Apoptosis

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

<p>Rasagiline (AGN1135) is an inhibitor of monamine oxidase used as adjunctive therapy in combination with levodopa and carbidopa in the management of Parkinsons</p>

<p>EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.</p>

<p>Caspase-3 activator 3 (compound 2h) effectively induces apoptosis in HL-60 and K562 cells by substantially activating caspase-3, demonstrating antileukemic</p>

<p>GSK-3β inhibitor 15 (Compound 54), with an IC50 of 3.4 nM, effectively suppresses Aβ 1-42-induced phosphorylation of GSK-3β and tau protein, as well as LPS-</p>

<p>UM4118 (N-quinolin-8-ylpyridine-2-carboxamide) is a copper ion carrier used in the study of acute myeloid leukemia.</p>

<p>Moracin N, a ferroptosis inhibitor derived from mulberry leaves, exhibits neuroprotective activity by mitigating oxidative stress [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>Salinomycin sodium salt (Sodium salinomycin), an antibiotic potassium ionophore, is an effective inhibitor of Wnt/β-catenin signaling.</p>

HSP90-IN-33 (compound 24e) is an effective Hsp90 inhibitor, demonstrating dissociation constants (Kd) of ≥200 µM for Hsp90α and 7.3 µM for Hsp90β. This compound induces cellular apoptosis (apoptosis) and arrests the cell cycle at the G0/G1 phase. Additionally, HSP90-IN-33 reduces the protein expression of ERα, CDK4, and Akt.

<p>YL5084 is a selective JNK2/3 inhibitor with IC50s: JNK2 (70 nM), JNK3 (84 nM), and antiproliferative, apoptosis-inducing effects.</p>

<p>Barakol, a primary compound found in Cassia siamea, inhibits MMP-3 activity and enhances the anti-metastatic effects of doxorubicin. Additionally, Barakol induces apoptosis (Apoptosis), generates reactive oxygen species, increases the Bax/Bcl-2 expression ratio, and activates caspase-9. This compound also exhibits laxative, anti-anxiety, central nervous system depressant, antioxidant, and anticancer properties.</p>

<p>Thalidomide-O-amido-C4-N3 (Cereblon Ligand-Linker Conjugates 4) is an E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and</p>

STK17A/B-IN-1 hydrochloride is a potent, selective, orally active inhibitor of STK17A/B, displaying an IC50 value of 23 nM against STK17A. It is utilized in the research of tumors.

<p>CQ-ER is a Coumarin-quinazolinone-based photosensitizer targeting the endoplasmic reticulum (ER). It induces ferroptosis, thereby enhancing photodynamic therapy (PDT).</p>

<p>1,2-Naphthoquinone inhibits urease, induces apoptosis in PBMC cells, inhibitory activity against hiCE, hCE1, hAChE, and hBChE.</p>

Asaretoclax is an effective inhibitor of B-cell lymphoma 2 (Bcl-2), demonstrating potential for use in cancer research.

<p>Pipernonaline is a useful organic compound for research related to life sciences. The catalog number is T124000 and the CAS number is 88660-10-0.</p>

<p>P53/TLR2 modulator-1 (Compound Z9) is an agent that targets both the P53 pathway and TLR2, exhibiting radioprotective properties. It mitigates apoptosis by inhibiting radiation-induced expression of P53 and Bax. Concurrently, it enhances the TLR2 pathway by upregulating downstream proteins MyD88 and P65, which promotes secretion of cytokines like IL-6, providing radioprotective effects. P53/TLR2 modulator-1 shows significant radioprotective activity in AHH-1 and HUVECs cells, enhances survival rates in C57BL/6J mice exposed to lethal radiation doses, and alleviates radiation-induced damage to their hematopoietic system, intestinal villi, and spleen. It is applicable for research on radiation-related diseases.</p>

