Apoptosis

<p>RETligand-3 is the ligand for PROTAC QZ2135, which targets RET.</p>

<p>PARP1/BRD4-IN-3 (compound HF4) is an effective inhibitor of BRD4 and PARP1, with IC50 values of 1210 nM and 2019 nM respectively. The compound exhibits antiproliferative activity, induces apoptosis (apoptosis) and cell cycle arrest at the G0/G1 phase. Additionally, PARP1/BRD4-IN-3 causes DNA damage and reduces the expression of the Rad51 protein, demonstrating anti-tumor activity.</p>

<p>PTD-p65-P1: a NF-kappaB inhibitor blocking activation from multiple inflammatory stimuli.</p>

<p>Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. It significantly promotes Nur77 expression and apoptosis, exhibiting excellent growth inhibitory effects on HepG2 and MCF-7 cells, with an IC50 of less than 5 μM. Nur77 modulator 4 activates Nur77-mediated ER stress through the PERK-ATF4 and IRE1 signaling pathways, leading to apoptosis. This compound is applicable in cancer research.</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>MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1). This compound effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest, and increases cellular apoptosis (Apoptosis). Additionally, MS41 reduces chromatin occupancy related to ENL-mediated transcription elongation mechanisms and suppresses the expression of oncogenes and the progression of leukemia.</p>

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

<p>RSM3 TFA is a stapled peptide and an inhibitor of METTL3-METTL14, exhibiting a dissociation constant (Kd) of 3.10 μM. It inhibits tumor growth and induces cell apoptosis. RSM3 TFA is utilized in cancer research.</p>

<p>ZYH-23 is a potent inhibitor of necroptosis. It targets HSP90 to inhibit the phosphorylation of RIPK1, RIPK3, and MLKL, effectively blocking programmed cell necrosis.</p>

<p>BGC4 is a gold(III) complex based on biphenyl. It inhibits human recombinant thioredoxin reductase (TrxR) with an IC50 of 10.7 μM, exhibits cytotoxicity with an IC50 of 5.4 μM in MDA-MB-231 cells, and induces apoptosis. Additionally, BGC4 demonstrates antitumor activity in mouse models.</p>

<p>GL392 is a senolytic agent that delivers the potent senescence-clearing compound Dasatinib specifically to senescent cells. By targeting the LBD domain, it binds lipofuscin in these cells and releases Dasatinib via an ester linkage, inducing apoptosis (Apoptosis) in senescent cells. Additionally, GL392 is encapsulated in PEO-b-PCL microcapsules to ensure efficient intracellular delivery while minimizing systemic toxicity. GL392 is applicable in cancer research.</p>

<p>CDK9-IN-24 (compound 21a) is a potent and selective inhibitor of CDK9 that exhibits a pronounced inhibitory impact on tumor proliferation.</p>

<p>Anticanceragent 272 (Compound 2) is an anticancer agent demonstrating significant activity against bladder cancer cells (T-24) with an IC50 of 2.81 μM. It depletes glutathione (GSH) through a Fenton-like reaction, generating reactive oxygen species (ROS) and hydroxyl radicals (•OH), thereby inducing apoptosis and ferroptosis. Anticanceragent 272 enhances chemodynamic therapy (CDT) and promotes tumor cell death through mitochondrial dysfunction and autophagy. It holds potential for further research in bladder cancer.</p>

<p>IPH10 is an anticancer agent with strong antitumor effects in vivo and exhibits no liver or kidney toxicity. It significantly increases the reactive oxygen species (ROS) levels in tumor cells, decreases mitochondrial membrane potential, and induces apoptosis (apoptosis) in these cells.</p>

<p>Antagonist G is an anticancer peptide and is also a broad spectrum neuropeptide growth factor antagonist.</p>

<p>DPP-4-IN-8 (compound 27) is a potent and selective inhibitor of dipeptidyl peptidase 4 (DPP4), with an inhibition constant (Ki) of 0.96 μM.</p>

<p>MDMX/MDM2-IN-2 is a potent dual inhibitor of p53-MDM2/MDMX, demonstrating dissociation constants (Kis) of 0.23 μM for MDM2 and 2.45 μM for MDMX.</p>

