Apoptosi

<p>FGFR1/VEGFR2-IN-2 (compound 6) is a dual inhibitor targeting both VEGFR2 and FGFR1 with IC50 values of 0.025 µM and 0.026 µM, respectively. This compound also exhibits inhibitory effects on EGFR and PDGFR-β, with IC50 values of 0.106 µM and 0.077 µM, respectively. FGFR1/VEGFR2-IN-2 demonstrates significant anticancer activity in the NCI-60 cell lines, showing a growth inhibition (GI) of 60.38%. In T-47D cell lines, it achieves an IC50 of 8.51 µM, exhibits anti-migratory properties, induces cell cycle arrest in the G1 phase, and promotes both apoptosis and necrosis. Additionally, while it has an IC50 greater than 100 µM in MCF-7 cell lines, it does so with an IC50 of 69.17 µM in MDA-MB-231 cell lines and shows no toxicity to normal cells.</p>

<p>Apoptosisinducer 24 (Compound 4) inhibits the proliferation of gastric cancer cells with an IC50 range of 1.2-4.8 μM. It arrests the cell cycle at the G2/M phase, induces apoptosis in BGC-823 cells, and causes mitochondrial dysfunction. In mice, Apoptosisinducer 24 exhibits antitumor activity without significant toxicity, having an LD50 of 91.2 mg/kg.</p>

<p>Claturafenib is a brain-permeable, selective, all-mutant BRAF inhibitor.PF-07799933 has shown antitumor activity, used in combination with MEK inhibitors.</p>

<p>Apoptosisinducer 26 (compound [AgCl(dap2SH)(PPh3)2]) is a mononuclear Ag(I) ligand-based autophagy inducer that exhibits antibacterial and anticancer activities against various bacterial strains and cancer cell lines. This compound facilitates the accumulation of Ag(I) ions in the periphery of bacteria, effectively inhibiting the growth of both Gram-positive (+) and Gram-negative (-) bacteria. Additionally, Apoptosisinducer 26 can intercalate between the base pairs of CT DNA, inducing apoptosis in A549 cells. It also possesses radical scavenging properties, which helps prevent oxidative stress.</p>

<p>Oxidosqualene cyclase inhibitor</p>

<p>LS-106 is an orally active, effective epidermal growth factor receptor (EGFR) inhibitor displaying antitumor activity both in vitro and in vivo. It inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S, with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, demonstrating stronger inhibition than Osimertinib. LS-106 induces cell apoptosis (Apoptosis), suppresses the proliferation of tumor cells carrying EGFR19del/T790M/C797S, and results in significant tumor reduction in a C797S mutant xenograft model.</p>

<p>A-1248767, a derivative of A-1210477, is an MCL-1 inhibitor (IC50=23.9 nM; Ki=0.41 nM) known for its anticancer properties. It binds to MCL-1 with high affinity, induces an increase in MCL-1 protein levels inside cells, and promotes apoptosis in tumor cells.</p>

<p>Sasanlimab (PF-06801591), a humanized IgG4-κ antibody, selectively targets PD-1 and is primarily produced in Chinese Hamster Ovary (CHO) cells [1].</p>

<p>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.</p>

<p>MBC-11 triethylamine, a first-in-class etidronate-araC conjugate, may treat TIBD.</p>

<p>Pro-GA is a cell-permeable γ-glutamylcyclotransferase (γ-GGCT) inhibitor that inhibit proliferation in multiple bladder cancer cell lines. antitumour.</p>

<p>Compound AuL9, also known as iNOS/TopoI-IN-1, is a multi-target hybrid molecule possessing anti-tumor, anti-inflammatory, and antioxidant properties. This compound effectively inhibits the growth of MCF-7 and MDA MB-231 breast cancer cells in vitro, exhibiting IC50 values of 3.5 μM and 6.3 μM respectively. It also prompts DNA damage and apoptosis in these cells by inhibiting human topoisomerase I (TopoI) with a K_i of 2.72 μM. Additionally, iNOS/TopoI-IN-1 reduces the expression of iNOS by suppressing the activation of NF-kB, with a K_i of 1.49 μM.</p>

Compound Ru2 (Antitumor photosensitizer-6) exhibits synergistic type I/II photosensitization and photocatalytic activities under illumination at 595 nm. It causes oxidative redox imbalance within cells, affecting biosynthesis and metabolic processes, leading to cell apoptosis (Apoptosis). Compound Ru2 is applicable in studies of photodynamic therapy (PDT).

