Apoptosis

<p>TFCP2L1-IN-1 is a TFCP2L1 transcription factor inhibitor that regulates cell proliferation and promotes antitumor effect of Sorafenib by STAT3/NANOG pathway.</p>

<p>Elocalcitol is a calcitriol analog for inhibition of prostate cell growth.</p>

<p>TrxR-IN-8 (Compound 6f) is a selective inhibitor of TrxR with an IC50 of 10.2 μM. It induces apoptosis through oxidative stress by stimulating the production of reactive oxygen species, reducing intracellular thiols, and lowering the glutathione/glutathione disulfide ratio. TrxR-IN-8 exhibits significant cytotoxicity against non-small cell lung cancer (NSCLC) cells.</p>

<p>PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) with a dissociation constant (KD) of 0.410 nM and nicotinamide phosphoribosyltransferase (NAMPT) with an inhibitory concentration (IC50) of 2.21 nM. It disrupts KRAS-related signaling by inhibiting NAMPT's role in the synthesis of nicotinamide adenine dinucleotide (NAD+), consequently inducing apoptosis in pancreatic cancer cells with KRAS mutations. This compound holds potential for research in KRAS-mutant pancreatic cancer.</p>

<p>06:0 PE (PE(6:0/6:0)) is a water-soluble phospholipid characterized by its short acyl chains. It possesses notable antitumor activity and can inhibit tumor progression in the body. Additionally, it exhibits antiproliferative and pro-apoptotic properties, and serves as a precursor for phosphatidylcholine and phosphatidylethanolamine.</p>

<p>HAC-Y6 exerts its anticancer effects by inducing cell cycle arrest. It prompts apoptosis in COLO 205 cells with an IC50 of 0.52 µM.</p>

<p>RIPK1-IN-24 is an inhibitor of receptor-interacting protein kinase 1 (RIPK1) with an IC50 of 1.3 μM. It is utilized in research on inflammatory diseases.</p>

<p>Sabialimon P (compound 16), with an IC50 of 18.12 μM, functions as a NO release inhibitor and exhibits anti-inflammatory properties. It effectively diminishes the secretion of TNF-α, iNOS, IL-6, and NF-κB, and suppresses the expression of COX-2 and NF-κB/p65 in LPS-induced RAW264.7 cells.</p>

<p>N-ω-chloroacetyl-L-ornithine (NCAO) serves as a powerful reversible competitive inhibitor of ornithine decarboxylase (ODC), displaying cytotoxic and antiproliferative properties against various tumor cell lines, with EC50 values spanning from 1 to 50.6 µM. In vitro studies reveal that NCAO promotes Apoptosis and restricts tumor cell migration. Additionally, it demonstrates significant antitumor efficacy in a mouse model, targeting both solid and ascitic tumors using the myeloma (Ag8) cell line. NCAO holds promise in the development of antitumor agents.</p>

<p>NA-17 is a naphthalimide compound with antitumor activity and exhibits lower toxicity to normal cells such as HL-7702 and WI-38. It demonstrates p53-dependent inhibition selectivity in various NSCLC cells, inducing the accumulation of active p53 in the mitochondria and nuclei of these cells. NA-17 causes cell cycle arrest in the G1 phase and promotes apoptosis and cell death.</p>

<p>Antiproliferative agent-63 (compound 4d) is a cyclic analog of cannabidiol that acts as an anticancer agent. It demonstrates favorable activity against breast and colorectal cancer. Moreover, this compound can arrest the cell cycle in the G1 phase and induce apoptosis through the mitochondrial pathway in breast cancer cell lines.</p>

<p>Thalidomide-NH-C5-NH2 is a synthetic E3 ligase ligand-linker conjugate, consisting of a Thalidomide-based cereblon ligand and a linker, used in the synthesis of PROTACs.</p>

<p>Compound 3 (DOR agonist 2) acts as a Delta Opioid Receptor agonist. It inhibits the expression of TNF-α, obstructs NF-κB transportation to the nucleus, and activates the G protein-mediated ERK1/2 pathway. This compound is useful for research into neurodegenerative diseases.</p>

<p>Thalidomide-NH-amido-PEG2-C2-NH2 is a synthetic E3 ligase ligand-linker conjugate comprising a Thalidomide-based cereblon ligand and a linker. It is utilized in the synthesis of PROTACs.</p>