<p>Bleomycin A5, or Pingyangmycin, is an oral glycopeptide antibiotic and acts as an antineoplastic and apoptosis inducer.</p>

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

<p>A unique collection of 193 endoplasmic reticulum stress (ER stress) related compounds used for high throughput screening (HTS) and high content screening (HCS);</p>

<p>KRASG12C IN-16 (Compound SK-17) is a selective, covalent, and orally active KRASG12C inhibitor. It can induce apoptosis and effectively prevent the activation of the MAPK and PI3K/mTOR signaling pathways. Additionally, KRASG12C IN-16 exhibits antitumor activity against pancreatic cancer.</p>

<p>DB818 dihydrochloride is the dihydrochloride salt form of DB818. It acts as an inhibitor of Homeobox A9 (HOXA9). By reducing the formation of the HOXA9-DNA complex, DB818 dihydrochloride inhibits the growth of AML cell lines OCI/AML3, MV4-11, and THP-1 and induces cell apoptosis (apoptosis).</p>

<p>TG101209 analog 1 (Compound 8h) serves as an inhibitor of BUB1B, exhibiting an IC50 of 10.36 μM. It also possesses cytotoxic properties, demonstrated by an IC50 of 1.347 μM against Caki-1 cells, and can induce necrosis and apoptosis.</p>

<p>Bcl-2-IN-4: potent, selective, oral Bcl-2 inhibitor with 1.5 nM IC50, &gt;200x selectivity over Bcl-xL.</p>

<p>Anticanceragent 273 (Compound 9q) is an effective anticancer compound identified from matrine. It inhibits cancer cell proliferation, with an IC50 of 4.48 μM against HeLa cells. Anticanceragent 273 exerts its anticancer effects by modulating PI3K/AKT expression and activating activating transcription factor 4 (ATF4), which induces endoplasmic reticulum stress and triggers apoptosis. It holds potential for cancer research, including cervical cancer.</p>

<p>FW-1 is a type I inhibitor of FLT3, with an IC50 of approximately 1 μM. It exhibits cytotoxic effects in FLT3-mutant AML cells, causes cell cycle arrest at the G0/G1 phase, and induces apoptosis in MV4-11 and MOLM-13 cells.</p>

<p>IC 86621: DNA-PK ATP-competitive inhibitor, IC50 120 nM, enhances DSB antitumor effects, EC50 68 µM for repair.</p>

<p>eIF4E-IN-2 effectively inhibits eIF4e, crucial for research on diseases like cancer.</p>

<p>hCAIX-IN-13 (Pt2) inhibits CAIX with 6.57 μM IC50, curbs cancer cell growth, and induces apoptosis for cancer research.</p>

<p>CDK9-IN-36 (Compound T7) is a potent, selective, and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. It effectively suppresses the proliferation of Osimertinib-resistant NSCLC cells by downregulating Mcl-1, reducing colony formation, and inducing apoptosis. Additionally, CDK9-IN-36 exhibits antitumor activity in xenograft models.</p>

<p>FB49 is a selective Bcl-2-associated athanogene 3 (BAG3) inhibitor with a Ki of 45 μM.</p>

<p>Photosensitizer-3, generates single-linear oxygen upon near-infrared light excitation in combination with FAP,potent and selective killing cancer cells.</p>

<p>3-methoxy-9H-carbazole: photosensitizer, anti-breast cancer, from Klauseneria spp., induces apoptosis.</p>

<p>Thalidomide-based cereblon ligand linked to PROTAC technology as E3 ligase ligand-linker.</p>

<p>NecroIr2, an iridium(III) compound, induces necroptosis in Cisplatin-resistant A549R lung cancer cells and disrupts mitochondria.</p>

<p>NecroIr1, an iridium(III) complex, induces necroptosis in Cisplatin-resistant lung cells, targeting mitochondria and disrupting MMP.</p>

<p>Ropeginterferon alfa-2b (Ropeginterferon alfa-2b-njft), a monopegylated interferon-alpha (IFN-α), is utilized in the study of myeloproliferative neoplasms [1].</p>