<p>EGFR-IN-144 (Compound 4B) inhibits EGFR (IC50=0.639 µg/mL) and tubulin polymerization (IC50=7.339 µg/mL). It exhibits cytotoxicity in various cancer cells with a GI50 at the nanomolar level. EGFR-IN-144 reduces the expression of mTOR, TNF-α, and IL-6, causes G1/S phase cell cycle arrest, and induces apoptosis.</p>

<p>Thalidomide-NH-(CH2)2-NH2 TFA is an alkyl-modified derivative of Thalidomide serving as a Cereblon ligand to recruit CRBN proteins and a pivotal intermediate in</p>

LBM22, a CLK2 inhibitor, exhibits an IC50 value of 3.9 nM. It possesses anti-proliferative properties by inhibiting the phosphorylation of SR proteins. Additionally, LBM22 downregulates the expression of Wnt-related proteins and anti-apoptotic proteins, making it applicable in the study of non-small cell lung cancer.

<p>PPIA-IN-1 (Compound 20b) is an inhibitor of peptidyl-prolyl isomerase A (PPIA) with a KD of 0.52 μM. It demonstrates antiproliferative activity across various cancer cell lines, including an IC50 of 0.69 μM in HCT116 cells, induces cell cycle arrest at the G0/G1 phase, and exhibits antimetastatic effects in HCT116 cells. PPIA-IN-1 elevates ROS levels, causing DNA damage, ER stress, and mitochondrial dysfunction, and induces apoptosis in HCT116 cells via the MAPK pathway. Additionally, PPIA-IN-1 shows antitumor activity in a CT26 xenograft mouse model.</p>

<p>BIO8898: potent CD40-CD154 inhibitor, IC50 of 25 µM, prevents CD40L-induced apoptosis.</p>

<p>Sarglaroids F (compound 6), an anti-inflammatory agent extracted from the roots of Grass Coral, suppresses LPS/ATP-induced IL-1β secretion by modulating K+</p>

<p>Raptinal activates caspase-3 directly and initiates intrinsic caspase-dependent apoptosis pathway in multiple cell lines.</p>

<p>EGFR-IN-143 (Compound 5f) is a potent EGFR inhibitor with an IC50 value of 0.15 μM. It induces apoptosis by arresting the cell cycle at the G2/M phase and exhibits antitumor activity.</p>

<p>MDM2ligand 4 is a ligand of MDM2 and can be used in the synthesis of the PROTAC degrader [KT-253].</p>

<p>15-acetoxyscirpenol: ASM that induces apoptosis, inhibits Jurkat T cell growth dose-dependently, and activates caspases other than caspase-3.</p>

<p>Bcl-2-IN-15 (Compound 13d) is a Bcl-2 inhibitor with an IC50 of 363 nM, which impedes the proliferation of the NCI leukemia cancer cell line [1].</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>

GPX4-IN-6 is a GPX4 inhibitor with antitumor activity.GPX4-IN-6 induces iron death and is used for the treatment and prevention of triple-negative breast cancer

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

<p>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.</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>Prodigiosin hydrochloride is a bioactive red pigment from bacteria with antibacterial, antifungal, anticancer properties, and inhibits Wnt/β-catenin.</p>

<p>JC2-11 is an anti-inflammatory agent blocking NLRC 4, AIM 2, ROS production, caspase-1 activity, and reducing GSDMD, IL-1β, and LDH in vesicles.</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>DP-15 acts as a degrader of GSPT1 and BRD4, with DC50 values of 5.25 nM and 0.48 nM, respectively. This compound exhibits antiproliferative activity in AML and NHL cells, showing IC50 values in the nanomolar range, induces G1 phase cell cycle arrest, and triggers apoptosis in MOLM13 cells. Additionally, DP-15 demonstrates anti-leukemic properties in the MOLM-13 xenograft mouse model. [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonThalidomide-5-OH]</p>

<p>CQ627 is a molecular glue that targets the degradation of RIOK2. It effectively recruits the E3 ubiquitin ligase RNF126, inducing the proteasomal degradation of RIOK2 via the ubiquitin-proteasome system (UPS) in MOLT4 leukemia cell lines, with a DC50 value of 410 nM. Additionally, CQ627 induces apoptosis in a dose-dependent manner in these cells, blocking the cell cycle at the G2/M phase, and exhibits antiproliferative activity across various cancer cell lines. It also demonstrates in vivo anticancer activity in MOLT4 xenograft mouse models.</p>

