Apoptosis

<p>(Rac)-Idroxioleic acid (2-Hydroxyoleic acid) sodium is a synthetic derivative of oleic acid (OA) that binds to the plasma membrane, altering lipid composition. This compound exhibits antitumor properties.</p>

<p>PI3Kα-IN-8 is a selective inhibitor of PI3Kα (IC50: 0.012 μM).</p>

<p>Bomedemstat (IMG-7289) hydrochloride, an oral LSD1 inhibitor, has anticancer properties, blocking cell growth and triggering apoptosis.</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>Top/HDAC-IN-3 (Compound 31) is a dual inhibitor of Topoisomerase and HDAC with oral activity. It induces DNA damage by elevating reactive oxygen species (ROS) levels, consequently inhibiting the clonal formation and migration of cancer cells, and triggering apoptosis (Apoptosis) and cell cycle arrest. Top/HDAC-IN-3 demonstrates a significant antitumor effect in NSCLC models, exhibiting a tumor growth inhibition (TGI = 77.5%, 100 mg/kg) superior to that of the HDAC inhibitor SAHA and the combination of SAHA with the topoisomerase inhibitor Irinotecan.</p>

<p>MA242 free base is a dual MDM2/NFAT1 inhibitor that triggers apoptosis in pancreatic cancer cells.</p>

<p>ZLWT-37: Oral CDK inhibitor, CDK9 IC50=0.002 µM, CDK2 IC50=0.054 µM; halts HCT116 cells at G2/M, induces apoptosis.</p>

<p>MTX-216 is an ATP-competitive inhibitor targeting both PI3K and EGFR. It simultaneously inhibits Ki-67 and ribosomal S6 phosphorylation, inducing apoptosis in NF1LOF cells. Additionally, MTX-216 suppresses SYK kinase activity with an IC50 of 281 nM. This compound is applicable for melanoma research.</p>

<p>Topoisomerase I/II inhibitor 3 suppresses cell growth and induces apoptosis in liver cancer by blocking PI3K/Akt/mTOR.</p>

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

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

<p>Mps-BAY1, an MPS1 inhibitor, exhibits anticancer activity. It inhibits cell proliferation and induces cell apoptosis by activating mitotic aberrations in cancer cells, leading to overall aneuploidy and polyploidy. Mps-BAY1 is used in research pertaining to colorectal and cervical cancer.</p>

<p>HSP90-IN-10 is a potent HSP90 inhibitor, targeting HCC1954 cells (IC50: 6 μM) and inducing apoptosis, sparing normal cells.</p>

<p>FLT3-ITD-IN-3 (13v) is an orally active inhibitor of FLT3-ITD (internal tandem duplication of FLT3), which works by blocking FLT3 signaling. This inhibition leads to cell cycle arrest in the G0/G1 phase and induces apoptosis. The compound is currently employed in studies related to acute myeloid leukemia (AML).</p>

<p>Tubulin polymerization-IN-68 (compound 32) serves as a tubulin inhibitor, disrupting cellular microtubule networks by hindering tubulin polymerization. It also upregulates PARP-1 and caspase-3 expression, thereby inducing apoptosis and exhibiting anticancer properties. Notably, Tubulin polymerization-IN-68 effectively suppresses HepG2 cells with an IC50 of 93 nM and markedly reduces the growth of HepG2 xenograft tumors in nude mice through oral administration.</p>

<p>DWP-05195 is a TRPV1 antagonist capable of inhibiting pain signal transduction. Additionally, it induces ER stress-dependent apoptosis in human ovarian cancer cells via the ROS-p38-CHOP pathway.</p>

<p>RIP3 Activator 1 (compound C8) is an effective RIP3 activator that inhibits cell growth and induces necroptotic cell death (necroptosis) and autophagy through the RIP3/p62/Keap1 signaling pathway. Additionally, this compound enhances the expression of p-MLKL and promotes the accumulation of LC3-II and p62 proteins.</p>

<p>VEGFR-2-IN-14 (Compound 5) is a potent inhibitor of VEGFR-2, which inhibits the growth of HepG2 cells in the Pre-G1 phase and induces apoptosis.</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>Tubulin inhibitor 13 (E27), IC50 16.1 μM, blocks tubulin polymerization, cancer cell migration, and invasion, induces apoptosis.</p>

