du-145

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 (ICI47699) is a selective and orally effective estrogen receptor modulator (SERM). Tamoxifen has both inhibitory (e.g., mammary cells) and activating (e.g., bone, liver, and uterine cells) activity against estrogens.

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.

Cyclophosphamide is an alkylating agent used in the treatment of several forms of cancer including leukemias, lymphomas and breast cancer.

Lithocholic acid (3α-Hydroxy-5β-cholanic acid) is a bile acid formed from chenodeoxycholate by bacterial action, usually conjugated with glycine or taurine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as cholagogue and choleretic.

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

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

Tanespimycin (KOS 953) (17-AAG) is an inhibitor of Hsp90 that selectively inhibits BT474 tumor cell Hsp90 (IC50: 5 nM).

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

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.

MDK-4204, an anticancer agent, shows significant anti-cancer activity with IC50 values of 8.8 µM and 9.5 µM in PC-3 and DU-145 cells, respectively.

1. 4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) has antiviral activity, including anti-HIV-1 integrase activity. 2. 4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) shows anti-hepatotoxic activity.

Panduratin A is a natural chalcone derivative with inhibitory activity against MMP-9 in human oral epidermoid carcinoma KB cells; inhibitory activity against the NS3 protease of DENV-2 (Ki=25 μM); significant cytotoxicity against human androgen-independent prostate cancer cells PC-3 and DU-145; and also able to activate the LKB1-AMPK- PPARα δ signaling pathway and enhance the oxidative capacity of myocyte mitochondria.

Calpain Inhibitor-2 is a lipophilic calpain inhibitor, and they showed moderate to good anti-proliferative effects in vitro compared to melanoma cell lines (A-375 and B-16F1) and PC-3 prostate cancer cells. was able to inhibit the invasion of 80% of DU-145 cells.

OXi8007 is a water-soluble phosphate and a prodrug for OXi8006, a microtubulin-binding compound. As a vascular disrupting agent with potential anticancer activity, OXi8007 exhibits strong cytotoxicity against the DU-145 tumor cell line and significantly disrupts the tumor vascular system.

TAK1 inhibitor is an inhibitor, which can inhibit MCF-7, A549, DU-145 and MDA MB-231, with IC50 of 0.021, 0.14, 0.064 and 0.19, respectively. TAK1 inhibitor showed good antibacterial activity with microphones ranging from 93.7 to 46.9μg mL and from 7.8 to 5.8μg mL.

Ethonafide is an anthracene-containing derivative of amonafide that belongs to the azonafide series of anticancer agents. The lack of cross-resistance in multidrug-resistant cancer cell lines and the absence of a quinone and hydroquinone moiety make ethonafide a potentially less cardiotoxic replacement for existing anthracene-containing anticancer agents. Ethonafide was cytotoxic against three human prostate cancer cell lines at nanomolar concentrations. Ethonafide was found to be better tolerated and more effective at inhibiting tumor growth compared with mitoxantrone in a human xenograft tumor regression mouse model. Mechanistically, we found that ethonafide inhibited topoisomerase II activity by stabilizing the enzyme-DNA complex, involving both topoisomerase IIalpha and -beta. In addition, ethonafide induced a potent G(2) cell cycle arrest in the DU 145 human prostate cancer cell line. By creating stable cell lines with decreased expression of topoisomerase IIalpha or -be......

PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4 SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with distribution to both plasma and bone marrow. No myelosuppression was seen in non-tumor bearing SCID mice given a single dose just under the acute lethal dose. The COMPARE algorithm in the NCI-60 cell line panel demonstrated that PC-046 closely correlated to other known tubulin destabilizing agents (correlation coefficients ≈0.7 for vincristine and vinblastine). Mechanism of action studies showed cell cycle arrest in metaphase and inhibition of tubulin polymerization. Overall, these studi......

Dihydrodaidzin shows cytotoxic activities against human stomach carcinoma (Hs 740.T, Hs 756 T), breast adenocarcinoma (Hs 578 T, Hs 742.T), and prostate carcinoma (DU 145, LNCaP-FGC) cell lines.