Apoptosis

<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>PK095 is a proprietary compound in the guanidine - based F1F0-ATPase inhibitor family.</p>

<p>Z-Ala-Ala-Asp-CMK (Z-AAD-CMK) is a selective granzyme B inhibitor that blocks granzyme B protease activity, for inflammatory diseases and tumours.</p>

<p>Conophylline, an alkaloid from Ervatamia microphylla, induces pancreatic cell differentiation and apoptosis, and suppresses HSC.</p>

<p>KB03-SLF is a protease with the capability to target specific proteins and regulate intracellular protein levels by inducing protein degradation. This mechanism renders KB03-SLF potentially valuable in the suppression of related diseases.</p>

Glutathione arsenoxide hydrochloride: anti-cancer, inhibits tumour metabolism, targets ANT, promotes apoptosis, marks cell proteins.

<p>Ianalumab (VAY-736) is a decarboxylated humanized antibody against BAFF-R.</p>

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

<p>Streptonigrin, from Streptomyces flocculus, has anti-tumor and anti-bacterial properties, inhibiting PAD1-4.</p>

6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile is a PDK1 inhibitor with anticancer and antiproliferative activity that can be used to study

<p>spisulosine is a natural product for research related to life sciences. The catalog number is T9664 and the CAS number is 196497-48-0.</p>

<p>Citreoviridin from Penicillium citreoviride blocks brain Na+/K+-ATPase; boosts Na+/K+- and Mg2+-ATPase in microsomes dose-dependently.</p>

<p>Phospholipid with stearic acid and 15(S)-HpETE boosts ferroptosis in MEFs upon GPX4 inhibition.</p>

<p>Fludioxonil (CGA 173506), a phenylpyrrole fungicide, inhibits the growth of B. cinerea from strawberry and blackberry crops.</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>

<p>Aspochalasin D, isolated from A. microcysticus, shows antibacterial properties and cytotoxicity affecting Ba/F3-V12 cells, with IC50s of 0.49 and 1.9 μg/ml.</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>

PROTAC-O4I2, a PROTAC ligand targeting splicing factor 3B1 (SF3B1), induced FLAG-SF3B1 degradation in K562 cells with an IC50 value of 0.244 μM.

<p>Δ8-Tetrahydrocannabinoquinone (HU-336) is a potent anti-angiogenic agent that inhibits angiogenesis by directly inducing apoptosis in vascular endothelial cells. It achieves this without altering the expression of pro-angiogenic and anti-angiogenic cytokines and receptors. Δ8-Tetrahydrocannabinoquinone also shows significant effectiveness against tumor xenografts in nude mice.</p>

Apoptosis Inducer 29 (compound Y9) demonstrates anticancer efficacy in non-small cell lung cancer by inducing lysosomal dysfunction and apoptosis, and exhibits superior performance to Gboixn both in vitro and in vivo.

<p>2-deoxy-D-Glucose-13C6 is an internal standard for GC/LC-MS, a glycolysis inhibitor, and induces apoptosis in certain cells at 2 mg/ml.</p>

<p>BKM1644 is an effective inhibition of the proliferation of metastatic, castration-resistant PCa (mCRPC) cells.</p>

FOXJ1 agonist 1 (compound 16c), an orally effective small molecule, effectively enhances FOXJ1 expression and acts on multiciliated cells (MCC) in the mammalian airway system to prevent chronic obstructive pulmonary disease (COPD). Foxj1-IN-1 induces motile cilia production in the respiratory system of both zebrafish and mammals and inhibits elastase-induced COPD in mouse models. Additionally, Foxj1-IN-1 demonstrates good liver microsomal stability and favorable in vivo pharmacokinetic (PK) curves and area under the curve (AUC). It exhibits negligible inhibition of CYP and hERG and lacks significant cytotoxicity.

<p>Solanidine is a cholestane alkaloid isolated from potato species with antitumor effects. Solanidine inhibits proliferation.</p>

<p>Oxidosqualene cyclase inhibitor</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>2-Chloronaphthalene is an organochlorine chemical compound and is a chlorinated derivative of naphthalene. The compound is an isomer for 1-chloronaphthalene.</p>

<p>Anti-Mouse PD-L1 Antibody (10F.9G2) is an IgG-class antibody against mouse PD-L1.</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>

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

<p>SPOP-IN-6lc is a SPOP inhibitor with oncogenic effects in renal cancer cells.SPOP-IN-6lc can be used to study apoptosis.</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>Latikafusp (AMG 256) is a fusion protein that is a PD-1 blocker and IL-21R agonist with antitumor activity.</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>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>CDK9-IN-24 (compound 21a) is a potent and selective inhibitor of CDK9 that exhibits a pronounced inhibitory impact on tumor proliferation.</p>

