Apoptosi

eIF4E-IN-1 inhibits eIF4E and boosts immunity by targeting PD-1, PD-L1, LAG3, TIM3, IDO, aiding cancer and infection treatment.

WEE1-IN-7 (compound 12h) is a potent, orally active WEE1 inhibitor with an IC50 value of 2.1 nM. This compound induces apoptosis and causes cell cycle arrest in the S phase, demonstrating antitumor activity.

OPBP-1 is a D-peptide developed through phage display screening, molecular docking, and molecular dynamics simulations. It exhibits high stability, strong antitumor activity, and oral bioavailability. OPBP-1 selectively binds to the PD-L1 protein, significantly blocking the interaction between PD-1 and PD-L1, which helps restore and enhance T lymphocyte function while reducing the proportion of myeloid-derived suppressor cells (MDSCs), counteracting tumor-induced immune evasion. OPBP-1 is applicable for research in cancer immunotherapy.

TopoisomeraseII inhibitor 17 (compound 4c) is a thiazolopyrimidine-based inhibitor of Topoisomerase II with an IC50 of 0.23 μM. This compound significantly disrupts the cell cycle and induces apoptosis.

S2/IAPinh is a conjugate composed of an inhibitor of apoptosis proteins inhibitor (IAPinh) and a ligand of sigma 2 SW43. It demonstrates anti-proliferative and apoptosis-inducing activity by degrading inhibitor of apoptosis proteins (clAP-1).

Ru-Poma is an Ru(II)-based photosensitizer designed to enhance the efficacy of photodynamic therapy (PDT) against tumors resistant to Cisplatin. It targets Pomalidomide to partially degrade CRBN, inducing ferroptosis by increasing lipid peroxides and downregulating GPX4 and GAPDH expression. In A549 cells, Ru-Poma exhibits cytotoxicity with IC50 values of 18.46 μM in the dark and 0.37 μM under illumination.

RIPK1-IN-13 (compound 28) is a selective inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK1), showing a pKi of 7.66 as measured by the ADP-Glo kinase assay. It exhibits inhibitory effects in human leukemia U937 cells with a pIC50 of 7.2.

Fascaplysin inhibits CDK4/D1 (IC50=0.35μM), triggers caspase-activated autophagy-apoptosis crosstalk, and blocks PI3K/AKT/mTOR in HL-60 cells.

Antimycobacterial agent-5 (compound 27) is an imidazopyridine amide compound that targets the Mycobacterium electron transport chain (ETC) respiratory CIII2CIV2 supercomplex. It acts on Mycobacterium smegmatis CIII2CIV2 with an IC50 of 441 nM.

CBI1 is a covalent BAX inhibitor. It selectively derivatizes BAX at C126 and inhibits BAX activation by triggering a ligand or through point mutations. CBI1 prevents the lipidation and oligomerization of BAX by t-2-hex. It also inhibits BAX activation induced by BH3 ligands, F116A mutation, or t-2-hex.

PD-1/PD-L1-IN-39 (X 14) is an orally active PD-1/PD-L1 inhibitor with an IC50 value of 15.73 nM. It exhibits strong binding affinity to human and mouse PD-L1, with KD values of 14.62 and 392 nM, respectively. PD-1/PD-L1-IN-39 also demonstrates antitumor activity.

C-Peptide 1 (rat) is a polypeptide isolated from proinsulin. C-Peptide acts as a β-catenin/GSK-3β activator, influences Na/K-ATPase, regulates apoptosis.

Antitumor agent-36: potent anti-cancer; causes DNA damage, triggers apoptosis, enhances immune response by upregulating T cells.

MS105 is an orally active, selective protein tyrosine kinase 6 (PTK6) PROTAC degrader. It recruits the VHL E3 ligase through a VHL ligand fragment, facilitating ubiquitination and proteasomal degradation of PTK6, thereby inhibiting the proliferation and migration of breast cancer cells and inducing apoptosis (apoptosis). MS105 is a promising compound for breast cancer research.

MKC-1 (Ro-31-7453) is an oral bisindolylmaleimide inhibitor that disrupts tubulin polymerization, potentially halting cancer cell division.

PD-L1 inhibitor IV, a polypeptide, competitively blocks hPD-1 with a Kd of 1.38 μM, preventing hPD-1/hPD-L1 interaction.

d-(KLAKLAK)2 is an antimicrobial and antitumor peptide, notable within the group of antimicrobial peptides, and exhibits strong anticancer properties. It kills bacteria by disrupting their cell membranes, causing leakage of cell contents. Additionally, d-(KLAKLAK)2 inhibits tumor cell proliferation by inducing apoptosis through mitochondrial swelling and membrane damage.

IDH1/2-IN-1 (Compound 6b) is a dual inhibitor of IDH1(R132H)/IDH2(R140Q) with IC50 values of 0.22 μM and 1.6 μM, respectively. This compound effectively inhibits tumor growth by suppressing tumor cell proliferation and activating antioxidative enzymes to enhance host defense. Additionally, IDH1/2-IN-1 reduces inflammation and promotes apoptosis, demonstrating significant anti-tumor activity. It is also utilized in leukemia research.