<p>TLBC, a borane-chalcone derivative, exhibits dose-dependent inhibitory effects across various glioma cell lines with IC50 values ranging from 5.5 to 25.5 μM. TLBC induces apoptosis independently of alterations in the tumor suppressor factor p53.</p>

<p>Tubulin/NRP1-IN-1 (compound TN-2) serves as a dual inhibitor targeting both Tubulin and NRP1, exhibiting IC50 values of 0.71 μM and 0.85 μM, respectively. This compound notably reduces the viability of prostate tumor cell lines and triggers apoptosis [1].</p>

<p>NLRP3-IN-26 (compound 15Z), with an IC50 of 0.13 μM, functions as an inhibitor of NLRP3. It is applicable in studies involving the DSS-induced colitis model [1].</p>

<p>Mcl-1 Inhibitor 9 (Example 2) is a potent inhibitor of myeloid cell leukemia 1 (Mcl-1), demonstrating anti-tumor activity with an IC50 value of 0.21889 nM.</p>

<p>Etalocib (LY293111) sodium is an orally active leukotriene B4 (LTB4) receptor antagonist with a Ki value of 25 nM for inhibiting [3H]LTB4 binding. It exhibits an IC50 of 20 nM against LTB4-induced calcium mobilization. Additionally, Etalocib sodium can induce apoptosis.</p>

<p>TNF-α-IN-14, a potent TNFα inhibitor, exhibits a selective inhibition profile with an IC50 of 1.1 µM and demonstrates antiinflammatory properties (WO2001072735A2; compound 12) [1].</p>

<p>PIM-1/HDAC-IN-1 (4d): inhibits PIM-1 (IC50: 343.87nM), HDAC1 (63.65nM), HDAC6 (62.39nM); induces apoptosis in MCF-7 cells.</p>

<p>Pim-1 Kinase Inhibitor 10 (compound 13a) acts as both a competitive and non-competitive inhibitor of PIM-1/2 kinase, promoting cell apoptosis and displaying anticancer properties. Additionally, this compound triggers the activation of caspase 3/7 [1].</p>

<p>ER covalent antagonist-1 (Compound 39D) acts as an antagonist of the estrogen receptor α (ERα). This compound inhibits the proliferation of ERα-positive MCF-7 cells with an IC50 of 0.98 μM, induces cell cycle arrest at the G0/G1 phase, and triggers apoptosis. Additionally, ER covalent antagonist-1 demonstrates antitumor activity in mouse models.</p>

<p>HDAC/PSMD14-IN-1 is a derivative of gambogic acid. It serves as an orally active dual inhibitor targeting PSMD14 and HDAC1, with IC50 values of 238.7 nM and 141.2 nM, respectively. The compound exhibits significant cytotoxicity against ESCC cell lines (IC50: 30-250 nM) and effectively reverses epithelial-mesenchymal transition (EMT). Additionally, HDAC/PSMD14-IN-1 can induce apoptosis. In KYSE30 cell xenograft models in mice, it displays antitumor activity. HDAC/PSMD14-IN-1 is useful for researching esophageal cancer treatment.</p>

<p>Antitumor agent-76 is a water-soluble, orally active, rapid-release prodrug of Triptolide that exhibits anticancer effects.</p>

<p>GQN-B37-E is an effective selective binder and inhibitor of MCL-1. It binds to the BH3-binding domain of MCL-1. GQN-B37-E demonstrates binding affinity for MCL-1 within the sub-micromolar range (Ki= 0.6 μM), yet shows negligible binding to BCL-2 or BCL-XL.</p>

<p>Necrosis Inhibitor 3 (compound B3) effectively inhibits necrosis, demonstrating an IC50 of 0.29 nM in HT29 cells [1].</p>

<p>Topo II/HDAC-IN-1 (7d) demonstrates potent dual inhibitory effects on Topo II and HDAC, while Topo II/HDAC-IN-1 (8d) effectively induces apoptosis [1].</p>

<p>ABL-L is able to induce apoptosis in human laryngeal cancer cells using a p53-dependent pathway.</p>

<p>MTDH-SND1 blocker 2 (compound C19) is an effective MTDH-SND1 inhibitor with an IC50 value of 487 nM. It binds to the SND1 protein with a Kd of 279 nM and can degrade the SND1 protein. Additionally, MTDH-SND1 blocker 2 exhibits antiproliferative activity and induces apoptosis, showing potential for breast cancer research.</p>

<p>L5-DA, a G-quadruplex ligand, stabilizes G4s in HeLa cells, induces apoptosis, and is cytotoxic with an IC50 of 4.3 μM.</p>

<p>MA242 is a nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy and dual inhibitor of murine double minute 2 (MDM2).</p>

<p>MG-B-28, a BTLA-HVEM inhibitor, demonstrates an IC50 value of 906 nM. It promotes T cell activation dose-dependently by inhibiting the interaction between BTLA and HVEM.</p>

<p>HC-7366 (GCN2 modulator-1) is an orally active GCN2 kinase activator with antitumor activity, inducing tumor growth inhibition.</p>

<p>KDM1/CDK1-IN-1 inhibits KDM1 (IC50: 0.096 μM) &amp; CDK1 (IC50: 0.078 μM), blocks HOP-92 G2/M phase, induces apoptosis, toxic to cancer cells.</p>

<p>Pan-Trk-IN-3: potent Trk inhibitor (IC50: 2-26 nM), effective against drug-resistant mutants, induces apoptosis, anti-tumor effects.</p>

<p>ZSH-512 is a potent inhibitor of RARγ with antiproliferative properties. It induces apoptosis and reduces the expression of CD133, NANOG, SOX2, and EPCAM proteins. ZSH-512 exhibits anticancer activity and shows potential for colorectal cancer research.</p>

<p>Spicamycin can be used as a potent inducer of differentiation of human myeloid leukemia cells (HL-60) and murine myeloid leukemia cells (M1).</p>

<p>Ganoderic acid R: potent anticancer, induces apoptosis, cytotoxic to MDR and sensitive tumor cells.</p>

<p>LSD1-IN-21: potent LSD1 inhibitor, crosses blood-brain barrier, IC50 of 0.956 μM; lowers TNF-α, anti-cancer, anti-inflammatory.</p>

<p>EGFR/HER2-IN-6 is a dual inhibitor of EGFR, HER2, and DHFR with IC50s: 0.122, 0.078, and 0.585 μM, showing anticancer potential and selectivity.</p>

<p>TopoisomeraseI/II inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of TopoisomeraseI/II that induces DNA damage and activates PARP-1, leading to the activation of RIPK1, RIPK3, and MLKL, ultimately causing necroptosis. It shows significant anticancer activity by effectively targeting cancer cell nuclei and inducing cell death through necroptosis, offering substantial clinical potential in overcoming resistance in cancer treatment.</p>

<p>MY-875 inhibits microtubule formation, binds like colchicine (IC50: 0.92 μM), activates Hippo pathway, and induces apoptosis with anticancer properties.</p>

<p>protease-activated receptor-1 (PAR1) antagonist</p>

<p>Bomedemstat (IMG-7289) hydrochloride, an oral LSD1 inhibitor, has anticancer properties, blocking cell growth and triggering apoptosis.</p>

<p>AZD0424: oral Src/Abl kinase inhibitor; potential anticancer; induces apoptosis, cell cycle arrest in lymphoma.</p>

<p>Tubulin inhibitor 14 blocks NQO2 and microtubule formation, disrupts blood vessels, and may target tumors; IC50 of 1.0 μM.</p>

<p>Compound 8a, a dual PARP10 &amp; PARP15 inhibitor, has IC50s: PARP10 at 0.14μM &amp; PARP15 at 0.40μM; it's cell-permeable &amp; anti-apoptotic.</p>

<p>NSC308848 is an effective apoptosis (cell death) inducer that operates in a Myc-dependent manner. It acts by inhibiting Myc transactivation and disrupting the DNA binding activity of Myc family proteins.</p>

<p>MLKL-IN-6 (compound P28) is a mixed lineage kinase inhibitor that specifically targets the Mixed Lineage Kinase domain-like (MLKL) protein.</p>

<p>Tandutinib (MLN518) sulfate is an effective and selective inhibitor of FLT3, with an IC50 value of 0.22 μM. It also inhibits c-Kit and PDGFR, displaying IC50 values of 0.17 μM and 0.20 μM respectively. This compound can be utilized in the treatment of acute myeloid leukemia and has the capability to cross the blood-brain barrier.</p>

