GSK217 (GSK-217) is a potent, highly selective BET BD2 inhibitor with pIC50 of 7.5 (BRD4 BD2), 300-fold selectivity over BRD4 BD1.
Ophiopogonin D', isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D' shows cytotoxic activity against two human tumor cell lines MG-63 and SNU387 with IC50s of 3.09 μM and 3.63 μM, respectively[1]. Ophiopogonin D' activates SIRT1 in a dose-dependent manner[2].
E3 Ligase Ligand-Linker Conjugates 20 is a degron-linker (refer to Compound DL7-TL). The PROTAC linker is bound lo at least one targeting ligand.
O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo[1]. Midostaurin is a multi-targeted protein kinase inhibitor with IC50 ranging from 22-500 nM.
PROTAC BRD9 Degrader-6 is a potent degrader of BRD9 (IC50=0.13 nM), can be used for research of BAF complex-related disorders[1].
JPS035 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I histone deacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells[1].
BETd-246 is a second-generation BET bromodomain (BRD) inhibitor, exhibiting superior selectivity, potency and antitumor activity[1].
PRMT5-IN-C17 is a novel potent, selective, and cell active protein arginine methyltransferase 5 (PRMT5) inhibitor.
HuR inhibitor KH-3 is a small molecule, selective inhibitior of HuR function with Ki of 0.83 and 0.72 uM in FP and AlphaLISA assays, respectively.KH-3 potently inhibits breast cancer cell growth in vitro and in vivo.KH-3 inhibits breast cancer cell invasion in vitro as well as delays initiation of lung colonies and improves mouse survival in an experimental metastasis model in vivo.KH-3 suppresses breast cancer cell invasion by disrupting HuR-FOXQ1 mRNA interaction.Inhibition of HuR with KH-3 yielded a significant reduced in the progression of pathological cardiac hypertrophy in a transverse aortic constriction model.
JNJ-9350 is an inhibitor of spermine oxidase (SMOX) with an IC50 value of 0.01 μM. JNJ-9350 also inhibits polyamine oxidase (PAO) with an IC50 value of 0.79 μM. JNJ-9350 can be used for the research of cancer[1].
Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model[1].
GeA-69 is a selective, highly cell permeable allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2, with a Kd of 2.1 µM[1].
Decitabine (NSC 127716) is a DNA methyltransferase inhibitor commonly used to treat myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML).
PRMT5-IN-10 has promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex.
(2S,3R)-LP99 is a potent and selective BRD7 and BRD9 inhibitor with an KD of 99 nM for BRD9. (2S,3R)-LP99 inhibits the association of BRD7 and BRD9 to acetylated histones in vitro and in cells. (2S,3R)-LP99 demonstrates that BRD7/9 plays a role in regulating pro-inflammatory cytokine secretion[1].
HDAC-IN-28, a novel HDAC inhibitor, shows potent activities against tumor growth and metastasis
CARM1-IN-1 is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM). IC50 value: 8.6 uM [1]Target: CRAM1 inhibitorin vitro: CARM1-IN-1(Cmp 7g) displayed high and selective CARM1 inhibition, with lower or no activity against a panel of different PRMTs or HKMTs. In human LNCaP cells, 7g showed a significant dose-dependent reduction of the PSA promoter activity.
Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM.
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and Akt. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors[1].
CD161 is a potent and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 28.2 nM and a Ki of 8.2 nM for BRD4 BD1[1]. CD161 is a C-type lectin-like receptor expressed on the majority of natural killer (NK) cells. CD161 demonstrates high selectivity over 24 non-BET proteins containing bromodomains[2].
PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes[1].
KG-501 is a CREB inhibitor, with an IC50 of 6.89 μM.
CG347B is a selective HDAC6 inhibitor[1].
MOCPAC is an HDAC1 specific substrate[1].
PARP7-probe-1 is a chemiluminescent labeled PARP7 probe. PARP7-probe-1 is a biotinylated probe binding to the PARP7 active site. PARP7-probe-1 can be used for the research of PARP7 function[1].
EPZ015866 is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 22 nM.
MC2590 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2590 is a inhibitor of HDAC1-3, −6, −8, and −10 (class I/IIb-selective inhibitor) with ic50 of 0.098 μM, 0.156 μM, 0.039 μM, 0.015 μM, 0.047 μM, 0.071 μM, respectively. MC2590 also inhibits HDAC isoforms HDAC4 (IC50=2.73 μM), HDAC5 (IC50=1.35 μM), HDAC7 (IC50=2.06 μM), HDAC9 (IC50=2.79 μM), HDAC11 (IC50=3.98 μM). MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction[1].
Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin can cross the blood-brain barrier and triggers autophagy[1].
TP-472 is a novel BRD9/7 chemical probe that has excellent potency (BRD9 KD=33nM; BRD7 KD=340 nM by ITC), >30 fold selectivity over all other bromodomain family members except BRD7 and is cell active (EC50 320 nM in a BRD9 NanoBRET assay); has a good PK profile and is suitable for in vivo applications.
FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN[1].