Ac-Gly-BoroPro is a selective FAP inhibitor with a Ki of 23 nM.
MnTE-2-PyP (BMX-010) chloride is a ROS scavenger and potent radioprotector. MnTE-2-PyP also is a manganese porphyrin, protects normal prostate tissue from radiation damage. MnTE-2-PyP can be used for the research of diabetic prostate cancer[1].
MBM-55 (compound 42g) is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice[1].
Cisplatin is a antineoplastic chemotherapy drug which works by cross-linking with DNA and causing DNA damage in cancer cells.
CeMMEC2 is a novel potent BRD4 inhibitor with IC50 of 0.9 uM, binds to both bromodomains of BRD4, comparably to (S)-JQ1.
Antineoplaston A10, a naturally occurring substance in human body, is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer[1].
BAY 1892005 is a regulator of p53 protein and acts on p53 condensates without causing mutant p53 reactivation[1].
Inotuzumab (Humanized Anti-CD22 Recombinant Antibody) is a humanized IgG4, κ antibody that targets human CD22. Inotuzumab can be linked to a toxic agent ozogamicin as an antibody-drug conjugate (ADC). Inotuzumab can be used for the research of acute lymphoblastic leukemia and non-Hodgkin lymphoma[1].
BRM/BRG1 ATP Inhibitor-3 is a BRG1/BRM inhibitor. BRM/BRG1 ATP Inhibitor-3 inhibits BRM and BRG1 with IC50 values of 10.4 nM and 19.3 nM, respectively. BRM/BRG1 ATP Inhibitor-3 can be used for the research of cancers and BAF complex-related disorders[1].
Corticotropin-releasing factor (ovine) is a preferential CRF1 receptor agonist. Sequence: Ser-Gln-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Met-Thr-Lys-Ala-Asp-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg-Lys-Leu-Leu-Asp-Ile-Ala-NH2.
UCL-TRO-1938 is a potent allosteric activator of PI3Kα with an EC50 value of approximately 60 μM. UCL-TRO-1938 can induce cell proliferation and has cardioprotective and neural regeneration effects[1].
BPIQ-I (PD 159121) is a potent and ATP-competitive EGFR tyrosine kinase inhibitor.. BPIQ-I shows anti-proliferative actively[1][2].
Trk-IN-20 is a kind of 3-vinylindazole derivatives. Trk-IN-20 suppresses Trk kinases functions by phosphorylation inhibition of TrkA/B/C with IC50 values of 1.6 nM, 2.9 nM and 2.0 nM, respectively[1].
2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines[1].
WYC-209, a synthetic retinoid, inhibits proliferation of malignant murine melanoma tumor-repopulating cells (TRCs) with an IC50 of 0.19 μM, has long-term effects and little toxicity, and induces TRCs apoptosis primarily via the caspase 3 pathway. The primary cellular target of WYC-209 is retinoic acid receptor (RAR)[1].
PROTAC BET Degrader-1 is a potent BET degrader based on PROTAC, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
Bergamottin is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
Tilsotolimod is a synthetic Toll-like receptor 9 (TLR9) agonist that has demonstrated antitumor activity in preclinical models.
LIMK1 inhibitor BMS-4 is a LIM Kinase (LIMK) inhibitor targeting to LIMK1/2. LIMK1 inhibitor BMS-4 inhibits phosphorylation of cofilin, the LIMK substrate. However, LIMK1 inhibitor BMS-4 is noncytotoxic on A549 cells[1][2].
Tamrintamab pamozirine (DC-1728001; SC-003; SC-003 ADC) an Antibody-Drug Conjugate (ADC) targeting to dipeptidase 3 (DPEP3 or MBD3). DPEP3 is a glycosyl phosphatidylinositol anchored metallopeptidase that is overexpressed in ovarian tumors. Tamrintamab pamozirine can specifically bind DPEP3-expressing cells to produce cytotoxicity. Tamrintamab pamozirine can be used in ovarian cancer research.[1].
HG6-64-1 is a potent and selective B-Raf inhibitor extracted from patent WO 2011090738 A2, example 9 (XI-1); has a IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells.
Motolimod is a selective Toll-like receptor 8 (TLR8) agonist, with an EC50 of approximately 100 nM.
Dihydrocephalomannine (compound 1b), an analogue of Paclitaxel, shows reduced cytotoxicity and tubulin binding compared to Paclitaxel[1].
HBX 41108 is an uncompetitive inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 of 424 nM. HBX 41108 inhibits USP7-mediated p53 deubiquitination to stabilize p53 and inhibits cancer cell growth. HBX 41108 induces p53-dependent apoptosis in p53 wild type and null isogenic cancer cell lines[1][2].
PROTAC SHP2 degrader-1 is a potent and effective SHP2 degrader. PROTAC SHP2 degrader-1 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins and is also neddylation- and proteasome-dependent[1].
Culmerciclib is a cyclin dependent kinase (CDK) inhibitor, and has antineoplastic activity[1].
Triethylene glycol bis(p-toluenesulfonate) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states[1].
Navitoclax (ABT-263) is a potent and oral Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM.
PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDAC. PTACH exerts potent growth inhibition against various human cancer cells, with EC50 values ranging from 1 to 10 μM.IC50 value: 1-10 μM (EC50)Target: HDACin vitro: In cancer cell growth inhibition assay, PTACH shows strong activity. PTACH inhibits various cancer cells with EC50 of 2.3, 9.1, 3.0, 2.6, 1.1, 4.5, 2.4, 5.0, and 4.5 μM for MDA-MB-231 breast cancer, SNB-78 central nervous system, HCT116 colon cancer, NCI-H226 lung cancer, LOX-IMVI melanoma, SK-OV-3 ovarian cancer, RXF-631L renal cancer, St-4 stomach cancer, and DU-145 prostate cancer.