<p>Poly (I:C):Kanamycin (1:1) is an equimolar mixture of Poly(I:C) and kanamycin. TLR3 agonist commonly used as a vaccine adjuvant; enhanced Poly(I:C) stability.</p>

<p>Arisostatin A is a secondary metabolite produced by microorganisms, recognized as an antibiotic (antibiotic) with activity against Gram-positive bacteria. This compound also exhibits potent antitumor properties. It induces apoptosis (apoptosis) by activating caspase-3 and generating reactive oxygen species (ROS) in AMC-HN-4 cells.</p>

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

<p>(±)-Indoxacarb is a pyrazoline insecticide with insecticidal activity and cytotoxicity, blocks sodium channels in insect neurons, and can induce apoptosis.</p>

<p>C188, a naphthol-based STAT3 inhibitor, blocks IL-6-induced STAT3 activity in HepG2 cells, sparing STAT1.</p>

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

<p>Lw13 is a PROTAC targeting Hsp90, exhibiting maximal degradation efficacy at a concentration of 0.05 μM in Siha cells. Lw13 induces apoptosis and demonstrates potent antitumor activity both in vitro and in vivo.</p>

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

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

<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>Cereblon ligand for PROTAC R&amp;D; has E3 ligase, alkylC1-PEG3-alkylC3 linker, terminal amine. Part of Arvinas-licensed tool molecules.</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.

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

<p>CAY10726, an arylurea fatty acid, cuts ATP by 28% and promotes apoptosis in breast cancer cells by depleting mitochondrial lipids.</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>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>SF1126 is a first-in-class PI3K/BRD4 inhibitor and RGDS-conjugated LY294002 prodrug, enhancing solubility and targeting tumor integrins.</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>Zigakibart (BION-1301) is a humanized monoclonal antibody targeting TNFSF13 with anti-inflammatory activity for the study of immunoglobulin A nephropathy (IgAN)</p>

<p>Tubulin polymerization-IN-72 (Compound 4a4) is a microtubule synthesis inhibitor with anticancer properties. By binding to the colchicine site, it disrupts the polymerization of tubulin, resulting in the arrest of cancer cells at the G2/M phase and inducing apoptosis (Apoptosis). The IC50 for its activity against cancer cells is 0.4-2.7 nM.</p>

<p>p38α inhibitor6 (compound 19) is a p38α inhibitor with an IC50 value of 0.68 μM. It induces apoptosis, arrests the cell cycle in the G0 and G2/M phases, reduces TNF-α concentration, upregulates the expression of the tumor suppressor gene p53, increases the Bax/BCL-2 ratio, and activates caspase3/7.</p>

<p>SI-2, a SRC-3 inhibitor, triggers breast cancer cell death (IC50: 3-20 nM), sparing normal cells.</p>

<p>Ferroptosis-IN-16 (Compound 13l) acts as a specific inhibitor of ferroptosis, demonstrating EC50 values of 0.7 nM in ES-2 cells and 0.9 nM in LX-2 cells. It effectively alleviates acute liver injury induced by Acetaminophen in mouse models and shows excellent metabolic stability in mouse liver microsomes.</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>(E/Z)-10-Hydroxy-2-decenoic acid is a useful organic compound for research related to life sciences.</p>

NQO2-IN-1, a resveratrol analog, is a potent NQO2 inhibito,antitumor,generation of ROS and up-regulation of DR5 (death receptor 5) to promote apoptosis.

<p>Rozanolixizumab (RYSTIGGO) is a humanized IgG4 monoclonal antibody that targets FcRn in newborns for autoimmune research.</p>

<p>RvD2 n-3 DPA is an SPM made from docosapentaenoic acid in human leukocytes, inhibiting neutrophil chemotaxis and adhesion.</p>

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

<p>(R)-JAK2/STAT3-IN-10a is the R-isomer of JAK2/STAT3-IN-1.JAK2/STAT3-IN-1 is a structural domain inhibitor of GP130 D1 with antitumor activity.</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>LIB3S0280 is a potent inhibitor of TBK1, with an IC50 of 493.9 nM. It suppresses TBK1 downstream signaling by reducing the phosphorylation of IκBα and AKT. LIB3S0280 causes G2/M phase arrest and induces apoptosis in pancreatic cancer cells. Notably, it exhibits significant inhibitory effects on pancreatic cancer cell lines with high TBK1 expression, with a 96-hour IC50 value ranging from 6.64-10.98 μM. LIB3S0280 shows potential for research in pancreatic ductal adenocarcinoma (PDAC).</p>

Photosensitizer-5, a photodynamic agent, exhibits cytotoxicity towards HeLa and HepG2 cells, with IC50 values of 10.4 nM and 6.9 nM, respectively. It induces cell death through lipid peroxidation via an iron-independent ferroptosis pathway. Additionally, Photosensitizer-5 displays antitumor activity in HeLa-tumor-bearing mice.