<p>BMS 310705, an Epothilone B analog, targets ovarian/renal/bladder/lung cancer, inducing apoptosis via mitochondria.</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>JAK-2-/3-IN-3 (ST4j) is a potent JAK2/3 inhibitor for leukemia research, with IC50s: JAK2, 13 nM; JAK3, 14.86 nM; induces apoptosis.</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>3-AP-Me is the dimethyl derivative of the ribonucleotide reductase inhibitor 3-AP (SML0568). It activates the endoplasmic reticulum (ER) stress pathway by promoting eIF2α phosphorylation and upregulating gene expression of transcription factors ATF4 and ATF6, thereby inducing apoptosis. Additionally, 3-AP-Me activates cellular stress kinases c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase, leading to the upregulation of spliced mRNA variant XBP1. It is applicable in cancer research.</p>

<p>Compound 12, an anticancer agent, halts G2/M phase, triggers cell death, and activates p53 &amp; PTEN for tumor suppression.</p>

<p>RMS5: hambanine analogue, inhibits P-gp, anti-cancer with cytotoxic, anti-proliferative effects, reduces Bcl-2 proteins, cleaves PARP.</p>

<p>NLRP3-IN-78 (compound 21) is an NLRP3 inhibitor with a 46.72% inhibition rate of GSDMD-induced pyroptosis at 5 μM. It binds to the NLRP3 protein and prevents GSDMD-NT oligomerization. Additionally, NLRP3-IN-78 inhibits GSDMD cleavage and upstream NF-κB signaling, demonstrating anti-inflammatory activity.</p>

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

<p>VEGFR-2-IN-18 is a potent VEGFR-2 inhibitor with a 60 nM IC50, promoting cell apoptosis and anticancer effects.</p>

<p>Microtubulin-IN-1 (Compound 8g) is an inhibitor of microtubulin, targeting the colchicine-binding site to disrupt tubulin integrity and induce upregulation of p53 protein expression. It exhibits antiproliferative activity across various cancer cell lines, including NCI-H460, BxPC-3, and HT-29, with IC50 values of 2.4, 1.6, and 2.07 nM, respectively. Additionally, Microtubulin-IN-1 induces cell cycle arrest at the G2/M phase and apoptosis in NCI-H460 cells.</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>Antitumor agent-78 blocks GPx-4, raises COX2, triggers apoptosis, halts EMT, and stifles cancer cell growth and migration.</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>ASK1-IN-8 (Compound 35) is an orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 value of 1.8 nM. In a mouse liver injury model induced by Acetaminophen, ASK1-IN-8 significantly reduces plasma alanine aminotransferase (ALT) levels, offering liver protection. This compound is useful for research in liver disease-related fields.</p>

<p>STAT3-IN-12,STAT3 signaling inhibitor. Blocks IL-6-induced JAK/STAT3 activation. Induces apoptosis. Used in HCC and esophageal cancer research.</p>

<p>ADH-6, a tripyridylamide, disrupts mutant p53 aggregates in cancer cells, reviving its function and inducing apoptosis.</p>

<p>RET-IN-10: Potent RET inhibitor, may treat congenital megacolon and tumors (Patent WO2021135938A1, compound 18).</p>

<p>Aeroplysinin I is an antibacterial compound from the sponge. It has cytotoxic activity against colon cancer cells by promoting β-catenin degradation.</p>

<p>SM-433 hydrochloride, a Smac mimetic &amp; IAP inhibitor, binds XIAP BIR3; potent IC50 &lt;1 μM. (Patent WO2008128171A2)</p>

<p>YK5 is an allosteric inhibitor pocket of Hsp70 and represents a previously unknown chemical tool to investigate cellular mechanisms associated with Hsp70.</p>

<p>TP-030-2 is a RIPK1 inhibitor (human K i =0.43 nM ; mouse IC 50 =100 nM) .</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>Potent dual c-Met/HDAC inhibitor, IC50: HDAC1 5.4 nM, c-Met 18.49 nM; anti-cancer, induces apoptosis, G2/M arrest in HCT-116.</p>

<p>Tubulin inhibitor 41 (Compd D19) is a promising lead compound for glioblastoma treatment, known for its ability to penetrate the blood-brain barrier (BBB). It functions as a tubulin inhibitor, inducing G2/M phase arrest, leading to cell apoptosis, and inhibiting the migration of U87 cells [1].</p>