<p>Ferrostatin-1 diyne (Fer-1 diyne) (compound 2) serves as an inhibitor of ferroptosis, accumulating in cellular lysosomes, mitochondria, and the endoplasmic reticulum. It notably inhibits ferroptosis independently of lysosomal and mitochondrial activity.</p>

<p>EGFR/VEGFR2-IN-3 (compound 9) is an effective inhibitor of EGFR and VEGFR-2, demonstrating IC50 values of 0.129 µM for EGFR, 0.142 µM for VEGFR-2, and 3.428 µM for COX-2. This compound exhibits cytotoxic properties and induces cell apoptosis (apoptosis) as well as cell cycle arrest at the G2/M phase.</p>

<p>TH-6, a potent HDAC inhibitor (IC50: HDAC1-0.115, 2-0.135, 3-0.242, 6-0.138, 8-2.120 μM), blocks cell migration, invasion, and has anti-tumor properties.</p>

<p>Anticancer agent 44 induces apoptosis, is selective, cytotoxic to cancer cells, and minimally toxic to human lymphocytes.</p>

<p>Rezatapopt (PC14586) is a p53 reactivator with antitumor activity for the study of locally advanced or metastatic solid tumors.</p>

<p>Topo I/COX-2-IN-1: potent dual inhibitor; IC50 0.24μM (COX-2), 4.42μM (Topo I); anti-cancer; induces apoptosis, halts migration.</p>

<p>TopoisomeraseII Inhibitor 20 TFA is a potent inhibitor of topoisomerase II with an IC50 of 0.98 µM. It can induce cell apoptosis and exhibits broad-spectrum anticancer activity.</p>

<p>Anticancer agent 64 (5m) induces apoptosis, has IC50 2.4μM in CCRF-CEM, activates caspases, cleaves PARP, affects mitochondria.</p>

<p>Metamizole (Dipyrone) hemimagnesium is an anti-inflammatory and antioxidant compound known for its ability to reduce fever. It decreases levels of C-reactive protein (CRP) and interleukin 6 (IL-6). Additionally, Metamizole hemimagnesium acts as an orally active cyclooxygenase (COX) inhibitor, suppressing cell proliferation and promoting apoptosis. It is utilized in the study of inflammation and fever.</p>

<p>Potent oral XIAP/cIAP1 inhibitor with EC50s: XIAP 5.1 nM, cIAP1 0.32 nM; curbs tumor growth in vivo.</p>

<p>VEGFR-2-IN-15 (Compound 14b) is a potent inhibitor of VEGFR-2. VEGFR-2-IN-15 inhibits the growth of HepG2 cells in the Pre-G1 phase and induces apoptosis.</p>

<p>MDK-3345 is a reversible covalent inhibitor for Mcl-1.</p>

<p>KIRA9 inhibits IRE1 with a 4.8 μM IC50, blocking ER-stress-induced mRNA decay and apoptosis by fully binding IRE1's ATP site.</p>

<p>BMS-751324: p38α MAPK inhibitor with carbamyl-methyl, esters, phosphate from HPA. Reduces rat arthritis swelling and TNFα.</p>

<p>VDX-111, an analog of vitamin D, exhibits cytotoxicity in ovarian cancer cells by upregulating the RIPK1/RIPK3 pathway and inducing necroptosis. It also promotes the expression of cytokines and demonstrates antitumor activity in a mouse model [1].</p>

<p>HBV/HDV-IN-2 (Compd 143) functions as an inhibitor for HBV, HDV, and PD-1/PD-L1, demonstrating an EC 50 of 35 nM in T cell activation.</p>

<p>SphK1-IN-2: SphK1 inhibitor, IC50: 19.81 nM; less effective on SphK2. Induces apoptosis, hinders cancer cell growth.</p>

<p>EGFR-IN-161 (Compound DD-8) is a potent and reversible inhibitor of the L858R/T790M/C797S mutant EGFR kinase, with an IC50 value of 0.87 nM. EGFR-IN-161 effectively inhibits tumor cell apoptosis, G1 phase arrest, and migration.</p>

<p>QTX125 TFA: Potent, selective HDAC6 inhibitor with antitumor effects.</p>

<p>VEGFR-IN-3 inhibits cancer cell growth (OVCAR-4, MDA-MB-468) with IC50s: 0.29, 0.35μM. Used in cancer research.</p>