Tubulin polymerization-IN-67 (Compound 5h) serves as an inhibitor of microtubule protein polymerization at the colchicine binding site, exhibiting an IC50 value of 2.92 μM. It effectively inhibits the proliferation of various cancer cell lines including HT29, A549, U2OS, MG-63, and HeLa, with IC50 values ranging from 0.12 to 4.13 μM. Additionally, Tubulin polymerization-IN-67 induces cell cycle arrest at the G2/M phase and triggers apoptosis in U2OS cells. It also inhibits cell migration in A549 and reduces mitochondrial membrane potential (MMP) while increasing intracellular ROS levels, thereby suppressing angiogenesis in HUVEC cells. Furthermore, this compound demonstrates antitumor activity in mice.

Ac-FEID-CMK: Potent inhibitor for zebrafish GSDMEb, reduces pyroptosis, and lessens septic AKI.

Azalamellarin N is a pyroptosis inhibitor that exhibits varying inhibitory effects on different pyroptosis inducers. It functions by targeting molecules upstream of NLRP3 inflammasome activation, instead of directly affecting the components of the NLRP3 inflammasome. Its inhibitory potency against various inducers is ranked as follows: Nigericin > R837 [1].

Trilexium (TRX-E-009-1), a third-generation benzopyran structurally related to TRX-E-002-1, increases p21 protein expression, induces apoptosis, depolymerizes microtubules, and demonstrates broad anti-cancer activity [1] [2].

PBE-AMF is a prodrug that activates H2O2 and exhibits anticancer activity. It impedes tumor proliferation by inhibiting DNA synthesis, reducing ATP levels, inducing cell death (apoptosis), and blocking the cell cycle. PBE-AMF effectively and selectively inhibits the proliferation of MDA-MB-231 cells (IC50=6.4 μM) while sparing non-cancerous MCF-10A cells.

Pep19-2.5: Synthetic antitoxin peptide inhibits LP/LPS signals via PRRs, preventing inflammation and pyroptosis.

Cot inhibitor-1 hydrochloride blocks TPL-2 kinase (IC50=28nM) and TNF-α synthesis (IC50=5.7nM) in human blood.

Compound T2S0062 is a natural product for research related to life sciences. The catalog number is T2S0062 and the CAS number is 135247-95-9.

Thalidomide-PEG conjugate for E3 ligase in PROTACs; has cereblon ligand and 3-unit PEG linker.

PROTAC FGFR2 degrader 1 (compound N5) is a potent PROTAC that efficiently targets FGFR2, boasting a DC 50 value of 6.46 nM and an FGFR2 IC 50 of 0.08 nM. This compound exhibits significant anti-proliferative effects and high selectivity. It induces G0/G1 arrest in the cell cycles of KATOIII and SNU16 and inhibits apoptosis by diminishing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. Additionally, PROTAC FGFR2 degrader 1 maintains over 50% inhibition of gastric cancer cells at a concentration of 0.17 nM and effectively suppresses the growth of SNU16 xenograft tumors in a mouse model.

Ilicicolin A is a useful organic compound for research related to life sciences. The catalog number is T125289 and the CAS number is 22581-06-2.

YX0798 is a selective, orally active CDK9 inhibitor (Kd: 0.28 nM). It downregulates the oncogenic protein c-MYC and the pro-survival protein MCL-1. YX0798 disrupts the cell cycle and causes transcriptome reprogramming, ultimately leading to apoptosis. The compound exhibits antitumor activity.

CDK2-IN-45 is a CDK2 inhibitor with an IC50 value of 0.64 μM. It effectively inhibits the proliferation of DU-145 and PC-3 cell lines, with IC50 values of 2.20 μM and 4.17 μM, respectively. Additionally, CDK2-IN-45 induces G0/G1 phase cell cycle arrest and apoptosis. It is utilized in prostate cancer research.

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

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

FL118 is a novel survivin inhibitor that inhibits cancer stem cell-like properties.FL118 is a novel camptothecin analog with anticancer activity that inhibits

Potent PROTAC degrader for FLT3/CDK9, induces apoptosis, and shows promise for FLT3-ITD mutated AML research.

Canfosfamide, a prodrug activated by GSTP1-1, induces apoptosis and inhibits DNA-PK, producing an alkylating agent for cancer research.

Ac-Trp-Glu-His-Asp-Aldehyde is a powerful and selective inhibitor of caspase-1, demonstrating a K_i value of 56 pM [1] [2].

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.

MMRi62, a MDM2-MDM4 inhibitor, induces ferroptosis and autophagy in PDAC, degrades FTH1 and mutant p53, and inhibits KRAS/TP53 mutant PDAC in mice.

NSC90616 is a mutant p53 rescue compound [1] .

sEH inhibitor-19 (Compound (R)-14i) is an orally active soluble epoxide hydrolase (sEH) inhibitor with an IC50 of 1.2 nM. This compound suppresses the expression of TNF-α and IL-6 and exhibits anti-inflammatory effects in mouse models of acute pancreatitis and Carrageenan-induced edema.

4-Nitrothalidomide is a modified form of thalidomide that inhibits the growth and proliferation of HUVEC cells and is commonly used in the synthesis of pomalidomide, which has anticancer potential.

GSK-1070916 (GSK-1070916A) is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM.

ASK1-IN-4 is an ASK1 inhibitor, IC50 = 0.2 μM.

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

Chloranthalactone B, a sesquiterpenoid from Sarcandra glabra, inhibits inflammation via AP-1 & p38 MAPK.

Solasodine hydrochloride (90 μM; 2 days) treatment induced significant budding in P19 cells. This compound strongly stimulated the expression of various neuronal markers, including βIII-tubulin, synaptophysin, MAP2, ChAT, and the neural progenitor marker doublecortin. Predominantly, Solasodine hydrochloride directed the differentiation of P19 cells towards neuronal pathways.