<p>Compound Z15 (ZNU-IMB-Z15) acts as an antagonist and degrader of the androgen receptor (AR). It inhibits the proliferation of castration-resistant prostate cancer (CRPC) cell lines that are AR-positive and induces apoptosis. Compound Z15 exhibits anticancer activity both in vivo and in vitro.</p>

<p>Lometrexol hydrate, an antipurine antifolate, inhibits GARFT and purine synthesis, leading to cancer cell apoptosis without causing DNA breaks.</p>

<p>GGTI-2154 hydrochloride: selective GGTase I inhibitor, IC50 21 nM, used in cancer research.</p>

<p>NTU281 inhibits transglutaminase-2, lowers creatinine in diabetic rats, reduces proteinuria, and fights glomerulosclerosis.</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>4-Bromo A23187 is a halogenated analog of the calcium ionophore A-23187. 4-Bromo A23187 is a calcium modulator and induces apoptosis in different cells.</p>

<p>eIF4A3-IN-6 is a potent eIF4A inhibitor, potentially used for treating eIF4A-related diseases like cancer. (US20170145026A1)</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>ZLMT-12: tacrine derivative, inhibits CDK2/CDK9, weak on AChE/BuChE, anti-proliferative, low toxicity, blocks S/G2/M phase, induces apoptosis.</p>

<p>Compound W10 is a dual inhibitor of Topo I (IC50: 0.90μM) and COX-2 (IC50: 2.31μM), inducing cancer cell apoptosis via mitochondria.</p>

<p>Kahweol Acetate, a semi-synthetic coffee bean derivative, inhibits osteoclasts, cancer cells, DNA damage, and oxidative stress.</p>

<p>Mcl-1 inhibitor22 (Example 36) is an MCL-1 inhibitor that suppresses its anti-apoptotic function by blocking the interaction between MCL-1 and pro-apoptotic proteins. It exhibits antiproliferative activity against various cancer cell lines and can be utilized for cancer research.</p>

<p>Tubulin polymerization-IN-61 (Compound 9a), a tubulin polymerization inhibitor, disrupts the microtubule skeleton, arrests the cell cycle at the G2/M phase, induces Apoptosis, and impedes cancer cell migration and colony formation. This compound demonstrates antitumor efficacy in vivo within the 4T1 xenograft model [1].</p>

NDs-IN-1 (Compound 3g) is a novel non-covalent multi-target inhibitor that inhibits the activities of key enzymes such as hBACE-1, hAChE, and hMAO-B, and is primarily used in the study of neurodegenerative diseases [1].

<p>TAS-117 HCl: potent oral Akt inhibitor (Akt1 IC50: 4.8nM, Akt2: 1.6nM, Akt3: 44nM), boosts anti-myeloma effects, induces cell death.</p>

<p>ZB-R-55 is an oral and highly potent bimodal RIPK1 inhibitor with excellent kinase selectivity in lps-induced sepsis models for the study of SIRS and sepsis.</p>

<p>Caspase-3 Activator 4 (compound 4o) is an effective caspase-3 activator that can cross the blood-brain barrier. This compound exhibits antiproliferative activity and can induce cell apoptosis (apoptosis). Additionally, Caspase-3 Activator 4 enhances the gene expression of TNF-α and reduces the expression of cleaved caspase-3/caspases 3.</p>

<p>HDAC-IN-37 inhibits HDACs 1, 3, 8, &amp; 6, induces histone acetylation, halts G1 to S phase, and triggers early apoptosis.</p>

<p>Ac-DMLD-CMK is a peptide designed to target the caspase3-Gsdme signaling pathway in mice. It specifically inhibits the activation of caspase 3 and Gsdme, preventing the cleavage of Gsdme by caspase 3, which reduces pyroptosis. This process helps alleviate damage to renal tubular epithelial cells and decrease the secretion of inflammatory cytokines. Ac-DMLD-CMK can lower serum creatinine and blood urea nitrogen levels in mice induced by Cisplatin, thereby mitigating the progression of renal dysfunction. It holds potential for research into chemotherapy-induced nephrotoxicity.</p>

<p>Tofacitinib Prodrug-1: an oral prodrug reducing Tofacitinib's side effects, treats ulcerative colitis in mice effectively with low toxicity.</p>