<p>EGFRkinase inhibitor 7 (compound 18i) is an EGFR inhibitor with an IC50 of 42.3 nM, exhibiting anticancer properties. This compound demonstrates significant in vitro cytotoxicity and capacity to induce apoptosis. Furthermore, EGFRkinase inhibitor 7 displays anti-proliferative activity against human colon cancer cell line HCT116 and human non-small cell lung cancer cell line A549, with IC50 values of 4.82 µM and 1.43 µM, respectively.</p>

<p>TOFA-Plasmalogen (compound 1), a derivative of glyceraldehyde, exhibits ferroptosis-inducing properties. This compound promotes lipid peroxidation in cell membranes, leading to cytotoxic effects with an inhibition concentration (IC 50 = 32.87 μM).</p>

<p>WF 10129 is a new angiotensin converting enzyme inhibitor generated by a fungus, Doratomyces putredinis.</p>

<p>BTK-IN-37 (compound 8d), a BTK inhibitor, demonstrates potent apoptotic effects on cancer cells by targeting BTK with K_i and IC_50 values of 5.07 nM and 3.6 nM, respectively. Additionally, this compound selectively promotes the enrichment of genes associated with necroptosis and pyroptosis.</p>

<p>A-1208746 is an inhibitor of MCL-1 with a Ki value of 0.454 nM. This compound effectively activates caspase-3/-7, induces apoptosis in H929 cells, and reduces mitochondrial membrane potential. Additionally, A-1208746 synergizes with Navitoclax, making it applicable in cancer research.</p>

<p>4-Nitro-3-cresol exhibits ciliate toxicity against Tetrahymena pyriformis and is widely used in biochemical experiments and drug synthesis research.</p>

<p>hCAIX/XII-IN-13 functions as an inhibitor targeting specific human carbonic anhydrases (hCA) IX and XII, crucial in tumor-related processes. Demonstrating efficacy, this compound offers inhibitory K i values of 0.08 µM for IX and 0.06 µM for XII. Additionally, under hypoxic conditions, hCAIX/XII-IN-13 enhances the effectiveness of Doxorubicin on MCF-7 cells by promoting G2/M phase cell cycle arrest and increasing apoptosis.</p>

<p>Danburstotug (IMC-001), an immunostimulant and antineoplastic [1], is a humanized IgG1-lambda monoclonal antibody targeting CD274 (PDL1, B7 homologue 1, B7H1).</p>

<p>Retifanlimab (MGA-012) is a monoclonal antibody targeting programmed cell death protein 1 (PD-1). Retifanlimab is used in studies of Merkel cell carcinoma.</p>

<p>Acrixolimab is a humanized IgG4-κ monoclonal antibody that selectively targets PD-1 [1] [2].</p>

<p>Feladilimab (GSK3359609) is an IgG4 monoclonal antibody that is an ICOS agonist.</p>

<p>Nofazinlimab (CS1003) is a human anti-PD-1 IgG4 monoclonal antibody for the study of unresectable hepatocellular carcinoma (uHCC).</p>

<p>Pidilizumab (CT-011), a humanized IgG1κ anti-PD-1 monoclonal antibody, serves as a DLL1 antagonist with potential applications in researching hematologic</p>

<p>SB 699551 is a selective 5-HT5A antagonist (Ki=6.31 nM) that enhances 5-HT neuronal function. It inhibits SERT (Ki=25.12 nM),inhibit breast cancer.</p>

<p>Camrelizumab (SHR-1210) is a human IgG4-κ monoclonal antibody with high affinity and directed against PD-1.Camrelizumab binds PD-1 with a binding affinity of up</p>

Thalidomide-NH-amido-C6-NH2 hydrochloride is a synthetic E3 ligase ligand-linker conjugate that includes a thalidomide-based cereblon ligand and a linker, designed for the synthesis of PROTAC.

