Chromatin/Epigenetics

Igermetostat, an EZH2 inhibitor, is utilized both in vivo and in vitro for cancer research [1].

G244-LM is a potent and specific inhibitor of tankyrase 1/2. G244-LM inhibits Wnt signaling.

Dihydro-5-azacytidine (DHAC) is a nucleoside analog that interrupts DNA methylation by integrating into DNA. It also exhibits notable antitumor properties.

PHD-IN-2 (Compound 91), a potent PHD antagonist with an IC50 of less than 5 nM, effectively stimulates erythropoietin synthesis in HEP3B cells with an EC50 of

Cycloastragenol, a saponin from Astragalus, could be a new depression treatment.

I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains.

JAK-IN-34 (compound 11n) is a potent inhibitor of Janus kinases (JAKs), demonstrating IC50 values of 0.40 nM for JAK1, 0.83 nM for JAK2, 2.10 nM for JAK3,

PARP10-IN-3: selective inhibitor for mono-ADP-ribotransferase PARP10 (IC50: 480nM), also affects PARP2 and PARP15 (IC50: 1.7μM).

Tilorone dihydrochloride is an orally active interferon inducer, and has antineoplastic and anti-inflammatory actions.

XMD8-92 is an effective and specific BMK1/ERK5 inhibitor (Kd: 80 nM).

SYP-5 is a novel inhibitor of HIF-1, suppresses tumor cells invasion and angiogenesis.

Anti-PARP1 Antibody (6I459) is an antibody targeting PARP1. Anti-PARP1 Antibody (6I459) can be used in ELISA, IHC.

SMD-3236 is a PRAOTAC degrader targeting SMARCA2, designed using SMARCA ligand and VHL-1 ligand, and exhibits prolonged anti-tumor activity in vivo. SMARCA2 acts as a synthetic lethal target in cancer cells lacking SMARCA4, with SMD-3236 showing 2000-fold selectivity for SMARCA2 over SMARCA4, having a DC50 of less than 1 nM and a Dmax of over 95%. In the human cancer xenograft models deficient in SMARCA4, notably the H838 model, SMD-3236 effectively induces loss of SMARCA2 in tumor tissue while sparing the SMARCA4 protein, thereby inhibiting tumor growth. The compound consists of a target protein ligand (red part) SMI-1074, a PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate, and an E3 ligase ligand (blue part) SMARCA2 ligand-14, forming the E3LigaseLigand-linker Conjugate 159.

PI3K/Akt/CREB activator 1 (AE-18) is an iNOS inhibitor that can be used to study vascular dementia and Parkinson's.

IMM-H007 is a novel lipid-lowering agent, increasing abca1 protein expression

(S,R)-CFT8634 is a selective and orally active BRD9 protein degrader with potential for researching BRD9-mediated disorders, such as abnormal cellular

Ethyl 2-amino-4-methyl-5-thiophene carboxylate is a SETD7 inhibitor (IC50=4.59μM) with anticancer properties.

JAK3/ BTk-in-2 is a potent JAK3/BTK inhibitor.

JQKD82 trihydrochloride, a cell-permeable and selective inhibitor of KDM5, enhances H3K4me3 levels and is utilized in multiple myeloma research.

GW779439X is an inhibitor of CDK.

SIRT5 inhibitor 9 (compound 14) is a moderately selective and substrate-competitive SIRT5 inhibitor with IC50=4.07 μM and has potential anticancer effects.

MAT2A Allosteric Inhibitor 2 is a potent, selective inhibitor exhibiting an IC50 of 5 nM and demonstrates nanomolar efficacy (IC50 = 5 μM) in proliferation

PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5/MEP50).

PHD2-IN-1, a potent and orally active HIF prolyl hydroxylase 2 (PHD2) inhibitor, exhibits an IC50 of 22.53 nM and is applicable in anemia research [1].

MRK-740 is a PRDM9 histone methyltransferase inhibitor that inhibits H3K4 methylation.

5-aminoisoquinolin-1(2H)-one is the inhibitor of calf thymus PARP1.

Compound C-31, a salidroside-based glycoside, activates HIF-1α and may aid in diabetic limb ischemia studies.

DNMT1/HDAC-IN-1 (compound (R)-23a), a potent dual inhibitor targeting both DNMT1 and HDAC, exhibits impressive inhibitory effects specifically on HDAC1 (HDAC1:IC50=0.05 μM), a major HDAC isoform that interacts with DNMT1 across multiple protein complexes involved in the transcriptional silencing of TSGs. This compound has been shown to remodel the tumor immune microenvironment and induce tumor regression, effectively reversing cancer-specific epigenetic abnormalities.

Bromodomain Inhibitor-12 Edisylate (example 303) serves as a bromodomain inhibitor applicable to autoimmune and inflammatory disease research [1].

AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.

WP1066 is a inhibitor of JAK2 (IC50: 2.30 μM) and STAT3 (IC50: 2.43 μM) in HEL cells; shows activity to JAK2, STAT3/5, and ERK1/2, not JAK1 and JAK3.

LSD1-IN-39 (Compound 14) is a reversible inhibitor of LSD1 with an IC50 of 0.18 μM, showing broad-spectrum antiproliferative activity against cancer cells, inhibiting HepG2 cell migration, and suppressing epithelial-mesenchymal transition. Additionally, LSD1-IN-39 exhibits antitumor activity in mouse models.

SC99 inhibits JAK2-STAT3, reducing STAT3 genes, platelet activity, and has anti-myeloma, anti-thrombotic effects.

JAK3 Covalent Inhibitor-1 is a compound characterized by its potent and selective inhibition of Janus kinase 3 (JAK3), possessing an IC50 of 11 nM and

PFI-1 (PF-6405761), a specific BET (bromodomain-containing protein) inhibitor for BRD4, is with the IC50 of 0.22 μM in a cell-free assay.

