PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε)[1][2].
PKCδ Peptide Substrate is an absolutely specific substrate for the δ-type of PKC, with a sequence corresponding to sequence 422-443 of murine eEF-1α and containing Thr-431[1].
BRD4-IN-3 (compound 141) is a potent BRD4 inhibitor with an IC50 of <0.5 µM. BRD4-IN-3 shows cytoxicity for MYC-Raji with an IC50 value of >1 µM[1].
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.
Amodiaquine dihydrochloride dihydrate is a histamine N-methyltransferase inhibitor, used as an antimalarial and anti-inflammatory agent.Target: histamine N-methyltransferaseAmodiaquine has been shown to be more effective than chloroquine in treating chloroquine-resistant Plasmodium falciparum malaria infections and may afford more protection than chloroquine when used as weekly prophylaxis. Amodiaquine is generally well tolerated.
Y08175 is a potent CBP bromodomain inhibitor. Y08175 exhibits considerable inhibitory effect with IC50s of 37 and 178.15 nM against CBP bromodomain in AlphaScreen assay and HTRF assay, respectively. Y08175 can be used for the research of prostate cancer[1].
JAK-STAT-IN-1 (compound 1) is a selective JAK-STAT inhibitor. JAK-STAT-IN-1 can be used for the research of autoimmune disorder[1].
B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines[1].
HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo[1].
EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.
Furamidine-d8 (DB75-d8) is the deuterium labeled Furamidine. Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent[1][2][3].
Zotiraciclib (TG02) is an orally active potent inhibitor of CDK2, JAK2 and FLT3 with IC50 values of 13, 73, and 56 nM, respectively. Zotiraciclib can be used for the research of advanced leukemias and multiple myeloma[1][2].
PAD2-IN-1, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. PAD2-IN-1 shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold)[1].
PROTAC PARP/EGFR ligand 1 is an active compound that can be used for the synthesis of dual PARP EGFR degraders by proteolytic targeting chimera (PROTAC) technology[1].
YW3-56 is a potent peptidylarginine deiminase (PAD) inhibitor, with an IC50 of 1-5 μM for PAD4.
UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively.
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties[1][2][3][4].
XP-524 (XL-223, XP524) is a potent, dual-BET/EP300 inhibitor, inhibits BRD4-BD (IC50=5.8 nM) and BRD4-BD2 (IC50=1.5 nM).XP-524 binds strongly to and inhibits EP300 and CBP proteins with IC50 of 28 and 116 nM, respectively.XP-524 (XL-223) showed high potency and selectivity (Kd < 1 nM) across BET family proteins. Selectivity for BRD proteins over all other bromodomain proteins was >400-fold.XP-524 significantly decreased expression of Myc pathway oncogenes such as c-MYC and n-MYC, increased expression of CDKN1B, a tumor suppressor that prevents the activation of the cyclin-D/CDK4 complex, and also reduced expression of cyclin-D (CCND1) itself.XP-524 showed increased potency and superior tumoricidal activity than the benchmark BET inhibitor JQ-1 in vitro, with comparable efficacy to higher-dose JQ-1 combined with the EP300/CBP inhibitor SGC-CBP30.XP-524 prevented KRAS-induced, neoplastic transformation in vivo and extended survival in two transgenic mouse models of aggressive PDAC.
DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors[1].
A-893 is a cell-active inhibitor of Methyltransferase SMYD2, with an IC50 of 2.8 nM.
PARP11 inhibitor ITK7 (ITK7) is a potent and selective PARP11 inhibitor. PARP11 inhibitor ITK7 can potently inhibit PARP11 with an IC50 value of 14 nM. PARP11 inhibitor ITK7 can be used for the research of cellular localization[1].
N-Myristoyl-Lys-Arg-Thr-Leu-Arg is a protein kinase C (PKC) inhibitor with an IC50 value of 75 μM. N-Myristoyl-Lys-Arg-Thr-Leu-Arg inhibits IL-2 receptor induction and IL-2 production in the human leukemic cell line Jurkat[1].
FT895 is a potent and selective HDAC11 inhibitor with an IC50 of 3 nM.
Nudifloramide-d3 (2PY-d3) is the deuterium labeled Nudifloramide. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro[1].
LW479, a novel HDAC inhibitor, could be a candidate drug for breast cancer prevention.
Butyzamide is an orally active activator of Mpl, a thrombopoietin (TPO) receptor. Butyzamide increases the phosphorylation level of JAK2, STAT3, STAT5 and MAPK. Butyzamide increases the level of human platelets in mouse xenotransplantation assay[1].
RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM.
HDAC1/MAO-B-IN-1 is a potent, selective and cross the blood-brain barrier HDAC1/MAO-B inhibitor with IC50 values of 21.4 nM and 99.0 nM for HDAC1 and MAO-B, respectively. HDAC1/MAO-B-IN-1 has the potential for the research of Alzheimer’s disease[1].
Resveratrol analog 1 is an analog of Resveratrol (HY-16561), compound 48. Resveratrol is a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties.