Apoptosis

CSRM617 is an inhibitor of the transcription factor ONECUT2 (OC2), thereby suppressing metastasis in mice.

MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53, induces apoptosis, and has anti-tumor activity.

Ac-DEVD-CHO is an aldehyde peptide and a CPP32/Apopain Inhibitor.

BDA-366 selectively inhibits BCL2, converting it to a cell death inducer.

LTX-315 is the oncolytic peptide that kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization.

BH3I-1 is a cell permeable BH3 mimetic that binds to Bcl-xL

Azoramide is a small-molecule modulator of the unfolded protein response with antidiabetic activity.

A-1331852 is a potent and selective BCL-XL inhibitor. BCL-XL is the major antiapoptotic survival protein and may be a novel therapeutic target in CML.

CID5721353 is a B-Cell Lymphoma 6 Inhibitor (BCL6 inhibitor).

GSK583 is a highly potent and selective inhibitor of RIP2 Kinase.

GSK2983559 active metabolite  is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.

RIP2 kinase inhibitor 2 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043437 A1, compound example 9.

Apogossypolone is a nonpeptidic small-molecule inhibitor of Bcl-2 with

(+)-Apogossypol is a potent inhibitor of Bcl-2 family proteins; competing with the BH3 peptide-binding sites on Bcl-2, Bcl-XL, Mcl-1, Bcl-W, and Bcl-B, but not Bfl-1, with IC50s of 0.5 to 2 μM.

CRT-0066101, potent inhibitor of protein kinase D (PKD); inhibits all PKD isoforms (IC50 values are 1, 2 and 2.5 nM for PKD1, PKD3 and PKD2 respectively).

(S)-Gossypol acetic acid is a inhibitor of Bcl-2, potently induce cell death in Jurkat cells overexpressing Bcl-2 (IC50, 18.1μM) or Bcl-xL (IC50, 22.9μM).

NVP-CGM097 is a potent and selective MDM2 inhibitor; an orally bioavailable HDM2 antagonist with potential antineoplastic activity.

Z-VAD(OH)-FMK is an irreversible tripeptide inhibitor of all caspases.

MX-69 is the MDM2/XIAP inhibitor, used for cancer treatment.

CFM 4, CARP-1 mimetic; interferes with CARP-1 binding to APC-2. Enhances CARP-1 expression and induces G2/M cell cycle arrest. Induces apoptosis and suppresses cell growth in cancer cells.

Pyridoclax is a potent Mcl-1 inhibitor with Kd value of 25 nM.

(S,S)-Z-FA-FMK is an irreversible inhibitor of cysteine protease

Cetrimonium bromide is an amine based cationic quaternary surfactant, is one of the components of the topical antiseptic Cetrimide.

Deferiprone is the only orally active iron-chelating drug to be used therapeutically in conditions of transfusional iron overload.

Diatrizoic acid (Diatrizoate) is an iodinated radiocontrast agent and has the potential for radiographic imaging of the airways. Diatrizoic acid induces mitochondrial turnover and oxidative stress, and activating apoptosis by dysregulating calcium.

Fenoprofen Calcium hydrate is a nonsteroidal, anti-inflammatory antiarthritic agent.

GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit Rap1A with IC50 of 3 μM; little effect on Ha-Ras with IC50 of >20 μM.

PK11000 is an anti-p53 drug that stabilizes wild type and mutant p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. It exerts antitumor functions not only via reactivating p53 but also via other cellular mechanisms, such as increase of cellular ROS to toxic levels and activation of the UPR.

HDM201 is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs Mdm4.

BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells.

CBL0137 hydrochloride activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex).

AZD-5991 is a potent and selective Mcl-1 inhibitor with an IC50 of 0.7 nM in FRET assay and a Kd of 0.17 nM in surface plasmon resonance (SPR) assay.

Trolox is an antioxidant like vitamin E and it is used to reduce oxidative stress or damage.

Cynaropicrin is a sesquiterpene lactone originally isolated from artichoke (C. scolymus) that has diverse biological activities. It inhibits the growth of SKOV3, LOX-IMVI, A549, MCF-7, HCT15, and PC-3 cancer cells (IC50s = 1.1-8.7 μg/ml).

COTI-2 is an orally available thiosemicarbazone that activates mutant forms of p53. It induces apoptosis in a wide variety of human tumor cells in culture, inhibits the proliferation of colorectal cancer cell lines, and is active against human glioblastoma cell lines at nanomolar concentrations.

Tebuconazole is a triazole fungicide used agriculturally to treat plant pathogenic fungi.

ASTX660 is an orally bioavailable, non-peptidomimetic antagonist of both X chromosome-linked inhibitor of apoptosis protein (XIAP) and cellular IAP 1 (cIAP1), with potential antineoplastic and pro-apoptoticctivities. 1799328-86-1 (free base) 1799328-50-9 (HCl) 1799328-90-7 (mesylate) 1799328-88-3 (sulfate)

Iberin is a sulforaphane homolog and antioxidant. It induces phase II enzyme activity and suppresses CDK expression, inducing apoptosis in cancer cells.

GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM.

SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation.

Ecteinascidin 770 (ET-770) is a 1,2,3,4-tetrahydroisoquinoline alkaloid with potent anti-cancer activities; inhibits U373MG cells with an IC50 of 4.83 nM.

PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.

F16 is a potent growth inhibitor of the neu-overexpressing cells and also selectively inhibits proliferation of mammary epithelial as well as a variety of mouse mammary tumor and human breast cancer cell lines.

PK 11195 is a 2?Phenylindolylglyoxylyldipeptide Murine Double Minute (MDM)2/Translocator Protein (TSPO) Dual Inhibitor, and is potentially useful for the Treatment of Gliomas.

BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM.

RO8994 is a highly potent and selective series of spiroindolinone small-molecule MDM2 inhibitor, with IC50 of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays).

CUDC-427 is a potent second-generation pan-selective IAP antagonist, used for treatment of various cancers.

WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation.

RIPK1-IN-4 (compound 8) is a potent and selective type II kinase inhibitor of receptor interacting protein 1 (RIP1) kinase and binds to a DLG-out inactive form of RIP1 with an IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase.

Nec-4, a tricyclic derivative, is a potent receptor interacting protein 1 (RIP1) inhibitor, with an IC50 of 2.6 μM, Ki of 0.46 μM.