<p>XZ338 is a highly selective degrader targeting BCL-XL without degrading BCL-2. It exhibits an IC50 value of 3.7 nM against MOLT-4 cells and possesses antiproliferative properties, making it useful for cancer research.</p>

<p>Pegsunercept (PEG sTNF-RI), a pegylated monoclonal antibody, selectively binds to TNFA, incorporating a polyethylene glycol (pegol) moiety [1].</p>

<p>Chol-CTPP targets the BBB and glioma cells; when combined with Chol-TPP, forms Lip-CTPP, enhancing anti-glioma drug efficacy.</p>

<p>UCM-1336 (3,3′-(Octylimino)bis[N-phenylpropanamide]) is a potent ICMT inhibitor with an IC50 of 2 μM which is selective against the other enzymes involved in</p>

<p>PKM2 modulator 1 (compound C998) is an effective PKM2 inhibitor with antiproliferative activity. It induces apoptosis and holds potential for research in glioblastoma studies.</p>

<p>RO7567132 is a bispecific antibody that binds and agonizes LTBR bivalently while binds and antagonizes FAP monovalently, inducing the formation of local TLS.</p>

<p>HEMTAC CDK4/6 degrader 1, a PROTAC targeting HSP90/CDK4/6, Kd of 35.7 μM, disrupts B16F10 melanoma cell cycle, and induces apoptosis.</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>Apoptosisinducer 27 (compound 1c) is a potent inhibitor of MDA-MB-231 breast cancer cells, demonstrating an IC50 of 12.8 μM and inducing early apoptosis in these cells. Additionally, it can bind to DNA molecules as well as Bax and Bcl-2 proteins, thereby inducing DNA damage.</p>

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

<p>VEGFR-2-IN-64 (Compound 28) is an inhibitor of VEGFR2 with an IC50 of 27.8 nM. It suppresses the proliferation of cancer cells A549, T-47D, and Caco-2, exhibits anti-migration and anti-colony formation activities in T-47D cells, and induces apoptosis in T-47D cells.</p>

<p>cytoplasmic peptide of the neurotrophin receptor p75NTR</p>

<p>Anti-Mouse PD-1 Antibody (D265A) is an IgG2a, κ antibody inhibitor derived from mice, specifically targeting mouse PD-1.</p>

<p>Thalidomide-O-amido-C3-COOH is a cereblon ligand-linker for PROTACs, melding Thalidomide with a standard linker.</p>

<p>Ferroptosisinducer-4 (Compound 5) is a phospholipid-based ferroptosis inducer featuring a terminal double bond at the sn-2 position. It exhibits significant cytotoxicity towards HT-1080 cells with an IC50 value of 18 μM. The toxicity mechanism involves the generation of lipid peroxides and oxidative damage to the cell membrane induced by the terminal double bond. Ferroptosisinducer-4 can be utilized in studies pertaining to the regulation of ferroptosis.</p>

<p>Curzerene, a sesquiterpene compound derived from the rhizome of Curculigo orchioides Gaertn, possesses potent anti-cancer properties.</p>

<p>Fluorescein-diisobutyrate-6-amide, a powerful inducer of ferroptosis, shows promise for cancer research applications [1].</p>

<p>FeTPPS, a decomposition catalyst for 5,10,15,20-tetrakis(4-sulfonatophenyl) porphyrin iron(III) chloride peroxynitrite, neuroprotective.</p>

<p>MDM2/4-p53-IN-2 (2q) is a dual MDM2/MDM4 inhibitor, p53 activator; IC50: 70.7 nM(MDM2), 81.4 nM(MDM4); tumor suppressor.</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>PAK4-IN-3 (compound 27e) is a PAK4 inhibitor exhibiting an IC50 of 10 nM and demonstrates antiproliferative effects on A549 cells with an IC50 of 0.61μM.</p>

<p>Vallesiachotamine, a recognized monoterpene indole alkaloid, exhibits anti-tumor activity [1].</p>

<p>BMSpep-57: Macrocyclic peptide, inhibits PD-1/PD-L1, IC50=7.68 nM, binds PD-L1 (Kd=19 nM/MST, 19.88 nM/SPR), boosts T cell IL-2 in PBMCs.</p>

