| DC70369 |
Dual DRAK1 and DRAK2 inhibitor 1 |
Dual DRAK1 and DRAK2 inhibitor 1 is a potent, dual DRAK2/1 inhibitor Kd value of 9/5 nM, respectively;
Dual DRAK1 and DRAK2 inhibitor 1 also is a functional inhibitor of DRAK2/1 enzymatic activity with IC50 of 0.86 and 2.25 uM.
Dual DRAK1 and DRAK2 inhibitor 1 is a chemical tool compound to study DRAK1 and DRAK2 biology. |
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| DC70473 |
GW440139B |
GW440139B is a potent RIPK3 inhibitor, suppresses necroptosis driven by dimerizable RIPK3 with IC50 of 73.6 nM.GW440139B inhibits TNF- and TRIF-mediated necroptosis independent of RIPK1-RIPK3 interaction, directly inhibited RIPK3-mediated MLKL phosphorylation at Ser345, thus inhibiting necroptosis. |
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| DC70475 |
H203 |
H203 is a potent dual Mdm2/MdmX inhibitor with Ki of 2/11 nM, respectively;
H203 significantly reduced cell viability in the cells overexpressing both Mdm2 and MdmX, and a significant and dose-dependent decrease in cell number in H203-treated cells lacking Mdm2 or MdmX.
H203-mediated decrease in cell viability is strictly p53-dependent and H203 affects MdmX more specifically than nutlin-3a.
H203 induced the expression of the p21 gene but not the p53 gene in treated cancer cells. |
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| DC70476 |
H210 |
H210 is a potent dual Mdm2/MdmX inhibitor with Ki of 9.66/2.89 nM, respectively. |
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| DC70504 |
iHPCAL1 |
iHPCAL1 is a ferroptosis inhibitor that effectively inhibits RSL3-induced cell death, directly interacts with HPCAL1 and significantly inhibits HPCAL1 protein expression at 1.25-5 uM in HT-1080 and Calu-1 cells.iHPCAL1 delayed thermal-induced HPCAL1 protein degradation in cellular thermal shift assays (CETSAs), failed to affect the phosphorylation of PRKCQ, but inhibited the phosphorylation of HPCAL1 as well as the autophagic degradation of CDH2 induced by RSL3.The suppression of HPCAL1 phosphorylation and function induced by iHPCAL1 occurs downstream of PRKCQ phosphorylation.Bortezomib, but not chloroquine, prevented iHPCAL1-induced HPCAL1 protein degradation, iHPCAL1 stimulates the degradation of HPCAL1 through the proteasome pathway, thereby limiting ferroptosis.iHPCAL1 inhibited the anticancer activity of Imidazole ketone erastin (IKE) in a xenograft tumor model after inoculating HT-1080 cells into athymic nude mice or in an orthotopic pancreatic tumor model in which KPC cells, with no significant effect on IKE-induced GPX4 degradation in the xenograft tumor model.iHPCAL1 (10 mg/kg) protects against ferroptosis-associated acute pancreatitis in mice. |
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| DC70564 |
Leusin-1 |
Leusin-1 (Leukemia specific inhibitor 1) is a cell cycle phase specific inhibitor that specifically arrest leukemia cells during G2-phase and triggers an apoptotic cell death (CCRF-CEM IC50= 2.66 uM and TOM1 IC50= 0.877 uM).Leusin-1 showed specificity towards acute lymphoblastic leukemia cells than other types of leukemias, non-bloodborne cancers, or normal cells.Leusin-1 also arrested cells with lower levels of p-H3 (present only in M-phase) and increased levels of Cyclin A (levels peak in G2-phase).Leusin-1 does not target tubulin, Leusin-1 inhibited colony formation similar to Taxol. |
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| DC70648 |
NH-23-C2
Featured
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NH-23-C2 (Caspase-2 inhibitor NH-23-C2) is a potent, selective and cell-permeable endogenous caspase-2 inhibitor, does not block caspase-3 or caspase-8.NH-23-C2 displays off-reactivity with cysteine and threonine proteases (cathepsins B, L, V, S).HCT116 cells were preincubated with NH-23-C2 inhibitor, MDM-2 cleavage was inhibited in a concentration-dependent manner (IC50 =3.11 μM).NH-23-C2 selectively block caspase-2 activity and caspase-2-mediated MDM-2 cleavage. |
