Flufenamic acid-d4 is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
Pacritinib is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).
SIRT1-IN-2 (compound 3h) is a potent and selective SIRT1 (silent information regulator 1) inhibitor, with an IC50 of 1.6 μM[1].
ZXH-3-26 is a selective BRD4 degrader with a DC50/5h (DC50/5h referring to half-maximal degradation after 5 hours of treatment) of ~ 5 nM[1].
PF-00956980 is a reversible pan-JAK inhibitor with IC50 values of 2.2, 23.1 and 59.9 μM for JAK1, JAK2 and JAK3, respectively. PF-00956980 can be used in the research of lung and skin inflammatory diseases[1].
MI-192 is a selective HDAC2 and HDAC3 inhibitor with IC50s of 30 nM and 16 nM, respectively. MI-192 is more selective for HDAC2/3 than other HDAC isomers.MI-192 induces myeloid leukaemic cells apoptosis. Anticaner and neuroprotective activities[1][2].
UNC1021 is a selective L3MBTL3 inhibitor with an IC50 of 0.048 μM[1].
HYDAMTIQ is a PARP-1/2 inhibitor (IC50: 29-38 nM) with anticancer, anti-inflammatory, and ischemic protective effects. HYDAMTIQ inhibits pulmonary PARP activity, is effective against allergen-induced cough and dyspnea, and inhibits bronchial hyperresponsiveness to methacholine. HYDAMTIQ has broad-spectrum tumor suppressor effects, including ovarian and breast cancers, prostate and pancreatic tumors, and glioblastoma multiforme. HYDAMTIQ has demonstrated in vivo efficacy in animal models of cerebral ischemia, asthma, cancer, and more[1].
CrBKA is a fluorogenic small-molecule substrate of SIRT6 with weak activity[1].
PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
GSK 525762A is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent[1].
Sirtuin modulator 4 (compound 12) is a sirtuin modulator. Sirtuin modulator 4 shows inhibitory effect to SIRT1 with an EC50 value of 51-100 μM. Sirtuin modulator 4 may be used for the research of increasing the lifespan of a cell, and preventing a wide variety of diseases and disorders including, for example, diabetes, obesity, neurodegenerative diseases, cardiovascular diseases, inflammation and cancer[1].
FTX-6058 hydrochloride is a potent and orally active inhibitor of Embryonic Ectoderm Development (EED). FTX-6058 hydrochloride can induce HbF protein expression in cell and murine models. FTX-6058 hydrochloride can be used for the research of select hemoglobinopathies, including sickle cell disease and β-thalassemia[1][2].
MS023 is a potent, selective inhibitor of protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively[1].
HDAC-IN-42 (compound 14f) is a potent and selective HDAC inhibitor with IC50 values of 0.19 and 4.98 µM for HDAC1 and HDAC6, respectively. HDAC-IN-42 shows anticancer and anti-proliferative activity. HDAC-IN-42 induces apoptosis and cell cycle arrest at G2/M phase[1].
RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 70 nM. RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC50 values of 0.51 μM and 2.785 μM respectively[1][2].
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression[1].
Tofacitinib-d3 (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
Dihydrochlamydocin is a Putative HDAC inhibitor.
Leucosceptoside A is a phenylethanoid glycoside with anti-hyperglycemic and anti-hypertensive activities. Leucosceptoside A shows inhibitory activity against α-glucosidase and PKCα (IC50 of 19.0 μM)[1][2][3].
5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd) is an orally active DNA methyltransferase I (DNMT1) inhibitor. 5-Aza-4'-thio-2'-deoxycytidine, a sulfur-containing deoxy-cytidine analog, has the potential for DNA hypomethylating and has antitumor effects[1].
Ac-Arg-Gly-Lys(Ac)-AMC is a substrate for HDAC[1].
UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH1/2 with IC50s of 10 nM and 45 nM, repectively.
Sirtinol is a sirtuin inhibitor, with IC50s of 48 μM, 57.7 μM and 131 μM for ySir2, hSIRT2 and hSIRT2, respectively.
4-Phenylbutyric acid-d5 is the deuterium labeled 4-Phenylbutyric acid[1]. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research[2][3][4].
Protein Kinase C (661-671) is a fragment peptide of β1 subspecies of protein kinase C (PKC). PKC plays a role in cellular growth control and tumor promotion[1][2].
Antitumor agent-69 (compound 12) is a potent inhibitor of protein-protein interaction between DOT1L and MLL-AF9/MLL-ENL, with Kis of 9 nM and 109 nM for AF9 and ENL, respectively. Antitumor agent-69 exhibits anticancer cellular activitiy[1].
Tubastatin A (TSA) TFA is a potent and selective?HDAC6?inhibitor with?IC50?of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A TFA also inhibits HDAC10 and metallo-β-lactamase domain-containing protein?2 (MBLAC2).
BET bromodomain inhibitor 2 is a potent BET bromodomain inhibitor with an IC50 of 14.1 µM[1].