Apoptosis

<p>Borrelidin (Treponemycin) is an inhibitor of trehalose-6-phosphate synthase, a nitrogen-containing macrolide antibiotic isolated from Streptomyces rochei.</p>

<p>CRM1-IN-2 (Compound KL2) is a noncovalent inhibitor that targets CRM1, localizing it to the nuclear periphery, depleting its nuclear presence, and inhibiting</p>

<p>Oxythiamine (Hydroxythiamin) is a TK inhibitor that inhibits cancer cell proliferation, induces cell cycle arrest, and induces apoptosis.</p>

<p>CSF1R-IN-26 (Compound III-1) is an inhibitor of CSF-1R with an IC50 of 20.07 nM. It promotes the polarization of M2 macrophages to M1 macrophages, inducing apoptosis in MC-38 cancer cells. CSF1R-IN-26 inhibits the activation of the AKT/ERK/STAT3 signaling pathways, remodels the tumor immune microenvironment, and exhibits antitumor activity in mouse models. In SD rats, CSF1R-IN-26 demonstrates favorable pharmacokinetic properties, with a half-life of 1.86 hours and an oral bioavailability of 79.22%.</p>

<p>FG-3019 (Pamrevlumab), a human antibody, targets CTGF, potentially treating idiopathic pulmonary fibrosis.</p>

<p>Thalidomide-O-amido-C8-NH2 is a thalidomide-based ligand-linker for PROTAC synthesis.</p>

<p>RWJ-56110 dihydrochloride is a potent PAR-1 inhibitor (IC50=0.44μM), blocking platelet aggregation, angiogenesis, and induces apoptosis. No PAR-2/3/4 effect.</p>

<p>Aspidin BB, a phloroglucinol from Dryopteris, inhibits cancer by causing cell cycle arrest and apoptosis in HO-8910 cells.</p>

<p>DL-Sulforaphane N-acetyl-L-cysteine (SFN-NAC), induces apoptosis through α-microtubulin and phosphorylation of ERK1/2-mediated Stathmin-1, and Hsp70 (NSCLC).</p>

<p>Conglobatin is a natural product for research related to life sciences. The catalog number is T36494 and the CAS number is 72263-05-9.</p>

<p>Thalidomide-5-PEG2-Cl is a cereblon ligand that recruits CRBN protein and forms PROTACs through linker conjugation.</p>

<p>PD-L1/LpxC-IN-1 (Compound 12b) is an inhibitor of PD-L1 and LpxC, with IC50 values of 5.2 μM and 0.081 μM, respectively. This compound disrupts bacterial lipopolysaccharide biosynthesis, leading to bacterial cell lysis and death. It effectively inhibits Gram-negative bacteria, exhibiting a minimum inhibitory concentration (MIC) of 0.25-0.5 μg/mL against K. pneumoniae ATCC 13883, E. coli ATCC 8739, S. typhimurium ATCC 14028, and P. aeruginosa ATCC 9027. Additionally, PD-L1/LpxC-IN-1 modulates the immune response by downregulating the expression of inflammatory cytokines IL-2 and IFN-γ, and upregulating CD4+ and CD8+ cells, thus activating the immune system and mitigating excessive inflammatory responses. In a mouse model of K. pneumoniae ATCC 13883 infection, PD-L1/LpxC-IN-1 demonstrated antibacterial activity.</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>Eciskafusp alfa, a cis-targeted IL2v immunocytokine, acts on programmed cell death 1 (PDCD1, commonly known as PD-1), preferentially targeting antigen-specific</p>

<p>IRAK4-IN-27 (Compound 22) is a potent and selective IRAK4 inhibitor, demonstrating an IC50 of 8.7 nM.</p>

<p>Emavusertib (CA-4948) hydrochloride, a selective and potent IRAK4/FLT3 inhibitor, is designed for oral administration. It achieves an IC 50 of 57 nM against IRAK4 in a FRET kinase assay and demonstrates anti-tumor activity [1] [2] [3].</p>

<p>Leucettamol A, from Leucetta microraphis, blocks LTB4 receptor and prevents Ubc13-Uev1A complex formation.</p>

<p>Ac-IEPD-AFC (IEPD) is a fluorescent substrate for granzyme B and can be used to measure granzyme B activity.</p>

<p>NCT-58 is a potent HSP90 inhibitor that blocks Akt, downregulates HER family, and induces apoptosis in HER2+ breast cancer without triggering HSR.</p>

<p>Taccalonolide E is a microtubule stabilizer and induces cancer cell apoptosis .</p>

<p>Vonlerolizumab (MOXR 0916) is a humanized IgG OX40 agonist monoclonal antibody with potential in cancer and immune disease research.</p>

<p>TopoisomeraseI/II inhibitor 6 (compound 3i) acts as an effective inhibitor of topoisomerase I and II, with IC50 values of 4.77 µM and 15 µM, respectively. Additionally, it exhibits antiproliferative activity against the human melanoma cell line LOX IMVI, demonstrating IC50 values of 26.7 µM and 25.4 µM.</p>

RET-IN-28 (Compound 16) is an inhibitor of RET (a transmembrane receptor tyrosine kinase). It specifically inhibits the activity of a mutant RET enzyme (RET-V804M) and is utilized in cancer research.

<p>Isorhamnetin 3-glucuronide is a useful organic compound for research related to life sciences and the catalog number is T124938.</p>

<p>SIN-1 chloride is a moxidomine metabolite with vasodilatory, anti-platelet, and antianginal effects, reducing myocardial ischemia-related damage.</p>

<p>Antiproliferative agent-23: destabilizes microtubules, induces apoptosis in cancer cells via mitochondrial path, and triggers ER stress.</p>

<p>Antitumor photosensitizer-7 (compound 15), a photosensitizer possessing anti-cancer properties, demonstrates substantial cytotoxic effects on the G361 melanoma cell line when exposed to 414 nm blue light irradiation.</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.

Anti-Mouse PD-1 Antibody (RMP1-14) is an IgG2a antibody inhibitor against mouse PD-1 and can block PD-1/PD-L1 signaling. High-Quality, Low-Cost!

<p>MBC-11 trisodium, a bisphosphonate-Ara-C conjugate, may treat TIBD.</p>

<p>Lipustobart is an IgG4-kappa humanized monoclonal antibody targeting PDCD1 (programmed cell death 1, PD1, PD-1, CD279), with immunostimulant and antineoplastic</p>

<p>ASR-488, an activator of the mRNA-binding protein CPEB1, promotes apoptosis and suppresses the growth of bladder cancer [1].</p>

<p>Zeluvalimab (AMG-404) is a monoclonal antibody designed to target the PD-1 receptor, and is utilized in cancer research [1].</p>

<p>Dehydrobruceine B, from Brucea javanica, enhances Cisplatin-induced apoptosis by affecting AIF, Bax, and Keap1-Nrf2.</p>

<p>WF 10129 is a new angiotensin converting enzyme inhibitor generated by a fungus, Doratomyces putredinis.</p>

<p>Betifisolimab (MSB-2311) is a humanized antibody targeting PD-L1 for solid tumors and blood cancer research.</p>

<p>Danburstotug (IMC-001), an immunostimulant and antineoplastic [1], is a humanized IgG1-lambda monoclonal antibody targeting CD274 (PDL1, B7 homologue 1, B7H1).</p>

<p>Milademetan tosylate hydrate, an oral MDM2 inhibitor targeting AML and solid tumors, induces G1 arrest and apoptosis.</p>

<p>Chloranthalactone B, a sesquiterpenoid from Sarcandra glabra, inhibits inflammation via AP-1 &amp; p38 MAPK.</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>Camrelizumab (SHR-1210) is a human IgG4-κ monoclonal antibody with high affinity and directed against PD-1.Camrelizumab binds PD-1 with a binding affinity of up</p>

<p>Anagrelide HCl monohydrate is a platelet-reducing imidazoquinazoline for ET and PV research.</p>

<p>Ganglioside GD3 disodium salt is a melanoma-associated antigen often targeted in immune therapy for melanomas.</p>

<p>R1-ICR-5 is a selective PROTAC degrader targeting serine/threonine-protein kinase 1 (RIPK1). Mediated by VHL, R1-ICR-5 promotes the degradation of RIPK1, disrupting the TNFR1 and TLR3/4 signaling hubs, enhancing NF-κB, MAPK, and IFN signal output, and facilitating RIPK3 activation and necroptosis induction. R1-ICR-5 holds potential for research in cancer and inflammatory diseases.</p>

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

<p>PRDX1-IN-2 (compound 15) is a selective inhibitor of the antioxidant enzyme Peroxiredoxin 1 (PRDX1) with an IC50 of 0.35 μM. It reduces mitochondrial membrane potential in SW620 cells, potentially due to increased ROS resulting from PRDX1 inhibition, leading to apoptosis. PRDX1-IN-2 is applicable in colorectal cancer research.</p>

<p>DA5-HTL is a compound that combines dasatinib with the HaloTag system, effectively inhibiting the growth of tumor cells, with a GI50 of 1.923 nM.</p>

<p>Thalidomide derivative for CRBN protein recruitment, used in PROTACs production for protein degradation.</p>

WD6305 is an effective and selective METTL3-METTL14 PROTAC degrader, with DC50 values of 140 nM and 194 nM for METTL3 and METTL14, respectively. It inhibits m6A modification and the proliferation of acute myeloid leukemia cells while inducing apoptosis. WD6305 also exhibits antitumor activity.

<p>PROTACGPX4 degrader-2 (compound 18a) is a proteolysis-targeting chimera (PROTAC) that targets the degradation of glutathione peroxidase 4 (GPX4), with a DC50, 48h value of 1.68 μM. It induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. Additionally, PROTACGPX4 degrader-2 exhibits antiproliferative activity.</p>