<p>Thalidomide-O-amido-PEG2-C2-NH2, which combines an E3 ligase ligand with a linker, serves as an immunomodulator for cancer treatment.</p>

<p>TQB-2858 is a bifunctional fusion protein composed of an anti-PD-L1 monoclonal antibody fused with the extracellular domain of the TGF-β receptor. It exhibits high affinity for PD-L1, TGF-β1, and TGF-β3, and demonstrates a high target occupancy rate for PD-L1. TQB-2858 can be used in research on osteosarcoma and alveolar soft part sarcoma (ASPS).</p>

<p>pdTp is a highly selective, small-molecule miRNA regulatory complex RISC subunit SND1 inhibitor.</p>

<p>FTO-IN-14 (Compound F97) is an inhibitor of the RNA demethylase Fat mass and obesity-associated protein (FTO), with an IC50 of 0.45 μM. It modulates the expression of the ASB2, RARA, and MYC proteins. FTO-IN-14 demonstrates antiproliferative activity in AML cancer cells, with IC50 values of 0.7-5.5 μM against MOLM13, NB4, HEL, OCI-AML3, MV4-11, and MONOMAC6, and induces apoptosis in NB4 cells. Additionally, FTO-IN-14 exhibits antitumor activity in a mouse NB4 xenograft model.</p>

<p>PD-166285 is an effective and broadly active inhibitor of protein tyrosine kinase.</p>

<p>NL13, a Polo-like kinase 4 (PLK4) inhibitor, exhibits an IC 50 value of 2.32 μM. It demonstrates the ability to suppress the viability of PC3 and DU145 prostate cancer cells with respective IC 50 values of 3.51 μM and 2.53 μM. NL13 also inhibits tumor growth in prostate cancer mice. Additionally, it deactivates the AKT signaling pathway by reducing CCNB1/CDK1 levels, leading to G2/M cell cycle arrest and initiating apoptosis through caspase-9/caspase-3 cleavage.</p>

<p>Thalidomide-O-C7-acid: A cereblon ligand from Thalidomide linked via a PROTAC-used linker.</p>

<p>AM-8553 is potent and selective piperidine the MDM2-p53 interaction inhibitor.</p>

<p>Nrf2 activator-11 (compound M11) is a Nrf2 activator that possesses blood-brain barrier permeability and offers anti-oxidation, anti-inflammation, anti-ferroptosis, and anti-apoptosis properties. It is applicable for use in studying cerebral ischemia-reperfusion (CI/R) injury models.</p>

<p>c-Met-IN-24 (compound 3g) serves as a dual-target inhibitor for STAT-3 (=4.7 μM) and c-MET (=12.67 μM), exhibiting anticancer properties. It arrests the G2/M cell cycle and induces apoptosis in SNB-75 cells, making it applicable in the research of central nervous system cancers.</p>

<p>Biotin-PEG6-Thalidomide is a PROTAC linker based on PEG.</p>

<p>USP1-IN-11 (compound 38-P2) is a selective, reversible, and non-competitive inhibitor of USP1 (Ubiquitin-specific protease 1). It activates the DDR (DNA damage repair) pathway, leading to cell cycle arrest and apoptosis, thereby inhibiting cell survival. USP1-IN-11 increases sensitivity to Olaparib in drug-resistant cells and works synergistically with Andrographolide in cancer cells with functional BRCA. In the MDA-MB-436 xenograft model, USP1-IN-11 demonstrates significant dose-dependent antitumor activity.</p>

<p>HQY1428 is an orally active CDK12 inhibitor. It impedes DNA replication, causing cell cycle arrest at the G2/M phase in SKOV3 cells, and induces DNA double-strand breaks as well as apoptosis. In the SKOV3 xenograft mouse model, HQY1428 demonstrates antitumor activity. Additionally, when combined with the HER2 inhibitor Lapatinib in the NCI-N87 xenograft mouse model, HQY1428 produces a synergistic therapeutic effect.</p>

<p>Maceneolignan A, a natural product isolated from the aril of Myristica fragrans (Myristicaceae), inhibits β-hexosaminidase release in RBL-2H3 cells, exhibiting</p>