<p>NiCur is an effective and selective inhibitor of CBP histone acetyltransferase (HAT), with an IC50 of 0.35 μM.</p>

<p>BTK-IN-7 is a potent inhibitor for BTK with 4.0 nM IC50, highly selective over ITK and EGFR, showing strong antitumor activity.</p>

<p>XIAP degrader-1 is a small primary amine molecule that promotes the degradation of X-linked apoptosis inhibitory protein (XIAP).</p>

<p>PD-1-IN-17 TFA is a potent PD-1 inhibitor, blocking 92% of splenocyte growth at 100 nM.</p>

<p>Compound 5f, a potent tubulin polymerization inhibitor (IC50 = 1.09 μM), blocks cell migration, tube formation, and has anti-angiogenic effects.</p>

<p>GRP78-IN-1 binds to GRP78 protein, inhibits cell growth, and triggers apoptosis in breast cancer; has -8.07 kcal/mol binding energy.</p>

<p>PD-1/PD-L1-IN-55 (compound D6) is a potent PD-1/PD-L1 inhibitor with an IC50 of 4.8 nM. It enhances IFN-γ secretion and decreases the proportion of late apoptosis due to PD-L1.</p>

<p>EGFR-IN-47: strong oral EGFRL858R/T790M/C797S blocker, induces cell death; promising for NSCLC research. IC50: 0.01 μM.</p>

<p>JR5-26B is an orally active apoptosis (apoptosis) inducer. It induces cell death via copper-mediated apoptosis and necroptosis (necroptosis). JR5-26B exhibits antiproliferative activity against MIA PaCa-2, PANC-1, PAN02, SU.86.86, and KPC-2 cells, with IC50 values of 0.6, 4.4, 8.0, 1.1, and 3.4 μM, respectively.</p>

<p>PIM1-IN-3 (HL8) selectively blocks PIM1, induces Colo320 cell apoptosis, and may be researched for cancer.</p>

<p>BRD-K56819078, a Bcl-2 inhibitor, significantly reduces the burden of senescent cells and the mRNA expression of aging-related genes in the kidneys. It exerts its anti-aging effects by inhibiting cell apoptosis (apoptosis).</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>Bcl-2-IN-3 (Compound 10) is an inhibitor of Bcl-2, utilized in cancer research.</p>

<p>WYJ-2, a selective agonist for toll-like receptor 2/1 (TLR2/1), demonstrates an EC50 of 18.57 nM in HEK 293T cells transiently co-transfected with human TLR2 and TLR1. It induces pyroptosis and has shown anticancer activity against non-small cell lung cancer (NSCLC) [1].</p>

<p>HER2-IN-11 is a psoralen derivative that induces apoptosis. HER2-IN-11 shows light-activated cytotoxicity and also exhibits anti-breast cancer activity [1].</p>

<p>Topo I-IN-1 (14d) is a powerful Topo I inhibitor with antitumor effects and DNA intercalation, inducing apoptosis.</p>

<p>eIF4E-IN-4 (Compound 33) is a selective inhibitor of the eukaryotic initiation factor 4E (eIF4E) with a biochemical activity value of 95 nM. It inhibits cap-dependent mRNA translation with an IC50 of 2.5 μM and is applicable in research on breast cancer, colon cancer, and head and neck cancer.</p>

<p>Anticancer agent 69 targets PC3 cells (IC50=26 nM), raises ROS, lowers EGFR, and induces apoptosis.</p>

<p>Z-3578 is a small molecule antagonist targeting the MrgX2 (Mas-related G protein-coupled receptor X2) with notable anti-pseudoallergic properties, exhibiting a KD value of 729 nM. It effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, with IC50 values of 4.90 µM and 6.18 µM, respectively, suppresses the release of β-hexosaminidase, and significantly reduces the release of histamine and TNF-α, as well as intracellular calcium flux. Additionally, in a mouse pseudoallergy model, Z-3578 significantly alleviates foot swelling, dye leakage, and reduces serum histamine levels, indicating a strong in vivo anti-allergic effect. Z-3578 presents as a promising lead compound in the field of anti-allergic treatments, particularly for pseudoallergic reactions.</p>

<p>LSD1/ER-IN-1 inhibits ER &amp; LSD1 (IC50: 1.55 μM), and fights MCF-7 breast cancer (IC50: 8.79 μM).</p>

