NSD3-IN-3 is a potent NSD3 inhibtor with an IC50 value of 1.86 μM. NSD3-IN-3 has anticancer activity and significantly inhibits the growth and proliferation of non-small cell lung cancer cell line H460[1].
ZL0420 is a potent, highly selective BRD4 inhibitor with IC50 of 27 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively; displays selectivity over BRD2, BRD3, and BRDT (BRD2-BD1 and BRD2-BD2, IC50=803 and 1736 nM); disrupts the BRD4 complex with Pol II and histones, inhibits poly(I:C)-induced expression of innate immune genes IL6 and CIG5 in human small airway epithelial cells (hSAECs) (IC50=0.54 and 0.51 uM); blocks Poly(I:C)-induced inflammation and neutrophilia in vivo.
EPZ028862 is a selective SMYD3 inhibitor for cancer research[1].
PROTAC CBP/P300 Degrader-1 is a potent PROTAC CBP/P300 degrader. PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancer cell lines[1].
Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders.
Spisulosine-d3 is deuterium labeled Spisulosine. Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKC
MDL-801 is an activator of SIRT6 deacetylation, with an EC50 value of 5.7 µM[1].
BRD4 Inhibitor-19 is a BET inhibitor with an IC50 of 55 nM for BRD4-BD1. BRD4 Inhibitor-19 can be used for multiple myeloma research[1].
GSK-121 Trifluoroacetates a selective PAD4 inhibitor[1].
Derrone, a prenylated isoflavones, is an Aurora kinase inhibitor, with IC50 values of 6 and 22.3 μM against Aurora B and Aurora A, respectively. Derrone shows anti-tumor activity[1][2].
Benzyl selenocyanate is a chemopreventive agent for various chemically induced tumors in animal models at both the initiation and postinitiation stages. Benzyl selenocyanate is an inhibitor of DNA (cytosine-5)-methyltransferase (Mtase), with an with an IC50 of 8.4 µM[1].
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable prodrug of GSK-J1[1][2][3].
ABBV-712 is a selective inhibitor of Tyrosine kinase 2 (TYK2), with IC50 of 0.195 μM, that play important role in autoimmune diseases[1].
JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research[1].
GSK3326595 is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 6.2 nM.
NSC 698600 is a potent PCAF inhibitor, with IC50 of 6.51 µM (PCAF/H31-21). NSC 698600 exhibits good activity of inhibiting the proliferation of cancer cells[1].
UNC0224 is a potent and selective G9a inhibitor with IC50 of 15 nM in the G9a Thioglo assay.IC50 value: 15 nM [1]Target: G9aUNC0224 (Compound 8) also potently inhibited GLP with an IC50 of 20 nM and 58 nM in the Thioglo assay and and AlphaScreen, respectively. 8 was more than 1000-fold selective for G9a over SET7/9 (a H3K4 HMT) and SET8/PreSET7 (a H4K20 HMT) in Thioglo-based biochemical assays [1] [2].
DC-CPin711 is a potent and selective inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 0.0626 μM. DC-CPin711 arrests cell cycle at G1 phase and induces apoptosis[1].
666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM.
Ep300/CREBBP-IN-3 (Example 61) is a potent Ep300 and CREBBP inhibitor with IC50s of 0.056 and 0.095 μM, respectively. Ep300/CREBBP-IN-3 can be used for the research of cancer[1].
MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2.
Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.
(-)-JQ-1 is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (−)-JQ1 has no effect.
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect[1][2][3][4].
Bromodomain inhibitor-8 (Intermediate 21) is a BET bromodomain inhibitor for treating autoimmune and inflammatory diseases[1].
SNS-314 is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively[1].
Aurora kinase inhibitor-10 (Compound 6c) is an orally active Aurora B inhibitor with an IC50 of 8 nM. Aurora kinase inhibitor-10 shows antitumor activity[1].
CRT0066854 hydrochloride is a potent and selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively[1].
MAK683 hydrochloride is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay[1][2].
A BIX-01294 derivative that inhibit malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death; inhibits P. falciparum 3D7 parasites in culture with IC50 of 100 nM, >22-fold more potent than IC50 toward two human cell lines and one mouse cell line; significant reduces histone H3K4me3 levels in a concentration-dependent and exposure time-dependent manner in treatment of P. falciparum parasites.