including HT29, A549, U2OS, MG-63, and HeLa, with IC50 values ranging from 0.12 to 4.13 μM. Additionally, Tubulin polymerization-IN-67 induces cell cycle arrest at the G2/M phase and triggers apoptosis in U2OS cells. It also inhibits cell migration in A549 and reduces mitochondrial membrane potential (MMP) while increasing intracellular ROS levels, thereby suppressing angiogenesis in HUVEC cells. Furthermore, this compound demonstrates antitumor activity in mice.</p>

<p>Fuscin, a quinonoid from O. fuscum, inhibits ADP/ATP translocase, depletes glutathione, disrupts NADH oxidation, and blocks MIP-1α/CCR5 binding (IC50: 21µM).</p>

<p>Azalamellarin N is a pyroptosis inhibitor that exhibits varying inhibitory effects on different pyroptosis inducers. It functions by targeting molecules upstream of NLRP3 inflammasome activation, instead of directly affecting the components of the NLRP3 inflammasome. Its inhibitory potency against various inducers is ranked as follows: Nigericin &gt; R837 [1].</p>

<p>HMGB1-IN-1 (compound 6) exhibits potent inhibition of NO production in RAW264.7 cells, with an IC50 of 15.9 ± 0.6 μM, and effectively disrupts the HMGB1/NF-κB/</p>

<p>Human PD-L1 inhibitor III is a human PD-L1 inhibitor.</p>

<p>FAK-IN-25 (4c) is an inhibitor of FAK with an IC50 value of 50.98 nM. It induces apoptosis and causes cell cycle arrest in the G1 phase, making it relevant for cancer research.</p>

<p>SF1126 is a first-in-class PI3K/BRD4 inhibitor and RGDS-conjugated LY294002 prodrug, enhancing solubility and targeting tumor integrins.</p>

FL118 is a novel survivin inhibitor that inhibits cancer stem cell-like properties.FL118 is a novel camptothecin analog with anticancer activity that inhibits

PD-L1inhibitory peptide is an inhibitor peptide that targets the programmed cell death ligand 1 (PD-L1). By binding to PD-L1, it lifts immune suppression and restores the anti-tumor activity of T cells. PD-L1inhibitory peptide holds promise for use in tumor research.

<p>IRF1-IN-2 is a small molecule IRF1 inhibitor that suppresses pyroptosis, protecting against radiation-induced skin damage.</p>

<p>RLX HCl is anticancer, inhibits tumour proliferation by suppressing the PI3K/Akt/FoxO3a in experimental colon cancer, antiproliferative.</p>

<p>GSK-1070916 (GSK-1070916A) is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM.</p>

<p>Atibuclimab is a chimeric monoclonal antibody targeting CD14, consisting of a mouse variable region and a human IgG4 Fc region.</p>

<p>XIAP BIR2/BIR2-3 Inhibitor-3 functions as a dual inhibitor targeting both BIR2 and BIR2-3 domains, exhibiting potent activity with IC50 values below 1 nM. This compound is utilized in cancer research [1].</p>

Compound Ir5 (Antitumor agent-145) serves as a tumor inhibitor characterized by significant fluorescence and mitochondrial targeting. It promotes anti-cancer activity by inducing necroptosis and stimulating the necroptosis-related immune response [1].

<p>Compound 5b (Anti-inflammatory agent 61) is a potent anti-inflammatory agent that diminishes TNF-α expression in LPS-induced inflammation within RAW 264.7 cells</p>

<p>SB-1295, an orally active CDK9/T1 inhibitor with an IC50 of 0.17 μM, exhibits antiproliferative effects on HCT 116 and MIA PaCa-2 cells.</p>

<p>PDE4B-IN-4 is an inhibitor of PDE4B (IC50: 2.82 nM) and TNF-α (IC50: 7.20 nM). It demonstrates anti-inflammatory properties by reducing neutrophilia in a mouse model of lipopolysaccharide (LPS)-induced sepsis.</p>

<p>Zamzetoclax (compound 1) acts as a potential inhibitor of Mcl-1.</p>

<p>CIGB-300 acetate (P15-Tat acetate) is a peptide that acts as an inhibitor of casein kinase 2 (CK2). It exhibits anticancer properties by disrupting the phosphorylation activity of CK2. CIGB-300 acetate induces apoptosis in various tumor cell lines and is applicable for cancer research.</p>

