du-145

Astaxanthin (trans-Astaxanthin) is a keto-carotenoid in the terpenes class of chemical compounds. It is classified as a xanthophyll but it is a carotenoid with no vitamin A activity. It is present in most red-colored aquatic organisms. Astaxanthin has shown to mediate anti-oxidant and anti-inflammatory actions. It may be found in fish feed or some animal food as a color additive.

Benproperine phosphate (Pirexyl phosphate) is a cough suppressant.

Podophyllotoxinone, a natural compound found in Dysosma versipellis, shows inhibitory activity against L1210 leukemia and KB cells in vitro.

Cyclophosphamide is an alkylating agent type of anti-tumor drug, and its main target is DNA. Cyclophosphamide inhibits the proliferation of tumor cells by undergoing alkylation reactions with DNA, interfering with the replication and transcription processes of DNA.

4-Hydroxytamoxifen (ICI 79280) is the active metabolite of Tamoxifen, an estrogen receptor modulator (SERM) with selective and oral potency. 4-Hydroxytamoxifen has antitumor activity and may be used in breast cancer research.

Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.

Pevonedistat (MLN4924) is a potent and selective NEDD8 activating enzyme (NAE) inhibitor (IC50=4.7 nM) with therapeutic potential for myelodysplastic syndromes (MDS) and antitumor activity.

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.

Topotecan hydrochloride (NSC609699) is an antineoplastic agent used to treat ovarian cancer.

Lithocholic acid (3α-Hydroxy-5β-cholanic acid) is a toxic secondary bile acid, They were FXR antagonists (IC50=0.7, 1.4 μM), EphA2 antagonists (IC50=48, 66 μM) and EphB4 antagonists (IC50=141 μM). Lithocholic acid can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is a cleanser that dissolves fat for absorption and is itself absorbed.

Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

Ecteinascidin 770 inhibits SARS-CoV-2 and Mycobacterium tuberculosis by inhibiting cancer cell viability through RDRP1 (RNA-dependent RNA polymerase 1).

EL-102 is a HIF1α inhibitor with anticancer activity that inhibits microtubule protein polymerization and can be used to study prostate cancer.

FX-11 (LDHA Inhibitor FX11) is A potent, selective and competitive specific inhibitor of lactate dehydrogenase A (LDHA) with a Ki of 8 μM. FX-11 can activate PKM2 (pyruvate kinase M2). FX-11 can reduce ATP levels, induce oxidative stress and ROS production, and cause cell death. FX-11 appeared antitumor activity during xenotransplantation of lymphoma and pancreatic cancer.

Everolimus (SDZ-RAD) is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.

GSTP1-1 inhibitor 2 (Compound 5g) is an inhibitor of hGSTP1-1 (glutathione S-transferase P1-1), exhibiting an IC50 of 12.2 μM. It demonstrates substantial cytotoxicity against the cell lines DU-145, PC3, and MCF-7, with CC50 values of 36.6, 11.9, and 17.4 μM respectively, making it relevant for research in cancer therapeutics.

Aurora A inhibitor4 (compound C9) is a potent inhibitor of Aurora A, with GI50 values of 4.26 μM in DU 145 cells and 7.08 μM in HT-29 cells.

Anticanceragent 264 (Compound 5w) is an anticancer compound that exhibits significant antiproliferative activity in tumor cell lines, with an IC50 range of 7.5-33.67 μM. It notably induces cell cycle arrest at the G2/M phase in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines. This compound reduces key cell cycle proteins CDK1, CDK2, and Cyclin B1 in a dose-dependent manner and has strong binding activity with differentiation inhibitors and DNA-binding proteins. Anticanceragent 264 is useful for research in the cancer disease domain.

CYP17A1-IN-1 (Compound 14) is an inhibitor of CYP17A1 with an IC50 of 26 nM. It exhibits cytotoxicity in androgen-sensitive prostate cancer cells, specifically LNCaP, and hinders the migration of DU-145 cells.

PLK1-IN-14 (Compound Hit-4) is a selective PLK1 inhibitor with an IC50 of 22.61 pM for PLK1, and an IC50 of 0.09 nM for inhibiting the proliferation of DU-145 prostate cancer cells. It is applicable in prostate cancer research.

GLI1-IN-3 (Compound 11a) is a triterpenoid-like compound that inhibits Hedgehog signaling in cancer cells with GLI1 overexpression. It suppresses the proliferation of non-small cell lung cancer and prostate cancer cell lines with excessive Hh signaling activation. Additionally, GLI1-IN-3 reduces the expression of GLI1 protein and its target genes associated with tumor progression and proliferation in A549 and DU-145 cancer cells.

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.

ADAR1-IN-1 is a potent ADAR1 inhibitor. It significantly suppresses the proliferation of DU-145 cells (IC50 = 1.11 μM), inhibits colony formation, migration, and invasion, and induces cell cycle arrest and apoptosis. ADAR1-IN-1 effectively and safely impedes tumor growth and can be utilized in prostate cancer (PCa) research.