Survivin Inhibitor

Sepantronium bromide (YM-155) is a survivin inhibitor with an IC₅₀ of 0.54 nM.

Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors.

FL118 (10,11-(Methylenedioxy)-20(S)-camptothecin), a Camptothecin (HY-16560) analogue, is a potent and orally active survivin inhibitor. FL118 binds to oncoprotein DDX5 (p68) to dephosphorylates and degrades DDX5. FL118 can be used for the research of cancer.

Levonorgestrel is an orally active inhibitor of progesterone (HY-N0437). Levonorgestrel has anticancer activity and can induce Apoptosis. Levonorgestrel can be used as a contraceptive and in combination with other medications. Levonorgestrel can be used in the study of osteoporosis and uterine leiomyoma.

Terameprocol is an inhibitor targeting the Sp1 transcription factor, which can selectively inhibit the transcription of Sp1-dependent genes. Terameprocol exerts its effects by inhibiting Sp1-mediated gene transcription, such as reducing the expression of genes like CDC2, survivin and HMGB1, thereby arresting the cell cycle, inducing apoptosis, and suppressing the inflammatory response. Terameprocol exhibits anti-proliferative, pro-apoptotic, and anti-inflammatory activities and is currently mainly used in the research of diseases such as cancer and pulmonary arterial hypertension[1][2][3].

Scopadulciol is an orally effective β-catenin degrader, HSV-TK activator and proton pump inhibitor. By inducing β-catenin degradation, Scopadulciol downregulates the expression of downstream target genes such as cyclin D1, c-myc, and survivin; it also upregulates DR4/DR5 and downregulates Bcl-2, thereby exerting cytotoxicity and inducing apoptosis in cancer cells. Scopadulciol enhances the tumor-killing and bystander effects of prodrugs via activating HSV-TK, and can inactivate HSV-1. It shows synergistic antiviral effects when combined with Acyclovir (HY-17422) or Ganciclovir (HY-13637), with no cytotoxicity as a single agent. Scopadulciol can be applied in research related to bladder cancer, cervical cancer, glioblastoma, and digestive system cancers.

Anticancer agent 324 is a Survivin inhibitor. Anticancer agent 324 competitively binds to Survivin’s linker region and triggers proteasomal IAP degradation. Anticancer agent 324 blocks Borealin binding and chromosomal passenger complex formation, and inhibits Survivin-CRM1 nuclear-cytoplasmic transport. Anticancer agent 324 activates extrinsic (caspase-8) and intrinsic (caspase-9) apoptotic pathways, activates executioner caspases-3 and caspases-7, and arrests cell cycle. Anticancer agent 324 can be used for the research of breast cancer.

N-Hydroxyphthalimide is a blocking agent and catalyst. N-Hydroxyphthalimide promotes oxidation reactions by generating PINO free radicals and activating hydrogen atom transfer processes. N-Hydroxyphthalimide reduces the expression of anti-apoptotic proteins Survivin and Bcl-xL and activates caspase 9 and caspase 3. N-Hydroxyphthalimide induces Apoptosis. N-Hydroxyphthalimide inhibits the phosphorylation of mTOR (Ser2448, Ser2481) and Akt (Ser473). N-Hydroxyphthalimide has anticancer effects against breast and colon cancer.

Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC₅₀ value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases.

Ganoderma Lucidum/Reishi Extract is a Ganoderma lucidum extract. Ganoderma Lucidum/Reishi Extract reduces the expression of c-Myc, BCL-2, BCL-XL, TERT, PDGFB, eIF4G, Survivin, β-catenin, and eIF4E. Ganoderma Lucidum/Reishi Extract downregulates the gene expression of MMP-9. Ganoderma Lucidum/Reishi Extract upregulates the expression of IL8. Ganoderma Lucidum/Reishi Extract is applicable to the research of inflammatory breast cancer. Ganoderma Lucidum is used in the research of various diseases, such as allergy, arthritis, hypertension, neurasthenia, inflammation, and cancer.