<p>HDAC-IN-34 inhibits HDAC1 (IC50: 0.022 μM) &amp; HDAC6 (IC50: 0.45 μM), binds DNA causing damage, and halts HCT-116 cell growth (IC50: 1.41 μM).</p>

<p>Antitumor agent-37: strong anti-growth, anti-spread, induces DNA damage, apoptosis via Bcl-2/Bax/caspase3, boosts immune response.</p>

<p>D18: Dual agonist for TLR7/8, boosts PD-L1, aids tumor sensitivity to PD-1/PD-L1 inhibitors, and is a cytotoxin for ADC HE-S2.</p>

<p>PARP1-IN-12: potent PARP1 inhibitor, IC50 2.99 nM, triggers cell apoptosis, G2/M arrest, induces DSBs in BRCA-deficient cells.</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>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>Siphonaxanthin is a carotenoid found in green algae, known for targeting the death receptor 5 (DR5) on cancer cells to induce apoptosis. In human leukemia HL-60 cells, it increases DR5 expression, reduces Bcl-2 levels, and activates caspase-3. It also inhibits fibroblast growth factor receptor-1 (FGFR-1) signaling in endothelial cells. Siphonaxanthin suppresses the proliferation, migration, and tubular formation of human umbilical vein endothelial cells (HUVECs), as well as the growth of microvessels in rat aorta rings. Additionally, it has anti-inflammatory properties by blocking the translocation of high-affinity IgE receptors (FcεRI) to lipid rafts in mast cells. Siphonaxanthin shows potential for research into diseases such as cancer, diabetic retinopathy, and rheumatoid arthritis.</p>

<p>HR-19011 (Compound 40) is an inducer of eIF2α phosphorylation that increases expression levels of downstream proteins ATF and CHOP,antiproliferative.</p>

<p>RIP1 kinase inhibitor 1 is an orally available and brain-penetrating inhibitor of RIP1 kinase with pKi of 9.04.</p>

<p>vacuolar H+-ATPases (V-ATPases) inhibitor</p>

<p>FAK-IN-2: potent oral FAK inhibitor, IC50 35 nM, reduces tumor growth, migration, and induces cell death.</p>

<p>Compound 14 is a peptidomimetic that significantly lowers TNFα, NO, CD40, and CD86, showcasing strong anti-inflammatory effects.</p>

<p>Antitumor agent-202 is a stabilizer of the p53Y220C mutant, selectively inhibiting the proliferation of tumor cells carrying the p53Y220C mutation. It is applicable for research focused on cancers associated with the p53 Y220C mutation.</p>

<p>AKT-IN-3: potent oral Akt inhibitor with low hERG blockage. IC50: 1.4-1.7 nM for Akt1-3. Inhibits AGC kinases like PKA, PKC.</p>

<p>CHI-KAT8i5 is a selective inhibitor of KAT8 with a KD of 19.72 μM. It induces apoptosis (Apoptosis) in a dose-dependent manner. CHI-KAT8i5 can inhibit tumor growth in esophageal squamous cell carcinoma, colon cancer, melanoma, gastric cancer, non-small cell adenocarcinoma, and liver cancer.</p>

<p>PF-3837 is an inhibitor of the Mps1 kinase, with a Ki value of 0.33 nM and an IC50 value of 5.5 nM. It disrupts cell cycle checkpoints by inhibiting the catalytic activity of Mps1, thereby reducing genomic stability and leading to cancer cell apoptosis (Apoptosis). PF-3837 is utilized in the study of breast cancer.</p>

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

<p>NF-κB-IN-4 (compound 17) is a potent inhibitor of NF-κB pathway which can cross blood brain barrier (BBB).</p>

<p>OICR12694 (JNJ-65234637) is an orally active inhibitor of B cell lymphoma 6 (BCL6) .</p>

<p>Urease-IN-20 (compound XBP2) is an inhibitor of Helicobacter pylori (H. pylori), with an IC50 of 0.14 μM for H. pylori inhibition. It effectively decreases apoptosis in GES-1 cells infected with H. pylori and reduces levels of ROS and γH2AX. Urease-IN-20 also demonstrates significant gastric mucosal protective effects, making it suitable for H. pylori research.</p>

<p>CDK-IN-9: A potent CDK inhibitor, gels to enhance CDK12/DDB1 binding, targets CDK2/E (IC50: 4 nM), induces apoptosis via dephosphorylation.</p>

<p>p53 Activator 14 (Compound 7A) is a derivative of Neratinib that can induce DNA damage and activate p53, thereby inhibiting the proliferation of various cancer cells, with an IC50 of 7.21 μM for HCT116 cells. This compound hinders adhesion, migration, and invasion of HCT116 cells, disrupts the cell cycle, and triggers apoptosis. In addition, p53 Activator 14 exhibits anti-tumor properties and inhibits angiogenesis in the chick embryo chorioallantoic membrane (CAM) model.</p>

<p>HL001 is an orally active small molecule inhibitor of cyclophilin A (CypA) and a receptor antagonist of lysophosphatidic acid 1 (LPA1). It induces cell cycle arrest and apoptosis in tumor cells via p53. By downregulating G3BP1, HL001 promotes reactive oxygen species production and DNA damage to stabilize p53. It disrupts the interaction between MDM2 and p53-72R in a CypA-dependent manner. HL001 exhibits antitumor activity and can also be used in research on pulmonary fibrosis.</p>

<p>TBC-1 is a chlorophyll-a derivative that acts as a photosensitizer for photodynamic therapy (PDT). It efficiently generates type I ROS and targets the endoplasmic reticulum. TBC-1 demonstrates in vitro biocompatibility and PDT effectiveness under both normoxic and hypoxic conditions.</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>NLRP3-IN-72 (Compound 2) is a benzimidazole derivative. It exhibits anti-inflammatory and antioxidant properties, with an IC50 of 0.3 μM for NLRP3 IL-1β, a PD50 of 0.4 μM for protection against cell pyroptosis, and an EC50 of 0.6 μM for inducing HO-1.</p>

<p>PD-L1-IN-1, potent PD-L1 inhibitor with 115 nM IC50, suppresses tumors, boosts immune response, and spares healthy cells.</p>

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

<p>Belotecan (CKD-602) inhibits DNA topoisomerase I, blocks cell cycle, induces apoptosis, and is a camptothecin-derived anticancer agent.</p>

<p>Cernuumolide J (TMJ-105) functions as a JAK2/STAT3 inhibitor and exhibits potent activity against HEL leukemia cells by inhibiting their growth in both time-dependent and concentration-dependent manners, with an IC 50 value of 1.79 μM. This compound effectively induces G2/M phase arrest and apoptosis by downregulating the phosphorylation of JAK2, STAT3, and Erk, while simultaneously upregulating the phosphorylation of JNK and p38 MAPK. Cernuumolide J holds potential for research applications in anti-cancer therapy.</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>DX3-234 is a OXPHOS inhibitor that acts by inhibiting complex I in the mitochondrial ETC,for cancers dependent on aerobic metabolism, such as pancreatic cancer.</p>

<p>Tubulin-IN-9 inhibits tubulin (IC50: 1.82 μM), halts K562 cells in G2/M, induces apoptosis, and has anti-cancer effects.</p>

<p>Compound C11 inhibits 14-3-3η protein (KD: 35 μM), targets liver cancer cells, blocks G1-S phase, and induces apoptosis.</p>

<p>RIPK1-IN-28 (compound 13) is an orally active inhibitor of RIPK1. It exhibits inhibitory effects on human I2.1 and Hepa1-6 cells, with IC50 values of 0.4 and 1.2 nM, respectively.</p>

<p>(S)-JDQ-443, an isomer of JDQ-443, is a selective, potent oral KRAS G12C inhibitor with antitumor properties.</p>

<p>WK88-1, an inhibitor of Hsp90, effectively induces the degradation of various oncogenic signaling molecules, including EGFR, ErbB2, and ErbB3, in the gefitinib-resistant H1975 cell line. This leads to subsequent growth arrest and apoptosis.</p>

<p>GNE684 inhibits RIP1; Ki app: 21 nM (human), 189 nM (mouse), 691 nM (rat).</p>

<p>(S)-Purvalanol B is the S enantiomer of Purvalanol B. Purvalanol B is an inhibitor of cyclin-dependent kinase(CDK) .</p>

<p>Samuraciclib (CT7001) is an oral CDK7 inhibitor with 41 nM IC50, notable for its high selectivity and potency against breast cancer cells.</p>

<p>FLT3/TrKA-IN-1: Potent dual kinase inhibitor for FLT3 &amp; TrKA, promising for AML research.</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>