<p>(+)-Mcl-1 inhibitor 21 (Example 1-37) is a chemical compound that acts as an Mcl-1 inhibitor with an IC50 value of 172 nM. It demonstrates pro-apoptotic and antiproliferative activities in SUDHL5 and SUDHL10 cell lines, making it useful for cancer research.</p>

WR-S-462 is a STAT3 inhibitor. It effectively blocks the phosphorylation and biological functions of STAT3 in vitro. The IC50 of WR-S-462 for inhibiting MDA-MB-231 cells is 0.03 μM, and it exhibits a strong binding affinity for STAT3 protein with a Kd of 58 nM. WR-S-462 prevents the nuclear translocation of p-STAT3 and selectively inhibits the expression of p-STAT3Tyr705 in MDA-MB-231 cells, as well as the expression of downstream target genes regulated by STAT3, such as Cyclin D1, Bcl-2, and Bcl-xl. This compound inhibits the growth and metastasis of triple-negative breast cancer (TNBC).

<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>

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

<p>EMB-02 is a bispecific antibody targeting both PD-1 and LAG-3. It inhibits the downregulation of T cell activation and proliferation mediated by PD-1 and LAG-3, showing potent anti-cancer properties.</p>

YTHDF2-IN-1 (Compound CK-75) is an inhibitor of YT521-B homology domain family 2 (YTHDF2) with a dissociation constant (Kd) of 26.2 μM, and it effectively blocks the interaction between YTHDF2 and m6A RNA. It suppresses colony formation in JAR cells and exhibits antiproliferative activity in various cancer cell lines, with an IC50 in the micromolar range. Additionally, YTHDF2-IN-1 induces apoptosis in K562 cells and causes cell cycle arrest at the G0/G1 phase.

<p>Tebentafusp (IMCgp100) is a protein that targets gp100 with potential anti-tumor activity.</p>

Asudemotide is a bioactive chemical.

<p>H-20 is a PD-1 agonist that reduces the required dosage of morphine for analgesia. It can be used in studies related to chronic pain.</p>

<p>CYP51/PD-L1-IN-2 (compound L20), a quinazoline with antifungal properties, is a potent dual inhibitor targeting both CYP51 (IC50: 0.263 μM) and PD-L1 (IC50: 0.</p>

<p>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.</p>

<p>Cytostatin: natural antitumor, inhibits cell adhesion, blocks melanoma, induces apoptosis, targets PP2A selectively, IC50s: 1.3-3.1 µg/ml &amp; 29 nM.</p>

<p>RMC-4998 formic is an orally active inhibitor targeting the GTP-bound state of the KRASG12C mutant. It forms a trimeric complex with intracellular CYPA and the activated KRASG12C mutant, displaying an IC50 value of 28 nM. This compound inhibits ERK signaling and induces apoptosis in KRASG12C mutant cancer cells and is utilized in tumor research.</p>

<p>DPH: antihistamine for cough, nausea, itching, allergy, Parkinson's, sleep aid, cold remedy.</p>

<p>Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and</p>

<p>ADAM-17 (TACE) and MMP inhibitor; attenuates TNF-α processing. Acts in concert with GM6001 to inhibit Chlamydia trachomatis growth.</p>

<p>Mcl-1 Inhibitor 16 (Compound 9), a platinum-based mitochondrial-targeting agent, inhibits Mcl-1 and induces Bax/Bak-dependent apoptosis in cancer cells.</p>

<p>Ecdysone is a major steroid hormone in insects and herbs.</p>

<p>CV-4-26 (Compound 22) acts as a covalent inhibitor of TEAD. By inhibiting YAP/TEAD-driven transcription, it diminishes the expression of CTGF and CYR61. Furthermore, CV-4-26 impedes colony formation in Huh7 and HepG2 cells, inducing cell cycle arrest and apoptosis (apoptosis). This compound demonstrates anti-tumoral activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB).</p>