<p>PROTACNCOA4 degrader-1 (Compound V3) is a PROTAC-based degrader of NCOA4, exhibiting a DC50 of 3 nM in HeLa cells. Besides acting as a ferroptosis inhibitor, this compound effectively reduces the levels of NCOA4 and decreases intracellular ferrous (Fe2+) levels. Moreover, PROTACNCOA4 degrader-1 ameliorates liver damage in a CCl4-induced acute liver injury model.</p>

<p>Alkyl phosphates like (E)-C-HDMAPP activate γδ-T cells, resist hydrolysis, and boost TNF-α synthesis and γδ-T cell count in vivo.</p>

<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>CYP51/PD-L1-IN-1 (compound L11), a quinazoline with antifungal properties, simultaneously inhibits CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM).</p>

<p>Cytotoxic and antiproliferative effects of Hellebrin on breast and lung cancer cells.</p>

<p>RBN013209 is a potent CD38 inhibitor. RBN013209 is useful in the treatment of cancer.</p>

<p>7-Methoxy-1-tetralone may have insecticidal activity.</p>

<p>XIAP BIR2/BIR2-3 inhibitor-1 (compound 3) serves as a potent dual inhibitor targeting BIR2 and BIR2-3 domains, with IC50 values of 1.9 nM and 0.8 nM, respectively. This compound is utilized in cancer research studies [1].</p>

<p>PL120131 is a PD-1/PD-L1 inhibitory peptide that disrupts the interaction between PD-1 and PD-L1 by binding to PD-1. This compound can inhibit the apoptosis signaling pathway mediated by PD-1, thereby preventing apoptosis (apoptosis) in Jurkat cells and primary lymphocytes. Additionally, PL120131 supports cytotoxic T lymphocytes (CTL) in exhibiting antitumor activity.</p>

<p>Ledostomig is an immunoglobulin (H-γ1-scFv-L-κ) dimer monoclonal antibody that targets human neurotensin receptor type 5 (NTS5) and programmed death-1 (PD-1). It shows potential for research in various cancer types.</p>

<p>Bcl-2-IN-5: BCL-2 inhibitor, IC50: 0.12 nM (wt), 0.14 nM (D103Y), 0.22 nM (G101V); Cell growth IC50: 0.2 nM, 0.44 nM (RS4;11).</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>AB-3PRGD2 is a radiolabeled agent that targets integrin αvβ3. It enhances tumor uptake and prolongs retention time in tumors, significantly improving the inhibition of tumor growth. AB-3PRGD2 also remodels the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.</p>

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

<p>INF200 (compound 5), a sulfonylurea-based inhibitor of NLRP3 and associated pyroptosis, exhibits cardiometabolic benefits in a rat model of high-fat diet (HFD)-</p>

<p>Ac-Pro-Gly-Pro-OH can be used as a CXCR2 agonist with bactericidal and anti-inflammatory activity for the study of sepsis and lung inflammation.</p>

<p>Ragifilimab (INCAGN-1876), a GITR-targeting agonist antibody, may treat advanced solid tumors.</p>

<p>Negative control for dTAGV-1.</p>

<p>Uvarigrin induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation. Uvarigrin is isolated from the roots of Uvaria calamistrata.</p>

<p>HDAC3-IN-2 (compound 4i), a pyrazinyl hydrazide-based HDAC3 inhibitor with an IC50 of 14 nM, effectively targets triple-negative breast cancer cells.</p>

<p>Mepacrine (Erion) is an acridine derivative formerly widely used as an antimalarial.</p>

<p>Ferroptosis-IN-17 (Compound 18) is an inhibitor of ferroptosis with an EC50 value of 0.57 μM. It effectively reduces the accumulation of intracellular ferrous ions and lipid peroxidation while restoring levels of glutathione (GSH) and glutathione peroxidase 4 (GPX4). In rat plasma, Ferroptosis-IN-17 demonstrates good solubility and notable metabolic stability. This compound holds potential for research in tumor suppression, neurodegenerative diseases, and cardiovascular disorders.</p>

