E67-2 is a potent and selective inhibitor of H3K9 Jumonji demethylase KIAA1718 (KDM7A) with IC50 of 3.4 uM; selectively inhibits H3K9 Jumonji demethylase over H3K9 methyltransferase as well as H3K4 demethylase, has low cytotoxicity.
6-Deoxyisojacareubin is a PKC inhibitor that inhibits the proliferation of QGY-7703 cells in a concentration-dependent manner. 6-Deoxyisojacareubin is also a natural product that can be obtained from Garcinia nervosa. 6-Deoxyisojacareubin can be used in cancer research[1].
HDAC8-IN-3 (compound P19) is a potent HDAC8 inhibitor with IC50 value of 9.3 μM and produces thermal stabilization. HDAC8-IN-3 has cytotoxicity and induces apoptosis in leukemic cell lines[1].
Cercosporin is produced by a plant pathogen, Cercosporakikuchii, and the elsinochromes, pigments of the elsinoe family of fungi. Cercosporin is a potent photosensitizer with a short activation wavelength, mostly suitable for superficial photodynamic therapy (PDT) treatments, especially when it is necessary to avoid perforations[1].Cercosporin contains the perylenequinone structural features necessary to PKC activity with an IC50 of 0.6-1.3 μM[2].
PROTAC BET Degrader-10 is a potent BET protein BRD4 degrader extracted from patent WO2017007612A1, example 37, with a DC50 of 49 nM[1].
PF 477736 is a potent, selective ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, 100-fold selectivity versus Chk2 (Ki, 47 nM).
Povorcitinib is a potent and selective inhibitor of JAK1. Povorcitinib has the potential for the research of disease selected from cutaneous lupus erythematosus (CLE) and Lichen planus (LP) (extracted from patent WO2021076124A1)[1].
α-Hydroxyglutaric acid-13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium[1]. α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[2].
A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity[1].
LXS196 is a potent and orally active protein kinase C (PKC) inhibitor under Phase I clinical trials for the treatment of uveal melanoma.
SKF 91488 (Homodimaprit) dihydrochloride is a potent and noncompetitive histamine N-methyltransferase inhibitor with a Ki value of 0.9 microM. SKF 91488 dihydrochloride inhibits the methylation of labeled histamine in mice[1].
BET-IN-2 is a BET inhibitor with an IC50 of 52 nM for BRD4-BD1.
PRMT5-IN-18 (Compound 002) is a potent PRMT5 inhibitor that can be used for the research of a disease mediated by PRMT5， such as cancer[1].
Isojacareubin can be isolated from Hypericum japonicum. Isojacareubin covalently inhibits SARS-CoV-2 3CLpro. Isojacareubin also has anti-helicobacter activity. Isojacareubin inhibits PKC, and suppresses hepatocellular carcinoma metastasis and induces apoptosis[1][2][3].
PDE5/HDAC-IN-1 (Compound 26) is a potent phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50 values of 46.3 nM and 14.5 nM, respectively. PDE5/HDAC-IN-1 induces cell apoptosis and shows anticancer activities[1].
Aurora Kinases-IN-2 (compound 12Aj) is a potent Aurora kinases inhibitor with IC50 values of 90 and 152 nM for Aurora A and Aurora B. Aurora Kinases-IN-2 arrests cell cycle at G2/M phase by regulating cyclin B1 and cdc2. Aurora Kinases-IN-2 can be used for cancer research[1].
α-Hydroxyglutaric acid (2-Hydroxyglutarate) is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases[1].
AR-C66096 (FPL 66096) tetrasodium is a selective platelet P2YT receptor antagonist. AR-C66096 tetrasodium effectively blocks ADP-induced platelet aggregation. AR-C66096 tetrasodium can be used in the research of thromboembolism[1].
[Ala113]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM[1].
Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice[1].
R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol[1][2][3].
PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer[1][2].
CPI-1205, a highly potent and selective EZH2 inhibitor (biochemical IC50=2 nM, cellular EC50=32 nM).
Protosappanin A (PTA), an immunosuppressive ingredient and major biphenyl compound isolated from Caesalpinia sappan L, suppresses JAK2/STAT3-dependent inflammation pathway through down-regulating the phosphorylation of JAK2 and STAT3[1].
WM-1119 is a highly potent and selective KAT6A inhibitor, with an IC50 of 0.25 μM for KAT6A in lymphoma cells, the binding KD values of WM-1119 with KAT6A, KAT5 and KAT7 are 2 nM, 2.2 μM, 0.5 μM , respectively.
SCH-1473759 is an aurora inhibitor with IC50s of 4 and 13 nM for aurora A and B, respectively.
[Ala107]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM[1].
K-252b, an indolocarbazole isolated from the actinomycete Nocardiopsis, is a PKC inhibitor. K-252b can be used to inhibit extracellular kinases of cells in culture because it can’t pass through cell membrane freely [1][2][3].
HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells[1].
Picolinamide (2-Picolinamide) is an inhibitor of Poly(ADP-ribose) synthetase of nuclei from rat pancreatic islet cells[1][3].