<p>KC01 selectively inhibits ABHD16A (IC50: 0.2-0.5 μM), much more potent than KC02 (&gt;10 μM); human ABHD16A IC50: 90±20 nM.</p>

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

Mcl-1 antagonist 1 is a Mcl-1 protein antagonist.

<p>ChoKα Inhibitor-4 is a bioisosteric agent that effectively inhibits human choline kinase α1 (HChoK α1) with an IC50 of 0.66 μM.</p>

<p>DTUN: lipophilic radical initiator, starts STY-BODIPY liposome co-autoxidization at 0.2 mM, useful in FENIX assays.</p>

anti-TNBC agent-1 targets TNBC effectively, with IC50 of 0.20-0.27 μM, inducing apoptosis and G1 arrest in SUM-159 cells.

<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>Carubicin, an anthracycline antibiotic from Actinomadura carminata, disrupts DNA replication and repair by intercalating DNA and inhibiting topoisomerase II.</p>

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

<p>Siomycin A: thiopeptide antibiotic, selectively inhibits FOXM1, anti-tumor, induces apoptosis.</p>

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

<p>DRI-C21041 DIEA serves as an inhibitor of CD40/CD40L interaction, exhibiting an inhibitory concentration (IC50) of 0.31 μM.</p>

<p>Dc-y13-27, a derivative of DC-Y13, is a potent YTHDF2 inhibitor (KD: 37.9 μM).</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>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>

<p>CSN5-IN-2 (Compound 31) is a CSN5 inhibitor with an IC50 of 0.36 μM. It increases Cullin 1 neddylation levels in cancer cells and downregulates the expression of RAD51 and PD-L1. CSN5-IN-2 exhibits antitumor activity, which is enhanced when used in combination with Talazoparib.</p>

<p>EM 163是一种 TIR-TIR 相互作用抑制剂，它是MyD88蛋白的TIR（Toll/白细胞介素-1受体）结构域拟态。EM 163针对IL-1受体中的TIR 结构域，阻断与MyD88的相互作用。EM 163抑制葡萄球菌肠毒素B（SEB）引起的体内炎症细胞因子的产生。EM 163能保护小鼠免受SEB 冲击引起的死亡。在体外的大鼠海马神经元中，EM 163阻断p38的激活和IL-1β对化学诱导的长期电位（LTP）引发的蛋白质合成的抑制作用。</p>

<p>Ajoene from garlic has antibacterial, anticancer, antiplatelet, and antioxidant effects; it combats various bacteria, yeasts, and cancer cells.</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>Calcimycin (A-23187) is an antibiotic calcium ionophore that raises intracellular Ca2+ to induce cell death.</p>

<p>Human membrane-bound PD-L1 polypeptide serves as an antigen for inducing the production of PD-L1 antibodies [1].</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>EGCG-4″-sulfate, a predominant polyphenol in green tea, demonstrates notable anticancer, antioxidant, and anti-inflammatory effects, particularly against</p>

<p>CXCR4-IN-2 (compound A1), a potent bifunctional fluorinated small molecule, inhibits CXCR4 and exhibits anticancer properties by exerting cytotoxicity (IC 50:</p>

<p>NC-R17, an RSL3-based noncovalent GPX4 degrader implicated in ferroptosis, demonstrates anti-tumor activity and is utilized in the design of noncovalent GPX4-</p>

<p>Thalidomide-based E3 ligase ligand linked to a PROTAC piperazine-piperidine chain.</p>

<p>HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4</p>

<p>(R)-1-(2-((2-MeO-4-(piperazin-1-yl)phenyl)amino)pyridin-4-yl)-N-(4-(CF3O)benzyl)piperidine-3-carboxamide HCl is anti-apoptotic and anti-cancer.</p>

<p>Gemcitabine monophosphate disodium salt is a monophosphate derivative of Gemcitabine.</p>

<p>(+)-Mcl-1 inhibitor 22 (Example 37) is an MCL-1 inhibitor that impedes the anti-apoptotic function of MCL-1 by blocking its interaction with pro-apoptotic proteins. It demonstrates antiproliferative activity against various cancer cell lines and is applicable for cancer research.</p>

<p>(Iso)-Z-VAD(OMe)-FMK is an isomer of Z-VAD(OMe)-FMK, which is a pan-caspase inhibitor with irreversible properties. Z-VAD(OMe)-FMK is also an inhibitor UCHL1.</p>

<p>RET-IN-26 (compound D5) is a kinase inhibitor that selectively targets the RET protein with an IC50 value of 0.33 μM [1].</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>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>