RIPK2-IN-4 is a potent and specific inhibitor of RIPK2 with an IC50 value of 5 nM.

<p>Chlopynostat (Compound 6c) is an HDAC1 inhibitor with an IC50 value of 67 nM. It induces apoptosis by inhibiting HDAC1, thereby reversing STAT4/p66Shc defects.</p>

<p>AEG 3482 blocks JNK, induces HSP70, binds HSP90, and boosts HSP25 expression, preventing cell death.</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>Anticanceragent 178 (compound C2) is a potent anticancer compound. It effectively inhibits the proliferation and metabolic activity of MDA-MB 231 cells, with IC50 values of 1.1 and 4.2 μM, respectively. Additionally, Anticanceragent 178 induces ferroptosis and necroptosis in cells.</p>

<p>Thalidomide-N-C3-O-C4-O-C3-OH is a conjugate of an E3 ligase ligand and a linker, used in the synthesis of the Aster-APROTAC degrader.</p>

<p>Necrosis inhibitor 2 hydrochloride (Compound B19) is an agent that inhibits cellular necrosis. It is useful for researching diseases associated with necrotic pathways, including inflammation, cancer, metabolic disorders, and neurodegenerative diseases.</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>

<p>p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.</p>

<p>DA5-HTL is a compound that combines dasatinib with the HaloTag system, effectively inhibiting the growth of tumor cells, with a GI50 of 1.923 nM.</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>MX106-4C is a survivin inhibitor that selectively targets ABCB1-positive colorectal cancer cells. It can work synergistically with Doxorubicin for enhanced anticancer effects or restore Doxorubicin sensitivity in drug-resistant ABCB1 cells.</p>

LZFPN-90 (LZ90) is a dual-target compound aimed at NAMPT and PD-L1. It inhibits the interaction between PD-1/PD-L1 and NAMPT activity. LZFPN-90 suppresses cell growth in a NAMPT-dependent manner, blocking the cell cycle and subsequently inducing apoptosis. Additionally, LZFPN-90 exhibits target-dependent antitumor activity, impacting metabolic processes and the immune system.

<p>PROTACGPX4 degrader-2 (compound 18a) is a proteolysis-targeting chimera (PROTAC) that targets the degradation of glutathione peroxidase 4 (GPX4), with a DC50, 48h value of 1.68 μM. It induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. Additionally, PROTACGPX4 degrader-2 exhibits antiproliferative activity.</p>

<p>WEE1-IN-7 (compound 12h) is a potent, orally active WEE1 inhibitor with an IC50 value of 2.1 nM. This compound induces apoptosis and causes cell cycle arrest in the S phase, demonstrating antitumor activity.</p>

<p>TopoisomeraseII inhibitor 17 (compound 4c) is a thiazolopyrimidine-based inhibitor of Topoisomerase II with an IC50 of 0.23 μM. This compound significantly disrupts the cell cycle and induces apoptosis.</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).

<p>Ru-Poma is an Ru(II)-based photosensitizer designed to enhance the efficacy of photodynamic therapy (PDT) against tumors resistant to Cisplatin. It targets Pomalidomide to partially degrade CRBN, inducing ferroptosis by increasing lipid peroxides and downregulating GPX4 and GAPDH expression. In A549 cells, Ru-Poma exhibits cytotoxicity with IC50 values of 18.46 μM in the dark and 0.37 μM under illumination.</p>

<p>AZD5582 TFA is a potent IAP antagonist that binds to the BIR3 domain of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM, respectively.AZD5582 TFA</p>

<p>Antimycobacterial agent-5 (compound 27) is an imidazopyridine amide compound that targets the Mycobacterium electron transport chain (ETC) respiratory CIII2CIV2 supercomplex. It acts on Mycobacterium smegmatis CIII2CIV2 with an IC50 of 441 nM.</p>

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.

