Apoptose

TNF-α-IN-11 (Compound 10) is a TNF-α inhibitor exhibiting a dissociation constant (K D) of 12.06 μM.

Cytostatin: Natural antitumor, inhibits cell adhesion, blocks B16 melanoma, induces apoptosis, selectively targets PP2A (IC50 = 29 nM).

eIF4E-IN-5 (Compound 6n) is a cell-permeable eIF4E inhibitor that binds to capped mRNA, thereby inhibiting cap-dependent translation [1].

Pipermethystine is a useful organic compound for research related to life sciences and the catalog number is T124340.

Antiproliferative Agent-42 (Compound 7m), a dihydrodipyrrolo compound, exhibits antiproliferative activity against the Panc-1 cell line, with an IC 50 of 12.54

Compound B12, a JOA derivative, collapses MMP to induce apoptosis, inhibits cloning/migration, and has an IC50 of 0.39 μM against HGC-27 cells.

CYP51/PD-L1-IN-3 (compound L21), a quinazoline with antifungal properties, serves as a dual inhibitor targeting CYP51 (IC50: 0.205 μM) and PD-L1 (IC50: 0.039 μM

XM-U-14 is a selective PROTAC USP7 degrader that induces the degradation of USP7 in the RS4;11 cell line with a DC50 of 0.74 nM. This compound elevates the levels of p53 and p21, and significantly inhibits the growth of acute lymphoblastic leukemia (ALL) cells, with IC50 values of 0.5 nM in RS4;11 cells and 8.3 nM in Reh cells. Moreover, XM-U-14 induces apoptosis and cell cycle arrest, and effectively inhibits tumor growth.

HSP70-IN-6 (Compound JL-15) acts as an inhibitor of the Hsp70-Bim protein-protein interactions (PPI) with an IC50 value of 70 nM. It induces apoptosis in chronic myeloid leukemia (CML) cells with EC50 values of 0.43 μM (BV173), 0.88 μM (K562), and 0.19 μM (K562-R3).

BcI-2/BcI-xI ligand 1, functioning as a BcI-2/BcI-xI ligand, is utilized in the synthesis of PROTAC BcI-2/BcI-xI Degrader-1 .

Human PD-L1 inhibitor II is a potent PD-L1 inhibitor with anti-cancer activity.

Human PD-L1 inhibitor I, a peptide, blocks PD-L1/PD-1 interaction with 3.39 μM affinity.

RPS6-IN-1 (Compound 22o) inhibits cell migration and induces apoptosis (increasing the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). It reduces mitochondrial membrane potential and activates autophagy (Autophagy) through the PI3K-Akt-mTOR signaling pathway, damaging mitochondria and lysosomes within the cell and causing endoplasmic reticulum stress. RPS6-IN-1 also inhibits the phosphorylation of RPS6. Notably, RPS6-IN-1 is a low systemic toxicity anticancer agent.

PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader of CDK4 and CDK6, with DC50 values of 10.5 nM and 2.5 nM, respectively. This compound effectively inhibits proliferation in Jurkat cells (IC50 of 0.18 μM), induces cell cycle arrest during the G1 phase, and triggers cell apoptosis (apoptosis).

DAPK Substrate Peptide TFA is a synthetic peptide that serves as a substrate for the enzyme death-associated protein kinase (DAPK), exhibiting a Michaelis

BMH-7 HCl is a p53 activator, showing anti-cancer activity by activating the p53 pathway.

TPP-1 TFA is a high-affinity PD-L1 inhibitor (KD=95nM) that boosts T-cell function to curb tumor growth.

Potent vasopressin blocker, Antagonist G TFA also mildly inhibits GRP & Bradykinin, triggers AP-1, enhances chemo response.

(E/Z)-Eltrombopag 13C4 is a mix of E/Z isotopologues, both 13C-labeled TPO receptor agonists for thrombocytopenia.

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.

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

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.

PD-L1inhibitory peptide is an inhibitor peptide that targets the programmed cell death ligand 1 (PD-L1). By binding to PD-L1, it lifts immune suppression and restores the anti-tumor activity of T cells. PD-L1inhibitory peptide holds promise for use in tumor research.

Carbonic anhydrase inhibitor33 (11D) is a dual inhibitor that targets both CA (carbonic anhydrase) IX/XII and CDK6. It exhibits Ki values of 19.7 nM for hCA IX and 26.1 nM for hCA XII. Additionally, Carbonic anhydrase inhibitor33 (11D) can induce G1 phase cell cycle arrest and apoptosis, making it relevant for research in non-small cell lung cancer (NSCLC).

TRAP1-IN-1 is a selective TRAP1 inhibitor, induces degradation of TRAP1 downstream proteins, inhibits OXPHOS, and disrupts mitochondrial membrane potential.

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.

FAK-IN-25 (4c) is an inhibitor of FAK with an IC50 value of 50.98 nM. It induces apoptosis and causes cell cycle arrest in the G1 phase, making it relevant for cancer research.

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

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

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].

Ac-LEVD-CHO, a caspase-4 inhibitor, is a peptide with the sequence Ac-Leu-Glu-Val-Asp-al [1].

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

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.

Vinepidine (LY-119863) sulfate, a derivative of vincristine, exhibits antitumor activity .

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

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.

FR900359 is a macrocyclic Gq protein inhibitor that inhibits melanoma cell proliferation and can be used to study asthma, inflammation and cancer.

PROTACGPX4 degrader-4 is a GPX4 PROTAC degrader with a DC50 of 5.32 nM. It inhibits the activity of cancer cell lines RT4, T24, and J82 with IC50 values of 0.09, 2.97, and 7.58 μM, respectively. This compound elevates lipid ROS levels and induces ferroptosis in T24 and RT4 cells. In T24 tumor-bearing BALB/c nude mouse models, PROTACGPX4 degrader-4 demonstrates antitumor activity. It is applicable to bladder cancer research.

PRMT5-IN-33 (compound A8) is a selective inhibitor of PRMT5 that competes with SAM, exhibiting an IC50 of 10.9 nM. It induces apoptosis and inhibits the proliferation of Z-138 and MOLM-13 cells, demonstrating antitumor activity.

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.

WK369 is an innovative small molecule inhibitor of BCL6, demonstrating remarkable bioactivity against ovarian cancer by inducing cell cycle arrest and triggering apoptosis. It binds directly to the BCL6-BTB domain, obstructing the interaction between BCL6 and SMRT, which results in the reactivation of p53, ATR, and CDKN1A.

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.

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).

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.

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.

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.

MX106-4C is a survivin inhibitor that selectively targets ABCB1-positive colorectal cancer cells. It can work synergistically with Doxorubicin for enhanced anticancer effects or restore Doxorubicin sensitivity in drug-resistant ABCB1 cells.

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.

Necrosis inhibitor 2 hydrochloride (Compound B19) is an agent that inhibits cellular necrosis. It is useful for researching diseases associated with necrotic pathways, including inflammation, cancer, metabolic disorders, and neurodegenerative diseases.

EGFR-PK/JNK-2-IN-1 (Compound 6c) is a dual inhibitor of EGFR-PK and JNK-2, with IC50 values of 2.7 and 3.0 μM, respectively. It can induce apoptosis and cause cell cycle arrest at various stages. This compound is applicable in cancer research.