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

<p>Hydrocinchonine is an Alkaloid from Olea europaea and is found in fruits.</p>

<p>Caspase-3 inhibitor. Inhibits MG 132-induced small cell lung cancer cell death in vitro.</p>

<p>Giloralimab (ABBV-927) is a antibody targeting CD40 with anticancer activity for the study of triple-negative breast cancer and non-small cell lung cancer.</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>Dc-y13-27, a derivative of DC-Y13, is a potent YTHDF2 inhibitor (KD: 37.9 μM).</p>

<p>Chloranil (tetrachloro-p-benzoquinone) induces inflammation and neurological dysfunction and can be used to model inflammation in mice.</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>Hypoxia inducer-1 (Compound N6) is a NO donor compound that is orally active and activated under hypoxic conditions. It exhibits high selectivity in releasing NO, inhibiting apoptosis, necrosis, and elevated levels of reactive oxygen species (ROS) associated with hypoxia. It modulates vasodilation and shows protective effects in a mouse model of myocardial hypoxic injury, making it useful for coronary heart disease research.</p>

<p>HKB99 suppresses NSCLC growth, metastasis, and overcomes erlotinib resistance.</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>Negative control for dTAGV-1.</p>

<p>"Urelumab (BMS-66513), a humanized IgG4 mAb CD137 agonist, boosts T-cell/NK cell-mediated cytotoxicity and anti-tumor activity."</p>

<p>AVJ16 as a member of the insulin growth factor 2 mRNA-binding protein family, binds to the mRNA of certain genes to regulate protein translation.</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>Rat form of the beta-Amyloid (1-40) peptide</p>

<p>CDK/HDAC-IN-4 is a highly selective dual inhibitor of cyclin-dependent kinase (CDK) and histone deacetylase (HDAC), with IC50 values of 88.4 nM and 168.9 nM, respectively. This compound exhibits antiproliferative effects in both hematologic and solid tumor cells. Additionally, CDK/HDAC-IN-4 induces apoptosis and S-phase cell cycle arrest in MV-4-11 cells. It has also demonstrated significant antitumor efficacy in an MV-4-11 xenograft model.</p>

<p>Bcl-2-IN-22 (compound 1), a gold (I) NHC complex, exhibits anticancer activity. It induces cell death (apoptosis) via the mitochondrial pathway with an IC50 value of 0.014 μM. Additionally, Bcl-2-IN-22 targets members of the BCL-2 family, promoting apoptosis and sensitization in multidrug-resistant leukemia cells overexpressing BCL-2.</p>

<p>Polyphyllin G (Polyphyllin VII), the the main member of polyphyllin family, shows strong anticancer activity against several carcinomas.</p>

<p>ZZM-1220, a covalent inhibitor of histone lysine methyltransferase G9a/GLP, exhibits IC50 values of 458 nM for G9a and 924 nM for GLP.</p>

<p>Src Inhibitor4 (Compound 18) is a derivative of KX-01 and functions as a Src inhibitor. It effectively disrupts tumor cells, damages microtubules, and induces cell cycle arrest, apoptosis, and immunogenic cell death. After introducing phenol or aniline functional groups, Src Inhibitor4 serves as a payload conjugation site for antibody-drug conjugates, showcasing antitumor activity.</p>

<p>TNF-α (31-45), human is a peptide of tumor necrosis factor-α.</p>

<p>Inuviscolide induces apoptosis, G2/M arrest in melanoma, and has anti-cancer, anti-inflammatory effects.</p>

<p>Thalidomide-O-amide-C5-NH2 is a synthetic E3 ligase linker combining cereblon ligand and PROTAC linker.</p>

<p>1-Alaninechlamydocin, a fungal metabolite from Tolypocladium sp., inhibits HDACs and reduces cell proliferation with GI50s 5.3-14 nM.</p>

