7-Ethylcamptothecin is one of camptothecin analogues. camptothecin (CPT), a cytotoxic alkaloid isolated from Camptotheca acuminate, is shown to have strong antitumor activity against L1210 leukemia and Walker 256 carcinosarcoma models[1].
N-Boc-diethanolamine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Romidepsin is a potent HDAC1 and HDAC2 inhibitor with IC50s of 36 and 47 nM, respectively.
8-Methylguanosine 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].
Boc-aminooxy-PEG4-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Nile Blue Methacrylamide is a Nile Blue-based nanosized pH densor that can be used for simultaneous far-red and near-infrared live bioimaging[1].
6-Chloro-2-iodo-9-(2’,3’,5’-tri-O-acetyl-β-D-ribofuranosyl)purine 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].
HF50731 (HF-50731) is a novel potent, selective CXCR4 antagonist with Ki of 19.8 nM in the CXCR4 competitive binding assay.HF50731 significantly inhibited SDF-1α-induced calcium mobilization (IC50=621 nM) and cell migration, and blocked HIV-1 infection via antagonizing CXCR4 coreceptor function (IC50=1.5 uM).The structure-activity relationship analysis demonstrated that HF50731 could primarily occupy the minor subpocket of CXCR4 and partially bind in the major subpocket by interacting with residues W94, D97, D171, and E288.
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent[1].
Benzyl-PEG3-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
c-Myc inhibitor 6 (compound A102) is a c-Myc inhibitor. c-Myc inhibitor 6 decreases cancer cell viability and degrades c-Myc protein. c-Myc inhibitor 6 can be used for the research of c-Myc imbalance, such as cancer, cardiovascular diseases, and viral infection[1].
Enocitabine, a nucleoside analog, is a potent DNA replication inhibitor and a DNA chain terminator. Enocitabine can be used as an effective chemotherapeutic agent for the treatment of acute myelogenous leukaemia and lymphocytic leukaemias[1].
Fulzerasib is a potent KRAS inhibitor[1].
PRMT5-IN-32 is an inhibitor of PRMT5. PRMT5-IN-32 inhibits HCT116 cell proliferation with an IC 50 of 0.13 μM[1].
Ftase inhibitor I (B581) is a potent, selective and peptidomimetic farnesyl transferase (FTase) inhibitor. Ftase inhibitor I shows selectivity for FTase over geranylgeranyl isoprenoid (Ras-GG) or the fatty acid myristate (Myr-Ras)[1].
LB-60-OF61 hydrochloride is a potent NAMPT (nicotinamide phosphoribosyltransferase) inhibitor. LB-60-OF61 hydrochloride is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines[1].
Adenine-13C is the 13C labeled Adenine[1]. Adenine (6-Aminopurine), a purine, is one of the four nucleobases in the nucleic acid of DNA. Adenine acts as a chemical component of DNA and RNA. Adenine also plays an important role in biochemistry involved in cellular respiration, the form of both ATP and the cofactors (NAD and FAD), and protein synthesis[2][3][4].
Phosphoramidite is a modified phosphoramidite monomer used for the oligonucleotide synthesis.
Val-Cit-PABC-Ahx-May TFA is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Pyridone 6 is a pan-JAK inhibitor, which potently inhibits the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, 5 nM for JAK3, and 15 nM for JAK1, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.
L-Methionine γ-lyase (Methionine lyase) is a multifunctional enzyme, which belongs to the γ-family of pyridoxal-5’-phosphate (PLP) dependent enzyme. L-Methionine γ-lyase can catylyse α, γ-elimunation of L-methionine and homocysteine. L-Methionine γ-lyase has anticancer and anti-infectious activity, and also can be used for homocysteinemia study[1][2][3].
Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
Ono 3403 is a synthetic serine protease inhibitor. Ono 3403 inhibits lipopolysaccharide-induced tumor necrosis factor-alpha and nitric oxide production. ONO-3403 also has an antitumor effect on malignant tumors.
OM-153 is a potent tankyrase inhibitor with IC50s of 13 and 2 nM for tankyrase 1 and tankyrase 2, respectively. OM-153 shows inhibition of WNT/β-catenin signaling and proliferation in COLO 320DM[1].
A2A receptor antagonist 1 is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.
SC79 is a selective and cell-permeable Akt activator which activates Akt phosphorylation and inhibits Akt membrane translocation.
Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.
CCT 137690 is an aurora kinase inhibitor with IC50s of 42, 198, and 227 nM for aurora A, B and C, respectively.
KS100 is a potent ALDH inhibitor with IC50s of 230, 1542, 193 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS100 shows antiproliferative and anticancer effects with low low toxic. KS100 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS10600 induces apoptosis and cell cycle arrest at the G2/M phase[1].