<p>EGFR/DHFR-IN-2 (9b) is a dual inhibitor of h-DHFR/EGFR TK, exhibiting IC50 values of 0.192 μM for h-DHFR and 0.109 μM for EGFR. It causes cell cycle arrest at the G1/S phase and induces apoptosis. Additionally, EGFR/DHFR-IN-2 (9b) is a potential inhibitor of CYP2C9 and CYP3A4. This compound can be utilized in cancer research.</p>

<p>Human PD-L1 inhibitor I, a peptide, blocks PD-L1/PD-1 interaction with 3.39 μM affinity.</p>

<p>Human PD-L1 inhibitor II is a potent PD-L1 inhibitor with anti-cancer activity.</p>

<p>BcI-2/BcI-xI ligand 1, functioning as a BcI-2/BcI-xI ligand, is utilized in the synthesis of PROTAC BcI-2/BcI-xI Degrader-1 .</p>

<p>β-Glucuronide-dPBD-PEG5-NH2 is a β-glucuronide-linked pyrrolobenzodiazepine dimer that functions as a proagent for the synthesis of the antibody-drug conjugate</p>

<p>PD-1/PD-L1-IN-48 (compound HD10) is an effective inhibitor of the PD-1/PD-L1 interaction, exhibiting an IC50 of 3.1 nM. It plays a vital role in cancer research.</p>

<p>Cholesteryl Hemisuccinate Tris Salt is a cholesteryl ester with anticancer activity.Cholesteryl hemisuccinate has antitumor activity and inhibits tumor growth.</p>

<p>BM-1244 is a potent Bcl-xL/Bcl-2 inhibitor with Kis of 134 and 450 nM for Bcl- xL and Bcl-2, respectively.</p>

<p>Compound B12, a JOA derivative, collapses MMP to induce apoptosis, inhibits cloning/migration, and has an IC50 of 0.39 μM against HGC-27 cells.</p>

<p>Anticancer Agent 157 (compound 15) is a nitric oxide (NO) inhibitor with IC50 values of 0.62 μg/mL, exhibiting both anti-inflammatory and anticancer effects.</p>

<p>Vonlerizumab (Anti-TNFRSF4/OX40/CD134 Antibody) is a humanized monoclonal antibody targeting OX40, used in tumor research.</p>

<p>Desmethyl-WEHI-345 analog, a protein kinase inhibitor, holds potential for colon cancer research.</p>

<p>Os30 is a potent fourth-generation EGFR inhibitor, specifically targeting the EGFRC797S-TK mutation with IC50 values of 18 nM for EGFRDel19/T790M/C797S TK and</p>

<p>Thalidomide-Piperazine 5-fluoride hydrochloride, a derivative of the cereblon (CRBN) inhibitor Thalidomide, serves as a ligand for E3 ubiquitin ligase (Ligands for E3 Ligase), facilitating the synthesis of PROTACs [1].</p>

<p>Fac-[Re(CO)3(L3)(H2O)][NO3] (Compound 3), a rhenium(I) tricarbonyl aqua complex, acts as an anticancer agent through the induction of mitochondrial dysfunction.</p>

<p>Eriosematin has anti-proliferative and apoptosis-inducing properties and is a compound extracted from the root of Flemingia philippinensis in the Philippines.</p>

<p>BODIPY FL thalidomide is a fluorescent probe that binds human cereblon protein with high affinity, exhibiting a dissociation constant (Kd) of 3.6 nM [1].</p>

<p>LL-K9-3, a selective hydrophobic tagging technology (HyT)-based degrader, specifically targets the CDK9-cyclin T1 complex, displaying DC50 values of 589 nM for</p>

<p>Aphidicolin blocks DNA synthesis, hinders herpes virus growth, and stimulates apoptosis in leukemia cells; it's a mold-derived DNA polymerase inhibitor.</p>

<p>3-Hydroxyterphenyllin from A. candidus is a fungal compound with antioxidant, anticancer, antibacterial, and antiviral effects.</p>

<p>DJ4 induces a dose-dependent pro-apoptotic effect in the micromolar range.</p>

Poly(I:C) potassium is a synthetic RNA analog, activates TLR3/RIG-I, used as a vaccine adjuvant, and induces apoptosis in cancer cells.

<p>MY-943, a potent inhibitor of tubulin polymerization and LSD1, exhibits anticancer properties by inducing G2/M phase arrest, promoting apoptosis, and</p>

<p>Tetrathiomolybdate (TM) promotes the dimerization of the metal-binding domain (WLN4) of the cellular copper efflux protein ATP7B through its characteristic</p>

<p>SSE1806, a podophyllotoxin derivative (a natural antimitotic agent), functions as a microtubule/tubulin inhibitor, exhibiting potent anticancer and</p>

<p>2,5-Dimethylcyclohexa-2,5-diene-1,4-dione inhibits the viability of HL60 and K562 cells and exhibits antibacterial and anticancer properties.</p>

<p>Lorigerlimab (MGD019) is a bispecific IgG4 DART that blocks PD-1/CTLA-4, enhancing T-cells for mCRPC research.</p>

<p>Pimivalimab (JTX-4014), a PD-1 inhibitor, is utilized in solid tumor research [1].</p>

<p>Tripchlorolide is a useful organic compound for research related to life sciences and the catalog number is T126047.</p>

<p>Thalidomide-O-C4-COOH is a synthetic E3 ligase linker derived from Thalidomide for PROTAC tech.</p>

<p>RWJ-56110 dihydrochloride is a potent PAR-1 inhibitor (IC50=0.44μM), blocking platelet aggregation, angiogenesis, and induces apoptosis. No PAR-2/3/4 effect.</p>

<p>Lenercept (Ro 45-2081) is a recombinant fusion protein combining the soluble TNF-receptor (p55) with the Fc portion of human IgG1 [1].</p>

<p>(Rac)-BIO8898 is a chemical compound that serves as an inhibitor of the co-stimulatory interaction between CD40 and CD154.</p>

<p>Anticancer agent 137 (8q), a potent PI3k inhibitor, exhibits broad-spectrum anticancer activity by inducing G2/M cell cycle arrest and apoptosis.</p>

JNK-1-IN-3 (Compound 9e) downregulates JNK1 and phosphorylated JNK1, reduces c-Jun and c-Fos expression in tumours, and restores p53 activity.

<p>Thalidomide-NH-PEG2-COOH: a synthesized E3 ligase ligand-linker with cereblon ligand and PROTAC linker.</p>

<p>ERK-IN-6, a potent agent, inhibits ESCC growth and induces apoptosis through the ERK pathway.</p>

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

<p>PH14, a dual PI3K/HDAC inhibitor, demonstrates potent inhibition with IC50 values of 20.3 nM for PI3Kα and 24.5 nM for HDAC3.</p>

<p>Anagrelide HCl monohydrate is a platelet-reducing imidazoquinazoline for ET and PV research.</p>

<p>Antitumor Agent-116 (Compound 6C) is an anti-tumor agent that exhibits anti-proliferative properties and induces apoptosis.</p>

<p>RET-IN-4: Oral RET inhibitor, IC50 ~1 nM for variants. Selective over JAK2/FLT3. Potent anticancer use.</p>

<p>OICR12694 (JNJ-65234637) TFA, an orally active B cell lymphoma 6 (BCL6) inhibitor [1], demonstrates effectiveness in targeting BCL6 pathways.</p>

<p>Ilicicolin A is a useful organic compound for research related to life sciences. The catalog number is T125289 and the CAS number is 22581-06-2.</p>

<p>Toremifene citrate is a selective estrogen receptor modulator (SERM). It is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on the mammary and uterine tissue.</p>

<p>Antitumor agent-36: potent anti-cancer; causes DNA damage, triggers apoptosis, enhances immune response by upregulating T cells.</p>

<p>Thalidomide-Piperazine-PEG3-NH2: a cereblon ligand-linker for PROTAC E3 ligase recruitment.</p>

<p>INF 195 is an inflammasome NLRP3 inhibitor that can be used to study myocardial ischemia and myocardial infarction.</p>