Venuloside A is a potent inhibitor of LAT3. Venuloside A inhibits the leucine uptake in LNCaP prostate cancer cells with an IC50 of 8.12 μM[1].
Btk inhibitor 1R enantiomer Hcl is a pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.IC50 value:Target: BtkFrom PCT Int. Appl. (2012), WO 2012158843 A2 20121122.
MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM.
Propargyl-PEG4-Tos is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Propargyl-PEG4-Tos is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1][2].
2’-β-C-Ethynylcytidine 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].
2’,3’,5’-Tri-O-acetyl-5-cyanouridine 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].
BAY-784 is a gonadotropin releasing hormone receptor (GnRH-R) antagonist probe with IC50s of 21 and 24 nM for human and rat GnRH-R, respectively[1].
Resencatinib is a potent tyrosine kinase inhibitor with antineoplastic activity[1].
Ac-VAD-CHO (Ac-Val-Ala-Asp-CHO) is a pan-caspase inhibitor. Ac-VAD-CHO inhibits dissipation of MMP and cytochrome c release in hypoxia-exposed cells[1].
OB-24 is a potent inhibitor of heme oxygenase-1 (HO-1). Heme oxygenase-1, a member of the heat shock protein family, plays a key role as a sensor and regulator of oxidative stress. OB-24 significantly inhibited cell proliferation in vitro and tumor growth and lymph node/lung metastases in vivo. OB-24 has potential for the research of advanced prostate cancer (PCA)[1].
CooP is a linear glioblastoma-targeting nonapeptide. CooP binds to the mammary-derived growth inhibitor/fatty acid binding protein 3 (FABP3) in the glioblastoma cells and its associated vasculature. CooP is used for the targeted delivery of chemotherapy and different nanoparticles[1].
IDO-IN-11 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50s of 0.18 μM (Kinase) and 0.014 μM (Hela Cell), extracted from patent WO 2016041489 A1, compound 13.
(Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.
FGN849 is the catabolite of DGN549-L ADCs[1].
Chamaejasmenin B can be extracted from Stellera chamaejasme L. Chamaejasmenin B suppresses cancer cells migration and invasion. Chamaejasmenin B inhibits tumor metastasis. Chamaejasmenin B can be used in the research of cancers, such as breast cancers[1][2].
Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.
ER degrader 7 (Compound 35t) is an ERα and ERβ degrader. ER degrader 7 inhibits tubulin polymerization. ER degrader 7 inhibits cell viability with IC50s of 0.06, 2.56, 15.84, 1.59, 1.67, 1.37 μM for MCF-7, T47D, MCF-10A, LCC2, T47D D538G, and T47D Y537S cells respectively. ER degrader 7 also inhibits breast cancer tumor growth[1].
Limonene-13C,d2 is 13C and deuterated labeled Limonene (HY-N0544)[1]. Limonene is a monoterpene in citrus peel oil. A popular disinfectant and food preservative. Antimicrobial activities[2]. Anti-proliferative activities[3]. Antioxidant and anti-inflammatory effect[4].
Rituximab (anti-CD20) is an anti-CD20 chimeric monoclonal antibody used to treat certain autoimmune diseases and types of cancer[1].
Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities.
FK-3000 is a potent anti-tumor agent that inhibits the growth of carcinoma cells through apoptosis and induction cell cycle arrest. FK-3000 also exhibit antiviral effects against HSV-1 and HIV-1[1][2][3][4].
RG-12915 is a selective 5-HT3 antagonist, with IC50 value of 0.16 nM.
Mead acid (5,8,11-Eicosatrienoic acid), an unsaturated (Omega-9) fatty acid, is an indicator of essential fatty acid deficiency[1].
GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
Galangin is an agonist/antagonist of the arylhydrocarbon receptor, and also shows inhibition of CYP1A1 activity.
Antitumor Compound 2, a butenylphenyl phosphate derivative, is a drug for mammary cancer and anovulatory sterility.
HDAC-IN-45 (Compound 14) is a small molecule HDAC inhibitor and has anticancer activity, also can forms a hydrogenbond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively[1].
CD00509 is a Tdp1 inhibitor, with an IC50 value of 0.71 μM. CD00509 can sensitize breast cancer cells to Camptothecin (HY-16560). CD00509 has anti-tumor activity[1].
PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain, blocks the growth of mutant KRAS cells and tumors[1].
AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ.IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans.)Target: RARα agonistCompound 4(AGN-195183) inhibited the growth of breast cancer cell lines, and was inactive in an in vivo model of topical irritation.Compound 4 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3, compound 4 does not cause the topical irritation induced by the RARa-selective retinoid, Am-580. Compound 4 (AGN 195183) is currently in Phase I/IIA clinical trials in cancer patients.