<p>(D)-PPA 1 TFA is a hydrolysis-resistant D-peptide antagonist and a potent PD-1/PD-L1 inhibitor, exhibiting an affinity for PD-1 of 0.51 μM and demonstrating</p>

<p>RMC-9805(Zoldonrasib) is a KRAS G12D inhibitor with anti-tumor and anti-proliferative activity for the study of pancreatic cancer.</p>

<p>ACBI3 is a pan-KRAS degrader with anticancer activity, degrading oncogenic KRAS.</p>

<p>Cuprichydroxide exhibits inhibitory activity against Ralstonia solanacearum and A549 cells and has acute pulmonary toxicity.</p>

<p>STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) is a PROTAC degrader targeting signal transducer and activator of transcription 3 (STAT3). It demonstrates anti-tumor activity with IC50 values of 1335 nM in HeLa cells and 1973 nM in MCF-7 cells. The compound binds to the DNA binding domain of STAT3, recruits the E3 ligase VHL to form a ternary complex, leading to ubiquitination and subsequent proteasomal degradation of STAT3. Additionally, STAT3-D11-PROTAC-VHL inhibits tumor cell growth, induces cell cycle arrest and apoptosis (apoptosis), and suppresses tumor immune evasion.</p>

<p>Tubulin/AKT1-IN-1 (Compound D1-1) serves as an inhibitor of both tubulin polymerization and AKT pathway activation, effectively suppressing proliferation and</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>Cardanol (C15:1), found in cashew nut shell liquid, induces mitochondria-associated apoptosis in human melanoma cells.</p>

Diethylnorspermine HCl (N1,N11-Diethylnorspermine tetrahydrochloride) potently induces SSAT (spermidine/spermine N1-acetyltransferase) mRNA and effectively

<p>HDAC6-IN-22 (compound 30), an HDAC6 inhibitor, exhibits an IC50 of 4.63 nM and demonstrates antiproliferative effects against multiple myeloma both in vitro and</p>

<p>Zigakibart (BION-1301) is a humanized monoclonal antibody targeting TNFSF13 with anti-inflammatory activity for the study of immunoglobulin A nephropathy (IgAN)</p>

<p>Anticanceragent 267 (Compound 5q) serves as an activator of RIPK3 and MLKL. It effectively inhibits the proliferation of several cancer cell lines, with IC50 values of 9.79, 10.77, and 5.94 μM for MDA-MB-231, MDA-MB-486, and MCF-7, respectively. The compound induces cell cycle arrest at the subG1 phase and triggers necroptosis in MDA-MB-231 cells. Additionally, Anticanceragent 267 demonstrates antitumor activity in mouse xenograft models.</p>

TopoII/tubulin-IN-1 (Compound 1B8) is an inhibitor of TopoII/tubulin. It effectively suppresses the proliferation of tumor cells and reduces ROS levels, while inducing apoptosis and cell cycle arrest, without showing significant cytotoxicity to normal cells. TopoII/tubulin-IN-1 exhibits antitumor activity.

<p>Antitumor agent-196 (Compound 6a (β, β, β)) is an artemisinin-based oligomer with anticancer properties, exhibiting an IC50 of 90 nM against MCF-7 breast cancer cells. This compound induces apoptosis by modulating the Bax-caspase 3 signaling pathway and triggers ferroptosis by regulating key signaling molecules (including GPX4). Antitumor agent-196 shows potential for cancer research applications.</p>

<p>JAK-IN-40 (Compound 46) is an inhibitor of JAK, effectively targeting JAK1, JAK2, and JAK3 with IC50 values of 0.022, 0.759, and 1.601 μM, respectively. It reduces the phosphorylation of STAT3 and inhibits the proliferation of cancer cells Ba/F3 and JAK1-TEL Ba/F3 with GI50 values of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle progression at the G2/M phase in H1975 and H2087 cells, leading to apoptosis. Additionally, JAK-IN-40 exhibits a synergistic anti-tumor effect when used in combination with Osimertinib.</p>