CBI1 is a covalent BAX inhibitor. It selectively derivatizes BAX at C126 and inhibits BAX activation by triggering a ligand or through point mutations. CBI1 prevents the lipidation and oligomerization of BAX by t-2-hex. It also inhibits BAX activation induced by BH3 ligands, F116A mutation, or t-2-hex.

<p>DB2313 is a potent PU.1 inhibitor (IC50=14 nM) that disrupts gene binding, induces AML cell apoptosis, and has anticancer properties.</p>

<p>PD-1/PD-L1-IN-39 (X 14) is an orally active PD-1/PD-L1 inhibitor with an IC50 value of 15.73 nM. It exhibits strong binding affinity to human and mouse PD-L1, with KD values of 14.62 and 392 nM, respectively. PD-1/PD-L1-IN-39 also demonstrates antitumor activity.</p>

<p>PD-L1-IN-5 (X22) is an orally active PD-L1 inhibitor with an IC50 of 785.6 nM, demonstrating antitumor activity in vivo.</p>

PRMT5-IN-33 (compound A8) is a selective inhibitor of PRMT5 that competes with SAM, exhibiting an IC50 of 10.9 nM. It induces apoptosis and inhibits the proliferation of Z-138 and MOLM-13 cells, demonstrating antitumor activity.

<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>

<p>Antitumor agent-150 (V10) is a breast cancer treatment that functions as a PROTAC degrader of MDM2.</p>

<p>TS-24 is a cysteine protease histone S (CTSS) inhibitor that promotes BRCA1-mediated apoptosis.</p>

<p>Sandalore boosts hair growth, reduces cell death, and raises IGF-1, acting on olfactory receptor OR2AT4.</p>

<p>MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).</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>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>

Saquinavir mesylate (Ro 31-8959/003) is an Inhibitor of HIV Proteaseused in antiretroviral therapy

<p>Tetrac (Tetraiodothyroacetic acid) is a derivative of L-thyroxine (T4), a thyroxine integrin receptor antagonist.Tetrac induces antiproliferation by blocking</p>

<p>Diphenyl disulfide fights breast cancer by inducing cell death and stopping growth.</p>

<p>2-Thiocytidine is a purine nucleoside analog that targets malignant tumors of the inert lymphatic system and has a broad spectrum of antitumor activity.2-</p>

<p>1,4-Dideoxy-1,4-epithio-D-ribitol is a purine nucleoside analog that targets malignant tumors of the inert lymphatic system and possesses a broad spectrum of</p>

<p>COX-2 expression inhibitor</p>

<p>Ancitabine is an antitumour drug that improves Hailey-Hailey disease-related phenotypes in yeast models. inhibits DNA synthesis, acute leukaemia.</p>

<p>Traumatic Acid aids wound healing in plants by stimulating cell division to create a callus.</p>

<p>Buparlisib Hydrochloride is an inhibitor of pan-class I PI3K (IC50: 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively).</p>

<p>CuATSP is a potent free radical trapping antioxidant (RTA) and ferroptosis inhibitor inhibit lipid peroxidation, for (ALS) and Parkinson's disease.</p>

<p>Methoxyacetic acid is an endogenous metabolite.</p>

<p>5-(N,N-Hexamethylene)-amiloride (5-HMA) is an amiloride derivative that inhibits TRPA1-mediated calcium signaling (IC50: 35 μM). It functions as an inhibitor of the Na+/H+ exchanger (NHE) with Ki values ranging from 0.013 to 2.4 μM for various NHE isoforms. Additionally, 5-HMA blocks ASIC3 channels by 51% at 20 μM.</p>