SGI-1027 (DNA Methyltransferase Inhibitor II) is an effective and selective inhibitor of DNA methyltransferase (DNMT).

AKBA (3-O-Acetyl-11-keto-beta-boswellic acid), a natural component from frankincense, is a novel activator of Nrf2.

SW155246 is a potent and selective inhibitor of DNMT1 (DNA methyltransferase 1; IC50 of 1.2 μM).

P300/CBP-IN-5 is a potent inhibitor of p300/CBP histone acetyltransferase (IC50 of 18.8 nM).

DualCathepsinL/JAK-IN-1 (Compound A8) serves as a dual inhibitor of Cathepsin L (CTSL) and JAK, exhibiting IC50 values of 0.68 μM for CTSL and 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for JAK1/2/3 and TYK2, respectively. This compound effectively prevents the activation of MAPK, NF-κB, and JAK/STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. DualCathepsinL/JAK-IN-1 is applicable in research on acute lung injury (ALI).

ZLD1039, an oral EZH2 inhibitor, shows strong PRC2 inhibition at low nanomolar IC50s, and halts breast cancer growth and spread.

BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.

Adaptaquin is an inhibitor of the hypoxia-inducing factor prolyl hydroxylase (HIF-PH) [1] [2].

PHD2-IN-4 (compound 1) is an inhibitor of PHD2, with an IC50 of 4 nM. It is utilized in research related to chronic kidney disease.

Picolinamide (Picolinoylamide) is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.

IV-275 is a dual inhibitor targeting the bromodomains of both BRG1 and BRM.

Antidiabetic agent 7 (Compound 5m) functions as a potent hyperglycemia inhibitor. It effectively stimulates GLUT4 translocation in skeletal muscle cells by activating the AMPK-dependent pathway. Additionally, this compound is capable of reducing blood glucose levels and exhibits favorable pharmacokinetic properties. Antidiabetic agent 7 is suitable for research related to antihyperglycemic treatments.

Ziftomenib (KO-539) is an inhibitor of menin-MLL interaction with antitumor activity and can be used to study leukemia.

TM6089 is an inhibitor of Prolyl Hydroxylase that stimulates HIF activity without iron chelation, induces angiogenesis, and protects organ against ischemia.

Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties.

BET bromodomain inhibitor is a potent BET inhibitor.

PARP1/2-IN-4 (compound 3) is an inhibitor of PARP1/2.

5-Fluoro-2'-deoxycytidine (2'-DEOXY-5-FLUOROCYTIDINE) is an inhibitor of DNA methyltransferase (DNMT) .

GDC-0339: oral Pim kinase inhibitor for multiple myeloma (Kis: Pim1 - 0.03 nM, Pim2 - 0.1 nM, Pim3 - 0.02 nM), well-tolerated.

Decernotinib (VRT-831509)(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.

PROTAC SMARCA2 degrader-28 (Compound 158) is a potent SMARCA2 PROTAC degrader that achieves degradation of SMARCA2 in HiBiT A549 cells, exhibiting a DC50 of 3 nM.

CTPB is a potent p300 histone acetyltransferase (HAT) activator that can be used in the preparation of hair growth promoters and/or hair loss treatments.

MRTX-1719 is a potent and selective inhibitor of the PRMT5/MTA complex with an IC50 value of <10 nM against PRMT5/MTAMTAPDELSDMA cell lines.Cost-effective and quality-assured.

FHD-286 is an inhibitor of BRM/BRG1 ATPase and can be used for studies on the treatment of BAF-related disorders such as acute myeloid leukemia.

dCBP-1 selectively degrades p300/CBP via CRBN, killing multiple myeloma cells.

AMI-408 is a PRMT1 inhibitor that effectively reduces the levels of H4R3me2as in MLL-GAS7 leukemia cells.

MS7972 is CREBBP inhibitor that blocks human p53 and CREB binding protein association. MS7972 can almost completely block this BRD interaction at 50 μM

Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor (IC50: 0.37 nM) and demonstrates ~3,700-fold greater selectivity than Aurora A.

AAPK-25, a dual Aurora/PLK inhibitor, disrupts mitosis, induces apoptosis, and has antitumor properties.

PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM).

KDM1A-IN-29 is a histone demethylase inhibitor.

Larsucosterol ammonium salt is a derivative of 25HC3S. It is a DNMT inhibitor, a LXR antagonist, an endogenous epigenetic modulator of lipid metabolism.

Hispidulin, a natural flavone with a broad spectrum of biological activities, is a Pim-1 inhibitor (IC50: 2.71 μM).

BI-9564, a specific cell-permeable BRD9 BD inhibitor. The Kd for BRD9 is 5.9 nM, and IC50 for BET family is > 100 μM.

PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor (IC50: 420 nM; Kd: 170 nM).

HDAC-IN-87 (Compound XII6) is a non-selective HDAC inhibitor with pIC50 values of 6.9 for HDAC4 and 5.8 for HDAC6. It exhibits fungicidal activity against P. sorghi and P. pachyrhizi. The acute oral LD50 in both male and female rats is greater than 500 mg/kg.

Pim1/AKK1-IN-1: LKB1/AAK1 inhibitor with Kd 35/53/75/380 nM for Pim1/AKK1/MST2/LKB1, also targets MPSK1, TNIK.

Milpecitinib (Compound 21a) is a potent and selective Janus tyrosine kinase (JAK) inhibitor with anti-inflammatory properties. It shows promise for research in cancer and inflammatory diseases.

BRD4-BD1-IN-2: Potent, selective BRD4-BD1 inhibitor, IC50=2.51µM; 20x less active on BD2; for cardiovascular/cancer research.