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| DC70652 |
Nigratine
Featured
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Nigratine (6E11) is a highly specific, non-ATP competitive inhibitor of RIPK1 kinase (IC50=1.6 uM), inhibits necroptosis and ferroptosis.Nigratine inhibits necroptotic cell-death induced by TNF-α in Jurkat-Fadd def cells with IC50 of 4.6 uM.Nigratine is significantly more potent than the specific RIPK1 necroptosis inhibitor, Nec-1s.Nigratine (50 uM) strongly inhibits the ferroptotic cell death induced by excess of glutamate, erastin, and RSL3, in both murine HT22 and human SH-SY5Y cell lines, protects SH-SY5Y human neuroblastoma cell line from cell death triggered by both class I and II-inducers of ferroptosis.Nigratine protects porcine kidney epithelial LLC-PK1 cell line from lipid peroxidation and cell death triggered by RSL3.Nigratine protects human bronchial organoids from necroptosis and ferroptosis. |
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| DC70660 |
NPD4928 |
NPD4928 (NPD 4928) is a small molecule that enhances ferroptosis via inhibition of ferroptosis suppressor protein 1 (FSP1).NPD4928 enhanced the sensitivity of various cancer cells to GPX4 inhibitor RSL3. |
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| DC70695 |
PG3d |
PG3d (Caspase-6 inhibitor PG3d) is a cell-active, allosteric and irreversible, non-competitive Caspase-6 inhibitor.PG3d preferentially inhibits the cleavage of protein over peptide substrates both with purified proteins and in live cells.PG3d prevents the C6 (Caspase-6)-HTT interaction and prevents mHTT1-586 mediated activation of procaspase-6.PG3d specifically inhibits the cleavage of protein, but not peptide substrates of Caspase-6. |
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| DC70698 |
PK68
Featured
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PK68 (RIPK1 inhibitor PK68) is a potent necroptosis inhibitor seletively targeting RIPK1 kinase activity, potently inhibits TNF-induced necroptosis (EC50, 23 and 13 nM in human and mouse cells, respectively).PK68 blocks cellular activation of RIPK1, RIPK3, and MLKL upon necroptotic stimuli.PK68 is a type II inhibitor of RIP1 kinase, highly selective inhibitor of RIPK1 kinase activity with IC50 of 90 nM, does not affect RIPK3 kinase activity at 1 uM, also demonstrated a reasonable selectivity against a panel of 369 kinases.PK68 exhibits a favorable pharmacokinetic profile and no obvious toxicity in mice.PK68 ameliorates TNF-induced systemic inflammatory response syndrome, and displays preventive suppression of tumor metastasis in the mouse cancer models. |
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| DC70710 |
Procaspase-6 inhibitor 12 |
Procaspase-6 inhibitor 12 is a small molecule, noncovalent, allosteric inhibitor of procaspase-6 with KD of 0.47 uM.Procaspase-6 inhibitor 12 binds to pro-C6 at the dimer interface and contacts amino acids Y198, T199 and E214.Procaspase-6 inhibitor 12 significantly stabilizes procaspase-6.Procaspase-6 inhibitor 12 prevents the activation of the Caspase-6 zymogen by mHTT1–586 in COS-7 cells. |
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| DC70711 |
Procaspase-6 inhibitor 13 |
Procaspase-6 inhibitor 13 is a small molecule, noncovalent, allosteric inhibitor of procaspase-6 with KD of 0.38 uM.Procaspase-6 inhibitor 13 binds to pro-C6 at the dimer interface and contacts amino acids Y198, T199 and E214.Procaspase-6 inhibitor 13 significantly stabilizes procaspase-6. |
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| DC70773 |
SGC-STK17B-1 |
SGC-STK17B-1 is a potent, selective, ATP-competitive inhibitor of death-associated protein kinase family member STK17B (DRAK2) with IC50 of 34 nM, >100-fold selectivity over STK17A;
SGC-STK17B-1 is also >100-fold selective over all of the other kinases tested, with only STK17A, CAMKK1, and AURKB (IC50s=5-9 uM) in panel of 403 wild type human kinase assays.