<p>MC1742 inhibits class I/IIb HDACs, blocks sarcoma CSC growth, and reactivates latent HIV. IC50: HDAC1-3/8 (0.02-0.61 μM), HDAC6/10 (7-40 nM).</p>

<p>MCL-1/BCL-2-IN-2 is a selective Mcl-1 and Bcl-2 inhibitor with potential antitumor activity for tumor research.</p>

<p>Prinaberel (ERB-041) is an effective and selective ERβ agonist and &gt;200-fold selective for ERβ.</p>

<p>Sodium catechol sulfate is a bioactive chemical.</p>

<p>Givinostat (ITF-2357) is a non-selective, orally active HDAC inhibitor capable of inhibiting STAT5 phosphorylation which is antitumour and anti-inflammatory .</p>

<p>Bz 423 is a potent immunomodulator that induces apoptosis by activating Bax and Bak to induce mitochondrial outer membrane permeabilization and cytochrome c</p>

<p>Acyclovir (Aciclovir) hydrochloride is an effective oral antiviral agent with potent anti-herpetic activity. It exhibits IC50 values of 0.85 μM for HSV-1 and 0.86 μM for HSV-2, indicating strong inhibitory effects against these strains. Additionally, Acyclovir hydrochloride induces cell cycle disturbances and apoptosis. This compound also prevents bacterial infections during induction therapy for acute leukemia.</p>

<p>Chiisanoside is a useful organic compound for research related to life sciences. The catalog number is T123983 and the CAS number is 89354-01-8.</p>

<p>Sunitinib D10, a deuterium-enriched version, inhibits VEGFR2 and PDGFRβ tyrosine kinases (IC50: 80 nM/2 nM).</p>

PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM).

<p>Mepazine hydrochloride (Pecazine hydrochloride) is a MALT1 inhibitor with anticancer and antitumor activity, inhibiting RANK-induced osteoclastogenesis.</p>

Thalidomide-O-amido-PEG4-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and a

<p>FKBP12 PROTAC RC32 is a PROTAC-like degrader targeting FKBP12. It can degrade FKBP12 in organs after intraperitoneal administration.</p>

<p>Condurango glycoside A activates p53, induces ROS generation, up-regulates p53 expression, and triggers apoptosis as well as premature senescence associated</p>

<p>(S)-Oxiracetam is a positive allosteric the AMPA receptorsmodulator.</p>

<p>GSK-843 (GSK'843) is a RIP3 inhibitor with analgesic activity, inhibits RIP3 expression, and can be used as an adjunctive treatment for inflammation.</p>

<p>KS100 inhibits ALDH1A1, ALDH2, ALDH3A1, boosts ROS, triggers apoptosis, and has anti-cancer properties.</p>

<p>Amoscanate is an antiparasitic agent. It is highly effective in animals against the four major species of schistosomes which infect humans.</p>

<p>M47 is a selective CRY1 (Cryptochrome 1) degradator that enhances nuclear degradation of CRY1, thereby extending the lifespan of p53 knockout mice.</p>

4-PQBH is a potent Nur77-binding agent with antitumour activity.4-PQBH is used in the study of hepatocellular carcinoma.

<p>Hydrolyzed Fumonisin B1 is the backbone and the main hydrolysis product of the mycotoxin fumonisin B1 (FB1), can weakly inhibit ceramide synthase.</p>

<p>Propylparaben sodium, a plant-based preservative used in cosmetics, pharma, and food, hinders follicle growth and sperm health.</p>

PETCM is a caspase-3 activator and acts as an cytochrome c (cyto c)-dependent manner.

<p>Olanzapine D3 is the deuterium labeled Olanzapine.</p>

<p>LNnT is a metabolite that reduces IL-8, has anti-inflammatory effects, and aids in wound healing.</p>

<p>Z-Ile-Leu-aldehyde is an effective and competitive peptide aldehyde inhibitor of γ-secretase and notch.</p>