Propionyl-L-carnitine is an orally active L-carnitine derivative. Propionyl-L-carnitine has a high affinity for muscle L-carnitine transferase. Propionyl-L-carnitine increases Apoptosis, Bax, and reduces NF-κB, VCAM-1, MCP-1, and survivin. Propionyl-L-carnitine activates Src kinase, Akt, induces p-AMPK and nitric oxide synthesis. Propionyl-L-carnitine alleviates cardiovascular disease, obesity, and colitis.

LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors.

Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.

2,5-Dimethylcelecoxib is an analogue of celecoxib (HY-14398) with anticancer activity but without COX-2 inhibitory activity. 2,5-Dimethylcelecoxib exerts its anti-cancer cell proliferation effect by inhibiting the core mechanism of the Wnt/β-catenin signaling pathway. 2,5-Dimethylcelecoxib also inhibits T-cell factor-dependent transcriptional activity and inhibits expression of the Wnt/β-catenin target gene products cyclin D1 and survivin.

GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells.

23-Hydroxybetulinic acid (Anemosapogenin) is an orally active triterpenoid with broad-spectrum anticancer activity. 23-Hydroxybetulinic acid reduces the levels of Bcl-2 and survivin, elevates the level of Bax, promotes the cleavage/activation of caspase-3 and caspase-9, and induces apoptosis via the endogenous mitochondrial pathway involving cytochrome C release and mitochondrial membrane potential disruption. 23-Hydroxybetulinic acid arrests the cell cycle at S and G1 phases, inhibits cancer cell proliferation, blocks the MAPK signaling pathway, regulates MMP2, and induces autophagic apoptosis by upregulating beclin-1. 23-Hydroxybetulinic acid inhibits the activity and efflux function of P-gp, increases the intracellular accumulation of chemotherapeutic drugs, and synergistically enhances cytotoxicity with Doxorubicin (HY-15142). 23-Hydroxybetulinic acid inhibits the phosphorylation and nuclear translocation of STAT6, blocks M2 macrophage polarization, and reduces M2 macrophage-mediated apoptosis resistance of colon cancer cells. 23-Hydroxybetulinic acid can be used in related studies on chronic myeloid leukemia, hepatocellular carcinoma, sarcoma 180, multidrug-resistant breast cancer, leukemia, Doxorubicin-induced cardiotoxicity, and colorectal cancer.

DK419 is a potent and orally active Wnt/β-catenin signaling inhibitor, with an IC₅₀ of 0.19 μM. DK419 reduces protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin and induces production of pAMPK.

LQZ-7F, a survivin dimerization inhibitor, induces spontaneous apoptosis and synergizes with Docetaxel in prostate cancer cells. LQZ-7F dose-dependently inhibits survival of both PC-3 and C4-2 cells with IC₅₀s of 2.99 and 2.47 µM, respectively.

Cucurbitacin IIa (Hemslecin A) is an orally active, blood-brain barrier-permeable EGFR inhibitor with an IC₅₀ of 1.455 nM against human EGFR. Cucurbitacin IIa induces caspase-3-dependent apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton via actin aggregation, arrests the cell cycle at the G2/M phase, and exerts anti-inflammatory activity by inhibiting the EGFR-MAPK signaling pathway. Cucurbitacin IIa can be used in the research of inflammation-related diseases, depression, and cancers such as non-small cell lung cancer.

α-Santalol (cis-α-Santalol), a naturally occurring sesquiterpene, is an orally active anticancer agent and apoptosis inducer. α-Santalol activates caspase-3 to drive apoptotic processes. >α-Santalol induces apoptosis, decreases cell viability, and causes PARP cleavage in human prostate cancer cells. α-santalol inhibits Akt/Survivin pathway to induce cell death. α-Santalol can be used for the research of prostate cancer and diabetes mellitus.