<p>Compound B6, also known as TOPOI/PARP-1-IN-1, is a dual inhibitor targeting TOPOI and PARP, exhibiting low cytotoxicity and oral activity with a PARP1 IC 50 of 0.09 μM. This compound effectively inhibits cancer cell proliferation and migration, induces cell cycle arrest at the G0/G1 phase, and triggers apoptosis. In murine models, TOPOI/PARP-1-IN-1 demonstrated a tumor growth inhibition rate (TGI) of 75.4% [1].</p>

<p>FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader for target validation by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V.</p>

<p>Ferroptosis-IN-15 (compound 12) serves as an effective inhibitor of ferroptosis, exhibiting EC50 values of 0.76 μM and 0.67 μM in A375 cells and 786-O cells, respectively. It acts as a potential iron chelator and radical-scavenging antioxidant.</p>

<p>HDAC-IN-27 dihydrochloride (Compound 11h) is a potent, orally active, HDACI class-selective inhibitor, with IC50 values ranging from 0.43 to 3.01 nM for HDAC1-3. This compound exhibits both in vivo and in vitro anticancer activity. HDAC-IN-27 shows significant antiproliferative effects against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). It is useful for research on acute myeloid leukemia (AML).</p>

<p>Multi-kinase-IN-1, a powerful kinase inhibitor, exhibits antitumor properties by inducing cell apoptosis.</p>

<p>HDAC-IN-9, a dual tubulin/HDAC inhibitor, impedes A549 cell invasion/migration and shows strong anti-tumor/angiogenic effects.</p>

<p>VNPP433-3β acts as a molecular glue degrader, targeting the androgen receptor (AR) and its splice variants (AR-Vs) as well as MAP kinase-interacting serine/threonine protein kinase Mnk1/2. It effectively inhibits the proliferation of cancer cells LNCaP, C4-2B, and CWR22Rv1, with GI50 values of 0.2, 0.3, and 0.31 μM, respectively. Additionally, VNPP433-3β shows favorable pharmacokinetics in CD-1 mice and suppresses tumor growth in the CWR22Rv1 xenograft mouse model.</p>

<p>Thalidomide-NH-amido-PEG2-C2-NH2 hydrochloride is a synthetic E3 ligase ligand-linker conjugate, comprised of a cereblon ligand based on Thalidomide and a linker, utilized in the synthesis of PROTACs.</p>

<p>HDAC6/HSP90-IN-2, a cancer research chemical, inhibits HDAC6 &amp; Hsp90 with IC50s of 105.7 &amp; 61 nM.</p>

<p>BRD1991 is a chemical compound that specifically disrupts the interaction between Beclin 1 and Bcl-2, thereby inducing autophagy.</p>

<p>RIPK1-IN-23 (compound 19) is an RIPK1 inhibitor with potent anti-necroptotic effects in HT-29 cells (EC50 = 1.7 nM). Additionally, RIPK1-IN-23 exhibits anti-inflammatory properties.</p>

<p>tDHU, acid is a dihydropyrimidine cereblon ligand consisting of an E3 ligase ligand and a benzoic acid linker. It serves as an E3 ubiquitin ligase ligand-linker conjugate in the development of PROTACs.</p>

<p>N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride (TLCK hydrochloride) is an irreversible serine protease inhibitor that functions by alkylating the histidine residue at the active site, thus inhibiting trypsin and trypsin-like proteases. It effectively inhibits caspase-3, caspase-6, and caspase-7 with IC50 values of 12.0, 54.5, and 19.3 μM, respectively. Additionally, N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride induces apoptosis in HL-60 cells and prevents the reduction of mitochondrial transmembrane potential during the apoptosis process.</p>

<p>Thalidomide-NH-amido-C4-NH2 is a synthetic E3 ligase ligand-linker conjugate composed of a Thalidomide-based cereblon ligand and a linker, which is utilized in the synthesis of PROTAC.</p>

<p>Nenocorilant (Relacorilant) is an orally active glucocorticoid receptor (GR) antagonist (Ki: 0.15 nM). Nenocorilant can be used to study tumours.</p>

<p>RET-IN-7 exhibits strong inhibitory effects against RET kinase in vitro and shows significant efficacy in treating RET-driven tumor xenografts in mice through</p>