Sirt2-IN-6 (compound 24a) potent and selective inhibitor of SIRT2, with an IC50 of 0.815 μM. Sirt2-IN-6 can be used for the research of cancer[1].
Ancitabine is an antileukemia drug[1].
Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR but not PI3K in vitro.
Tariquidar methanesulfonate, hydrate is a potent and specific inhibitor of P-glycoprotein (P-gp) with a Kd of 5.1 nM.
Thalidomide-5-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-COOH can be connected to the ligand for protein by a linker to form PROTACs[1].
Tos-PEG4-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
AcLys-PABC-VC-Aur0101 intermediate-1 is a cathepsin cleavable ADC linker that is used for making antibody-drug conjugate[1].
Furimazine is an imidazopyrazinone substrate. NanoLuc (Nluc) paired with Furimazine produced 2.5 million-fold brighter luminescence in mammalian cells relative to Oluc-19 with Coelenterazine.
Antitumor agent-53 is a potent antitumor agent. Antitumor agent-53 induces cell cycle arrest at the G2/M phase. Antitumor agent-53 inhibits the PI3K/AKT pathway to induce the apoptosis of HGC-27 cells. Antitumor agent-53 has the potential for the research of gastrointestinal tumors[1].
Me-Tet-PEG4-Maleimide is an ADC Linker containing 4 PEG units. Me-Tet-PEG4-Maleimide can utilize its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups. Its maleimide group (-Maleimide) degrades in aqueous media and has been used in drug delivery studies.
Violacein, a secondary metabolite produced by several microorganisms, possesses potent anticancer and low side effects. Violacein possesses antioxidant properties. Apoptosis inducer[1][2].
9-cis-Retinoic acid-d5 (ALRT1057-d5) is the deuterium labeled 9-cis-Retinoic acid. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities[1][2][3][4][5][6].
dBET23 is a BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=50 nM) in cellular degradation assays.
Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC)[1].
EPZ020411 hydrochloride is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8.IC50 value: 10 nMTarget: PRMT6in vitro: EPZ020411 inhibits methylation of PRMT6 substrates in cells. EPZ020411 does-dependently inhibits H3R2 methylation in PRMT6-overexpressing cells.in vivo: EPZ020411 shows good bioavailability following subcutaneous (SC) dosing in rats making it a suitable tool for in vivo studies.
AZ628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.
Tubulysin H is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis[1]. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[2]. Tubulysin H is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[3].
KRAS G12C inhibitor 39 is a potent inhibitor of KRAS G12C. KRas is a highly attractable target of the pharmaceutical industry for cancer research. KRAS G12C inhibitor 39 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2019099524A1, compound 494)[1].
IK-930 (compound I-32) 是一种有效的口服活性 TEAD 抑制剂，EC50 <0.1 µM。
DGKα-IN-2 (example 48) is a DGKα inhibitor with the IC50 of 0.9 nM, extracted from patent WO2021105115. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-2 has the potential for cancer and immunology study.
AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer[1].
3’-O-MOE-5Me-C(Bz)-2’-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].
Eldocasiran is a micro-ARN-193a-3p analogue, Eldocasiran has anticancer activity. Eldocasiran can be used for cancer research[1].
UT-155 is a selective androgen receptor (AR) antagonist, with a Ki of 267 nM for AR-RBD.
Glutaminase C-IN-1 (968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
BAY-299 is a very potent, dual inhibitor with IC50s of 67 nM for BRPF2 bromodomains (BD), 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2.
BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect[1].
Omesdafexor is a FXR agonist. Omesdafexor can be used in the research of liver disease or a metabolic inflammation-mediated disease[1][2].
N4-Benzoyl-2’-O-methylcytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP), including PP1 (IC50=15-50 nM), PP2A (IC50=0.1-0.3 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), with a significantly higher affinity for PP2A. Okadaic acid increase of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter[1] [2].