SGC-STK17B-1 demonstrated the highest cell potency in the NanoBRET target engagement assay (IC50=190 nM).
SGC-STK17B-1 is the first truly potent and selective chemical probe of STK17B. |
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| DC70790 |
SN-6109 |
SN-6109 (SN6109) is a small molecule inhibitor RIPK-1 with IC50 of 0.45 uM in radiometric kinase assays.SN-6109 reduced MLKL activation EC50 2.5-11.5 uM under long-term necroptosis execution in murine fibroblast L929 cells, and full protection from ATP depletion and membrane leakage in human and murine cells.SN-6109 decreased p-MLKL/MLKL and p-RIPK3/RIPK3 ratios in mouse liver tissue, showed efficacy in an in vivo model of tissue injury and inflammation driven by RIPK1/3-dependent cell death. |
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| DC70813 |
SW IV-134 |
SW IV-134 is a sigma-2/SMAC drug conjugate, chemically linked the sigma-2 ligand SW43 to the Smac mimetic SW IV-52.SW IV-134 slowed tumor growth and improved survival in murine models of pancreatic cancer.SW IV-134 significantly reduced tumor burden and improved overall survival in a mouse xenograft model of ovarian cancer without causing significant adverse effects to normal tissues.SW IV-134 induced degradation of cIAP-1 and cIAP-2 leading to NF-қB activation and TNFα-dependent cell death. |
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| DC70814 |
SW IV-52 |
SW IV-52 is a pro-apoptotic small molecule SMAC mimetic and XIAP inhibitor. |
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| DC70904 |
WEHI-7326 |
WEHI-7326 (WEHI 7326) is a specifi mitotic inhibitor and potential anticancer agent, causes cell cycle arrest in G2/M, cell death in vitro (MDA-MB-231 IC50=24.4 nM), and displays efficacious anti-tumor activity in vivo.WEHI-7326 induces cell death in a broad range of cancer cell lines, including taxane-resistant cells, and inhibits growth of human colon, brain, lung, prostate and breast tumors in mice xenografts.WEHI-7326 exceeded potency of myoseverin B by almost ten-fold, did not show any significant cytotoxic activity in vitro (IC50>40 uM) in HepG2 cells.WEHI-7326 prolongs survival in mouse models of high-risk neuroblastoma and leads to complete tumor regression when used in combination with standard-of-care relapse therapies. |
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| DC70928 |
ZB-R-55 |
ZB-R-55 is a potent and selective RIPK1 inhibitor with IC50 of 5.7 nM, 10-fold more potent than GSK2982772.ZB-R-55 is a dual-mode RIPK1 inhibitors occupying both the allosteric and the ATP binding pockets.ZB-R-55 exhibits excellent kinase selectivity, good oral pharmacokinetics and good therapeutic effects in the LPS-induced sepsis model. |
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| DC70933 |
ZH07 |
ZH07 (Dual Mcl-1/Bfl-1 inhibitor 24) is a potent, selective dual Mcl-1 and Bfl-1 inhibitor, binds both Mcl-1 and Bfl-1 with Ki of 97 nM and 100 nM, respectively.ZH07 displays appreciable selectivity (>250-fold) over Bcl-2/Bcl-xL.ZH07 induces dose-dependent disruption of interactions between BL-Bim and endogenous Mcl-1 and Bfl-1, without affecting the complexes between BL-Bim and Bcl-2 or Bcl-xL.ZH07 demonstrates on-target cellular activity in model lymphoma cell lines. |
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| DC70934 |
ZH97
Featured
