HCT 116

Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2/PLK3 (IC50s: 5/56 nM).

ABT-737 is a BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w (EC50=30.3 nM/78.7 nM/197.8 nM). ABT-737 exhibits antitumor activity and anti-aging activity.

Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.

LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF.

Oxiconazole nitrate (Ro 13-8996) is the nitrate salt form of oxiconazole, a broad-spectrum imidazole derivative with antifungal activity. Likely inhibiting cytochrome P450-dependent demethylation of lanosterol, it prevents ergosterol synthesis, a crucial component of the fungal cell membrane. This disruption of membrane synthesis and integrity alters permeability, promotes loss of essential intracellular components, and inhibits fungal cell growth.

AGI-24512 is a potent inhibitor of methionine adenylyltransferase 2α (MAT2A) (IC50: 8 nM).AGI-24512 shows antiproliferative activity in MTAP-deficient cancer cells.AGI-24512 inhibits MAT2A, which causes DNA damage in MTAP, and is often used in conjunction with anticancer compounds in cancer research.

GN44028 (N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-1,4-dihydroindeno[1,2-c]pyrazol-3-amine) is a hypoxia-inducible factor inhibitor of (HIF)-1 (IC50: 14 nM). GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity. However, It can not be suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.

Indotecan (LMP-400) is an effective inhibitor of topoisomerase 1(Top1) (IC50: 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively).

Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase and a potent first-in-class anti-cancer agent, inducing cell apoptosis and inhibiting the growth of TNBC cancer cell lines (IC50s: 10 nM - 20 nM).

Bromosporine is a broad spectrum inhibitor for bromodomains for BRD2/4/9 and CECR2 (IC50: 0.41/0.29/0.122/0.017 μM), respectively.

CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.

MG-101 (Calpain inhibitor I) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.

AP-III-a4 (ENOblock) is the first non-substrate analogue that directly binds to enolase to inhibit its catalytic activity with an IC50 of 0.576 μM, thereby blocking cancer cell metastasis in vivo. AP-III-a4 can be used in research on tumor metabolism, metastasis, and diseases related to carbohydrate metabolism.

VLX600 is an iron-chelating oxidative phosphorylation (OXPHOS) inhibitor, is a cell-permeable anticancer agent. It acts by reducing mitochondrial oxidative phosphorylation in tumor cells.

HM03 is a potent and selective inhibitor of HSPA5 and exhibits anticancer activity.

NSAH (2-hydroxy-N'-[(E)-(2-hydroxynaphthalen-1-yl)methylidene]benzohydrazide) is a nonnucleoside inhibitor of human ribonucleotide reductase (hRR).with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively.

HS-1793, a resveratrol analogue, downregulates the expression of hypoxia-induced HIF-1 and VEGF and inhibits tumor growth of human breast cancer cells in a nude mouse xenograft model

LY3405105 (1-Piperidinecarboxylic acid, 4-[[5-methyl-3-(1-methylethyl)pyrazolo[1,5-a]pyrimidin-7-yl]amino]-, 1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]-3-pyrrolidinyl ester) is a novel CDK7 inhibitors.

β-catenin-IN-2, a potent inhibitor of β-catenin, is suitable for use in colorectal cancer research.

MPT0B390 is an inhibitor of HDAC and a TIMP3 inducer inhibiting tumor growth, metastasis, and angiogenesis.

TNIK-IN-5 is an potent TNIK inhibitor (IC50= 0.05 μM). TNIK-IN-5 potently inhibits Wnt signaling in intact cells. TNIK-IN-5 exhibits excellent in vitro anti-colorectal cancer activity.

(E)-[6]-Dehydroparadol ((6)-Dehydroparadol), an oxidative metabolite of [6]-Shogaol, is a potent Nrf2 activator.

NSC 66811is a novel inhibitor of the murine double minute 2 (MDM2)-p53 interaction. It binds to MDM2 with a Ki of 120 nM and activates p53 in cancer cells with a mechanism of action consistent with targeting the MDM2-p53 interaction.

TC-A 2317 hydrochloride is an inhibitor of Aurora kinase A (Ki of 1.2 nM) and Aurora kinase B (Ki of 101 nM), exhibiting antitumor activity.