Staurosporine is a potent and non-selective inhibitor of protein kinases with IC50s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively.
Alisertib (MLN 8237) is a selective Aurora A inhibitor with an IC50 of 1.2 nM.
Igermetostat is EZH2 inhibitor, used in cancer research in vivo and in vitro[1].
Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, compound 6)[1].
Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC[1].
SIRT6-IN-2 (Compound 5) is a selective SIRT6 inhibitor (IC50: 34 μM). SIRT6-IN-2 increases acetylation of H3K9 and increases glucose uptake in cultured cells. SIRT6-IN-2 also reduces T cell proliferation. SIRT6-IN-2 has immunosuppressive and chemosensitizing effects[1].
CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1].
Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis[1].
Anemonin (Pulsatilla camphor), a selective iNOS inhibitor, is also a PKC-θ inhibitor. Anemonin can significantly inhibit the translation or protein stability of PKC-θ protein. Anemonin also ameliorates dextran sodium sulfate-induced acute ulcerative colitis (UC) in mice. Anemonin can be used in the research of inflammation-related diseases[1][2].
Valemetostat tosylate (DS-3201 tosylate) is a first-in-class EZH1/2 dual inhibitor, used in the research of relapsed/refractory peripheral T-cell lymphoma[1].
Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.IC50 value: 0.41/0.29/0.122/0.017 uM (BRD2/BRD4/BRD9/CECR2) [1]Target: BRD inhibitorIn cell-based assays, Bromosporine (1 μM) accelerates FRAP recovery of BRD4 and CREBBP, while shows no activities against TIF1α, BAZ2A, and SMARCA2 even at 10 μM. Bromosporine shows moderate cytotoxicity in HeLa cells at 18 μM. Bromosporine, as a chemical probe for bromodomain functional assays, will be very useful in elucidating further biological roles of reader domains.
A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM.
BamHI Methyltransferase is a DNA methyltransferase which modifies the underlined cytosine (GGATCC)[1].
Acetaminophen-13C2,15N is the 13C and 15N labeled Acetaminophen[1]. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM;is a widely used antipyretic and analgesic agent[2][3][4]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[5].
UNC0642 is a potent and selective G9a/GLP inhibitor, with an IC50 of less than 2.5 nM.
Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.
α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis[1].
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively[1].
PF-249 is a potent, selective AMPK β1-containing complexes activator; increases the phosphorylation of the AMPK substrate ACC at S79 with EC50 of 296 nM, potently inhibits de novo lipogenesis (IC50=15 nM) in primary rat hepatocytes.
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.
HL271, a chemical derivative of metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. HL271 attenuates aging-associated cognitive impairment[1][2].
(E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
ME0328 is a potent and selective ARTD3/PARP3 inhibitor with an IC50 of 0.89±0.28 μM.
CBB1007 is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).IC50 Value: 5.27 uMTarget: hLSD1CBB1007 efficiently can block LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ≤ 5 μM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC50 ≤ 5 μM), and causes activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC50 ≤ 3.74 μM). CBB1007 was Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC50 ≥ 100 μM).
Iniparib (BSI-201) is an irreversible inhibitor of PARP1, used in the research of triple negative breast cancer.
Go6976 is a Protein Kinase C (PKC) inhibitor, with an IC50 of 20 nM.
Sinefungin is a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication[1]. Sinefungin, a SET7/9 inhibitor, ameliorates renal fibrosis by inhibiting H3K4 methylation [2].
PLK1/BRD4-IN-1 (9b) is an orally active dual PLK1 and BRD4 inhibitor with IC50 values of 22 nM and 109 nM against PLK1 and BRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest and apoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity[1].
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects[1].
LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1[1].