<p>Suramin is an RdRp and PTPase inhibitor with anti-parasitic, anti-tumor, and anti-angiogenic activities, inhibiting sirtuins and DNA topoisomerase II.</p>

<p>KRN 5500, a derivative of the nucleoside antibiotic spicamycin, has a wide range of antitumor activity against human cancer cell lines.</p>

<p>iNOs-IN-5 (Compound BN-4) is an inhibitor of iNOS with an IC50 value of 0.1707 μM, effectively reducing NO expression in RAW264.7 cells stimulated by LPS (HT-D1056). It further diminishes the expression of ROS and lactate dehydrogenase induced by hypoxic injury, displaying anti-necrotic and anti-apoptotic properties. In an SD rat model, iNOs-IN-5 exhibits neuroprotective effects against cerebral ischemia and is capable of crossing the blood-brain barrier.</p>

<p>YF135 is a reversible-covalent KRAS G12C PROTAC that degrades its target via the VHL-proteasome pathway.</p>

<p>PARP1-IN-17 is an inhibitor that targets PARP-1 (IC50=19.24 nM ) with a slightly reduced affinity for PARP-2 (IC50=32.58 nM ) and induces apoptosis.</p>

<p>S65487 (VOB560) sulfate, a potent and selective Bcl-2 inhibitor, demonstrates activity against BCL-2 mutations, including G101V and D103Y.</p>

<p>CQ1373 is a potent RET inhibitor that demonstrates cellular activity against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C, and CCDC6-RET-G810R, with IC50 values of 13.0, 25.7, and 28.4 nM, respectively. It shows excellent selectivity for wild-type RET and solvent front mutants G810C/R, with IC50 values of 4.2, 7.1, and 32.4 nM. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. Additionally, it induces apoptosis (Apoptosis) and cell cycle arrest in BaF3 cells. CQ1373 possesses antitumor efficacy, making it a candidate for cancer research.</p>

<p>Scr-IN-1 (Compound 4e) is a tyrosine kinase inhibitor demonstrating inhibitory activity against HCT-116 and MIA-PaCa-2 cells, with IC50 values of 0.16 μM and 1.16 μM, respectively. It shows selectivity towards HCT-116 cells and MIA-PaCa-2 cells, with a selectivity index (SI) greater than 625 and 86. Scr-IN-1 induces apoptosis in HCT-116 colon cancer cells without altering the proportion of necrotic cells and is a potential novel SRC kinase inhibitor for HCT-116 cells. This compound is suitable for cancer research.</p>

<p>DHFR-IN-23 (compound 5) is a dual inhibitor of DNA binders/DHFR, exhibiting an IC50 value of 0.08 μM against hDHFR. It serves as an apoptosis inducer and is applicable in research on ER+ breast cancer.</p>

<p>FLT3-IN-29 (Compound MY-10) is an FLT3 inhibitor with IC50 values of 6.5 nM and 10.3 nM for FLT3-ITD and FLT3-D835Y mutants, respectively. It induces cell cycle arrest at the G0/G1 phase and effectively triggers apoptosis (Apoptosis). Additionally, FLT3-IN-29 reduces reactive oxygen species (ROS) and mitochondrial membrane potential (MMP), displaying anti-leukemic properties.</p>

<p>Lisaftoclax, an oral Bcl-2/Bcl-xl inhibitor (IC50: 2 nM &amp; 5.9 nM), treats CLL by promoting leukemia cell death.</p>

<p>Haemanthamine hydrochloride, an alkaloid from Amaryllidaceae, has anticancer, antioxidant, antiviral, antimalarial, and anticonvulsant properties.</p>

<p>Necroptosis-IN-5 (Compound 26) is an orally active inhibitor of necroptotic cell death (necroptosis). This compound also exhibits potent inhibitory activity against receptor-interacting protein kinase 1 (RIPK1). It can be utilized in research related to inflammatory diseases, neurodegenerative disorders, and cancer associated with necroptosis.</p>

<p>FLT3-IN-21 (compound LC-3), a potent FLT3 inhibitor with an IC50 value of 8.4 nM, induces apoptosis and arrests the cell cycle in the G1 phase.</p>