Androgen receptor antagonist 3 (Compound C18) is an androgen receptor (AR) antagonist with an IC50 of 2.4 μM. Androgen receptor antagonist 3 shows anticancer activities[1].
Citarinostat is a HDAC6 specific inhibitor, with IC50 of 4 nM and 76 nM for HDAC6 and HDAC3, respectively.IC50 value: 4 nM (HDAC6), 76 nM (HDAC3)Target: HDACThe detailed information please refer to WO2015061684A1 and 2015054197A1.
Mal-PEG2-Val-Cit-PABA is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
5-Benzylamino carbonyl-3’-O-acetyl-2’-O-methyl-5’-O-DMTr-uridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
sulfo-SPDB-DM4 is a drug-linker conjugate for ADC by using the maytansinebased payload (DM4) via the sulfo-SPDB linker.
Cevipabulin fumarate (TTI-237 fumarate) is a microtubule-active, oral active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line[1][2].
BI-4916 is a prodrug of BI-4924. BI-4924 is a NADH/NAD+-competitive PHGDH inhibitor[1].
Gamabufotalin (Gamabufagin), a major bufadienolide of Chansu, has been used for cancer therapy due to its desirable metabolic stability and less adverse effect.IC50 value:Target: in vitro: Gamabufotalin (CS-6) strongly suppressed COX-2 expression by inhibiting the phosphorylation of IKKβ via targeting the ATP-binding site, thereby abrogating NF-κB binding and p300 recruitment to COX-2 promoter. In addition, CS-6 induced apoptosis by activating the cytochrome c and caspase-dependent apoptotic pathway [1]. Gamabufotalin significantly potentiated human breast cancer cells with different status of ER-alpha to apoptosis induction of TRAIL, as evidenced by enhanced Annexin V/FITC positive cells (apoptotic cells), cytoplasmic histone-associated-DNA-fragments, membrane permeability transition (MPT), caspases activation and PARP cleavage [2].in vivo: CS-6 markedly down-regulated the protein levels of COX-2 and phosphorylated p65 NF-κB in tumor tissues of the xenograft mice, and inhibited tumor weight and size [1].
DMT-2'-F-dC(Bz)-CE-Phosphoramidite is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
ZEN-3411 is a BET inhibitor with IC50s of 0.05, 0.05 and 0.06 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3411 can be used to form PROTACs to induce degradation of BRD4[1].
AC-93253 is a selective, potent SIRT2 inhibitor. AC93253 can inhibit SIRT2 with an IC50 value of 6 μM. AC93253 can be used for the research of tumors[1].
Goralatide TFA is an inhibitor of cell cycle progression. Goralatide TFA enhances selectivity of hyperthermic purging of human progenitor cells. Goralatide TFA has the potential for the research of leukemia[1].
SPP-DM1 is a drug-linker conjugate for ADC with potent antitumor activity by using DM1 (a potent microtubule-disrupting agent), linked via the ADC linker SPP[1].
7-Epi-10-oxo-docetaxel (Docetaxel Impurity D) is a impurity of docetaxel detected by high performance liquid chromatography (HPLC).
PROTAC Linker 24 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 24 can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
eIF4A3-IN-10 (compound 58) is a silvestrol (HY-13251) analogue. eIF4A3-IN-10 interferes the assembling of eIF4F translation complex with EC50s of 35 and 100 nM for myc-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-10 can be used for the research of human cancer pathogenesis[1].
ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 μM in neuroblastoma and non-neuroblastoma cell lines, respectively.IC50 Value: 1.5 μM(neuroblastoma); 3.4 μM(non-neuroblastoma)Target: Microtubule/Tubulinin vitro: ABT-751 shows the selective cytotoxicity with IC50 of 0.6–2.6 μM in neuroblastoma and 0.7–4.6 μM in other solid tumor cell lines. Furthermore, ABT-751 also exhibits a selective effect on dynamic microtubules and spares stable microtubules, accounting for the persistence of acetylated and detyrosinated α-tubulin positive polymerized tubules at the IC90 concentration of ABT-751. in vivo: In Calu-6 xenograft model, ABT-751 as a single agent at 100 and 75 mg/kg/day shows significant antitumor activity, while in combination with cisplatin, ABT-751 shows a dose-dependent enhancement in growth delay. In the HT-29 colon xenograft model, ABT-751 also shows significant antitumor activity as a single agent and produced a dose-dependent enhancement in growth delay In combination with 5-FU. In dogs with lymphoma, ABT-751 exhibits the dose-limiting toxicities that included vomiting, diarrhea, anorexia, or some combination of these with a maximum tolerated dose (MTD) of 350 mg/m2 PO q24h. Furthermore, the mean AUC and Cmax for ABT-751 at the MTD of 350 mg/m2 is 5.55 μg-hour/mL and 0.9 μg/mL, respectively.
GW 610 (NSC 721648), an antitumor agent, shows potent and selective anticancer activity against lung, colon, and breast cancer cell lines[1][2][3].
DS12881479 is a potent and selective Mnk1 inhibitor with an IC50 value of 21 nM. DS12881479 can be used in cancer research[1].
13-Methyltetradecanoic acid (13-MTD), a saturated branched-chain fatty acid with potent anticancer effects. 13-Methyltetradecanoic acid induces apoptosis in many types of human cancer cells[1][2].
BAMB-4(ITPKA-IN-C14) is a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A((ITPKA) with IC50 of 37 uM in ADP-Glo Assay.IC50 value: 37 uMTarget: ITPKA inhibitorBAMB-4 exhibit the lowest inhibition frequency among the InsP3-Kinase inhibitors. only in one from 42 targets tested,BAMB-4 showed an inhibitory effect. Noteworthy, in kinasescreens no targets of BAMB-4 were detected, indicating that thecompound does not belong to the typical kinase inhibitors. Thus,the relative high speci?city and the high cellular uptake ofBAMB-4 now for the ?rst provide the possibility to effectively inhibit InsP3kinase in vivo. e InsP3Kinase activity is essentially involved in ITPKA promoted metastasis of lung cancer cells, BAMB-4 is a promising therapeutic approach in lung cancertherapy.
ACG416B (compound 18) is a potent inhibitor of ChoK (choline kinase) with an IC50 of 0.4 μM. ACG416B renders higher ChoK inhibitory and antiproliferative activities against the HT-29 human colon cancer cell[1].
Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitor with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. IC50 Value: 6 nM(cdc2/cyclin B); 6 nM(cdk2/cyclin A); 9 nM(cdk2/cyclin E); 6 nM(cdk5-p35)[1]Target: cdc2/cyclin B; cdk2/cyclin E; cdk5-p35in vitro: In vitro inhibitory activity against Cyclin-dependent kinase 1-cyclin B complex from starfish oocytes is 6 nM (IC50) [1]. In addition to CDK1, p42/p44 MAPK were found to be two major purvalanol-interacting proteins in five different mammalian cell lines (CCL39, PC12, HBL100, MCF-7 and Jurkat cells), suggesting the generality of the purvalanol/p42/p44 MAPK interaction. When cells were treated with purvalanol, p42/p44 MAPK and CDK1 activities were inhibited in a dose-dependent manner. Furthermore, purvalanol inhibited the nuclear accumulation of p42/p44 MAPK, an event dependent on the catalytic activity of these kinases [2].in vivo:
Lentinan is purified β-glucan from Shiitake mushrooms. Lentinan has been approved as a biological response modifier for gastric cancer in Japan[1].
ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC50=300 nM) and TRPC6 channel (IC50>10 μM).
Thalidomide-5-CH2-NH2 (hydrochloride) is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-CH2-NH2 (hydrochloride) can be connected to the ligand for protein by a linker to form PROTACs[1].
Transcrocetin (trans-Crocetin), extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.
3’-Deoxy-3’-flluoro-3-deazauridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Agerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAFV600E with a Kd of 14 nM.
UBA5-IN-1 (compound 8.5) is a selective UBA5 inhibitor with an IC50 value of 4.0 μM. UBA5-IN-1 inhibits cell proliferation of Sk-Luci6 cancer cells with high expression levels of UBA5[1].