skov3

Tubulin inhibitor 6 (iHAP1) is an inhibitor of tubulin and a potent inhibitor of multiple cancer cell lines.

DOTA-NHS-ester is a linker for affibody molecules with applications in small animal PET, SPECT, and CT. It can be used to label radiotherapeutic agents or imaging probes for tumor detection.

Aloesin is a C-glycosylated chromone compound found in aloe (Liliaceae) that inhibits tyrosinase (IC50 = 0.9 mM), an enzyme responsible for catalyzing the first step of the conversion of tyrosine to melanin.

T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively; it inhibits nuclear factor/κB (NF/κB).

NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.

Songorine (Napellonine) shows favorable anti-tumor activity in preliminary pharmacological verification trials including cell proliferation and molecular docking assays.

RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.

Ceranib-2 (3-[(E)-3-(4-hydroxyphenyl)prop-2-enoyl]-4-phenyl-1H-quinolin-2-one) is an inhibitor of ceramidase with an IC50 of 28 μM in SKOV3 cells. Ceranib-2 decreases levels of sphingosine and S1P, induces cell apoptosis and exhibits anticancer activity.

Tubulin inhibitor 8 is an inhibitor of tubulin and various cancer cell lines and inhibits tubulin polymerisation and K562 cell growth with an IC50 of 0.73 μM and 14 nM respectively.

ATG7-IN-1 is a selective ATG7 inhibitor with an IC50 of 62 nM.

Carboplatin (JM-8) is a cisplatin derivative, a DNA synthesis inhibitor. Carboplatin binds to DNA, inhibits replication and transcription, and induces cell death. Carboplatin has antitumor activity.

Capsaicin is an active natural component found in chili peppers and acts as a TRPV1 agonist (EC50 = 0.29 μM). It possesses multiple activities, including pain relief, antitumor, anti-inflammatory, antioxidant, and neuroprotective effects, as well as some neurotoxicity. Capsaicin can be used to establish itch models.

HP-β-CD (HP-β-CD) is a widely used drug delivery vehicle to improve stability and bioavailability.

Duocarmycin TM is a DNA alkylator. Duocarmycin TM is an exceptionally potent antitumor antibiotic.

Antitumor agent-187 (compound I) is an isoflavone derivative with antitumor activity. It exhibits IC50 values of 5.23 μM and 2.63 μM against A2780 and SKOV3 cell lines, respectively.

Apoptosis inducer37 (Derivative 10) is an agent that induces apoptosis and exhibits anticancer properties by causing cell cycle arrest at the S-G2/M phase and promoting cell apoptosis. It significantly inhibits HCT116, SKOV3, and HepG2 cancer cells with IC50 values of 24.98 μM, 26.15 μM, and 23.09 μM, respectively. Apoptosis inducer37 demonstrates antitumor activity and can be utilized in ovarian cancer research.

HQY1428 is an orally active CDK12 inhibitor. It impedes DNA replication, causing cell cycle arrest at the G2/M phase in SKOV3 cells, and induces DNA double-strand breaks as well as apoptosis. In the SKOV3 xenograft mouse model, HQY1428 demonstrates antitumor activity. Additionally, when combined with the HER2 inhibitor Lapatinib in the NCI-N87 xenograft mouse model, HQY1428 produces a synergistic therapeutic effect.

Tubulin polymerization-IN-66 (Compound 13) inhibits colony formation and tubulin polymerization while also inducing apoptosis. It reduces cell viability in A549, A2780, SKOV3, and HCC827 cells, with IC50 values of 0.84, 0.38, 0.31, and 0.34 nM, respectively. Additionally, Tubulin polymerization-IN-66 is effective against the Paclitaxel-resistant A2780/T cancer cell line as well as its parent cell line, A2780.

SB-743921 hydrochloride (SB743921 HCl) is an effective inhibitor of kinesin spindle protein, KSP, (Ki =0.1 nM).

NSC756093 potentially inhibits GBP1:PIM1 interaction. NSC756093 can be used in ovarian cancer studies.

Erysolin is a natural product with anti-cancer potential. It is cytotoxic to a variety of cancer cells (DU145, HCT 116, MCF7, HEP3B, SKOV3, SF-268) and has antibacterial activity against Escherichia coli.

19,20-Epoxycytochalasin D is a fungal metabolite that has been found in the endophytic fungus Nemania sp. UM10M. It is active against the chloroquine-sensitive and -resistant strains of P. falciparum (MIC = 0.4 ng/ml for both) without inducing cytotoxicity in Vero cells. It is cytotoxic to BT-549, LLC-PK11, and P388 cells (IC50s = 7.84, 8.4, and 0.16 µM, respectively) but not SK-MEL, KB, or SKOV3 cells up to a concentration of 10 µM.

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50= 46 nM) and STAT3 activation.1It binds to STAT3 (Kd= 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16/F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg/kg, respectively. 1.Huang, R., Jing, X., Huang, X., et al.Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3J. Med. Chem.63(4)1544-1563(2020)

Anhydroepiophiobolin A is a sesterterpenoid fungal metabolite that has been found in B. oryzae. It is cytotoxic to HepG2 and K562 cells (IC50s = 47.1 and 35.6 μM, respectively) as well as A549, SKOV3, SK-MEL-2, XF498, and HCT15 cells (IC50s = 1.6-1.9 μg/ml). Anhydroepiophiobolin A is phytotoxic to S. viridis and D. erucoides in a leaf puncture assay.