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ZH97 is a selective and covalent small-molecule inhibitor of BFL-1 protein with binding Ki of 0.41 uM, >200-fold selectivity over MCL-1.ZH97 does not bind to BCL-xL, BCL-2, TEAD2, TEAD4, MDM2, MDMX, BRD2 BD1, BRD2 BD2, BRD3 BD1, BRD3 BD2, BCL9, PD1/PD-L1 (Ki>400 uM).ZH97 modifies BFL-1 at the C55 residue, blocks BFL-1/BID interaction in vitro.ZH97 dose-dependently increased cytoplasmic cytochrome c level in U937 cells, has cell growth inhibition with IC50 of 2.8 uM, 5.5 uM, 7.7 uM, 6.8 uM, and 3.9 uM in U937, Kasumi-1, K562, MM.1S, and MV4-11 cell lines, respectively.ZH97 inhibits BFL-1/PUMA interaction in cell lysate and is effective in cancer cells that harboring highexpression level of BFL-1. |
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| DC70938 |
ZJU-37 |
ZJU-37 is a novel small molecule, BBB penetrant RIPK1 kinase inhibitor (IC50=366.4 nM) with higher potency than Nec-1s, prevents TNFα-induced necroptosis of Jurkat FADD−/− cells with IC50 of 185.2 nM.ZJU-37 promotes oligodendrocyte progenitor cells (OPCs) proliferation in vitro with higher efficacy than Nec-1s, enhances remyelination in vivo.ZJU-37 promotes transcription of PDGFRα and proliferation of OPCs via NF-κB. |
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| DC70951 |
JMX0293 |
JMX0293 is an O-alkylamino-tethered salicylamide derivative compound. JMX0293 maintains good potency against MDA-MB-231 cell line (IC50 = 3.38 μM) while exhibiting very low toxicity against human non-tumorigenic breast epithelial cell line MCF-10A (IC50> 60 μM). JMX0293 inhibits STAT3 phosphorylation and contribute to apoptosis in TNBC MDA-MB-231 cells. JMX0293 significantly suppresses MDA-MB-231 xenograft tumor growth in vivo without significant toxicity. |
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| DC71004 |
Apaziquone |
Apaziquone (EO-9), an analog of Mitomycin C, is a prodrug that is activated to DNA damaging species by oxidoreductases (particularly NQO1). Apaziquone has the ability to kill aerobic and/or hypoxic cancer cells. Apaziquone, a bioreductive alkylating agent, inhibits cell proliferation and induces apoptosis in oral squamous cell carcinoma (OSCC) cells. Apaziquone significantly reduces oral tumor xenograft volume in immunocompromised NOD/SCID/Crl mice. |
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| DC71015 |
Cardanol monoene |
Cardanol monoene (Cardanol C15:1) is a phenolic compound which can be found in cashew nut shell liquid. Cardanol monoene can induce mitochondria-associated apoptosis in human melanoma cells. |
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| DC71076 |
M24 |
M24 is a Mcl-1 selective inhibitor. M24 exhibits good binding affinity against Mcl-1 with Ki value of 0.33 μM. M24 exhibits good anti-proliferative activity and induce apoptosis in HepG2 cells. |
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| DC71137 |
AG6033 |
AG6033 is a potential novel CRBN modulator. AG6033 suppresses various tumor cells by modulating the interactions between CRBN and various antitumor target proteins. AG6033 can cause GSPT1 and IKZF1 degradation. AG6033 induces CRBN-dependent cytotoxic effect. |
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| DC71166 |
YM281 |
YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma. |
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| DC71167 |
DMUP |
DMUP is a potent CD47-SIRPα axis inhibitor. DMUP induces apoptosis and increases the macrophage phagocytosis in A549 cells. DMUP decreases the expression of CD47 and SIRPα protein. DMUP shows antitumor activity. |
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| DC71225 |
Lumichrome |
Lumichrome, a photodegradation product of Riboflavin, is an endogenous compound in humans. Lumichrome inhibits human lung cancer cell growth and induces apoptosis via a p53-dependent mechanism. |
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