Cromatina/Epigenetica

HD-TAC7 is a PROTAC HDAC degrader; IC50s: HDAC1 (3.6μM), HDAC2 (4.2μM), HDAC3 (1.1μM); reduces NF-κB p65; researched for asthma, COPD.

Myristoylated pep2m peptide; inhibits GluA2-NSF interaction, reducing AMPA receptor function and surface expression.

Curcuphenol in concentrations in the range of 29-116 μg/ml inhibited cell proliferation and DNA replication and induced cell death in a dose-dependent manner.

Menin–KMT2A-IN-1 (Compound 20) is an inhibitor of menin–KMT2A, binding to menin with an IC50 of 8 nM, and disrupting the interaction between menin and lysine methyltransferase 2A (KMT2A). It inhibits hERG channels with an IC50 of 65 μM and suppresses MV4-11 cells with an IC50 of 74 nM. Furthermore, Menin–KMT2A-IN-1 exhibits favorable pharmacokinetic properties in CD-1 mice, with an oral bioavailability of 74%.

SW2_110A acetate is a selective, cell-permeable chromobox inhibitor of homologue CBX8 (Kd = 800 nM) bound to CBX8 N-terminal color gamut (ChD).

N-Desmethyltamoxifen, tamoxifen's main human metabolite, regulates AML cell ceramide metabolism and is a more potent PKC inhibitor than tamoxifen.

SGC3027 is an inhibitor of histone methyltransferase,also is a first potent, selective and cell active chemical probe for PRMT7.

JPS014: A potent benzamide-based VHL E3-ligase PROTAC that degrades HDAC1/2, altering gene expression and inducing apoptosis in HCT116 cells.

Neuropeptide DF2 is an FMRFamide-related neuropeptide from crayfish.

DAO-dBET1, a dual-action PROTAC incorporating the PROTAC degrader dBET1, effectively serves as a potent BRD4 degrader and exhibits a DC50 value of 277 nM in the presence of CoCl2. Additionally, DAO-dBET1 inhibits hypoxia and Cath-L activation with an IC50 value of 281 nM.

RBN012811 is a PROTAC specifically targeting PARP14.

(S,R,S)-AHPC-C2-amide targets Smad3 degradation and boosts HIF-α; it has anti-fibrotic and renal protective roles.

LSD1/HDAC6-IN-1 is an oral dual inhibitor of LSD1/HDAC6 with anti-tumor effects, useful for multiple myeloma research.

HDAC6-IN-61 (Compound 4e) is an HDAC6 inhibitor with an IC50 of 73 nM, demonstrating greater selectivity compared to other HDAC isomers. It also acts as an activator of GPR40. HDAC6-IN-61 can increase the acetylation of tubulin and phosphorylation levels of ERK. This compound is relevant for studying neuroinflammation, including Alzheimer's disease.

Deuruxolitinib functions as an inhibitor of JAK1/2.

<p>HSP70/SIRT2-IN-1 (Compound 2a) serves as a dual inhibitor targeting both SIRT2 and HSP70, exhibiting an IC50 of 17.3±2.0 μM against SIRT2.</p>

BRD4-binding moiety 1 links to cereblon, forming a PROTAC that degrades BRD4 efficiently.

TDI-012804 is a TNKS2 inhibitor that selectively inhibits endogenous TNKS2 protein within cells. It enhances the expression of AXIN1 protein in Tnks1 heterozygous (Tnks1HET) and knockout (Tnks1KO) cells. TDI-012804 suppresses the proliferation of ApcQ1405X/Tnks1KO organoids with an EC50 of 59.1 nM and exhibits selective toxicity towards Tnks1KO AKP-G12D and AKP-G13D organoids.

BRD4 degrader-6 is a dimeric BDR4PROTAC class degrader with a DC50 of less than 0.1 μM. It effectively induces the ubiquitination and degradation of BDR4, exhibiting anticancer properties.

Dihydrochlamydocinanalog-1 (compound 2) is a Chlamydocin analog that inhibits the deacetylation of histone H4 peptides, with an IC50 of 30 nM.

4-PivO-NMT chloride is an indole derivative-based regulator of the AMPK signaling pathway. It modulates neurogenesis or neurite outgrowth by influencing AMPK activity and holds potential for research in neurological disorders, pain, and inflammation.

CAM2602 is an inhibitor of Aurora A-TPX2 interaction, demonstrating a binding affinity of 19 nM with Aurora A. This compound has been shown to inhibit the growth of pancreatic cancer cells. In solid tumor xenograft models, CAM2602 increases the proportion of PH3-positive cells while decreasing the ratio of P-Thr288Aurora A-positive cells, ultimately inhibiting tumor growth.

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.

HDAC1-IN-9 (13c) is an HDAC1 inhibitor. It inhibits the HDAC1 enzyme with an IC50 value of 1.07 µM. This compound exhibits the strongest antiproliferative activity against HT-29 (human colon adenocarcinoma cells), with an IC50 of 1.78 μM. In HCT-116 (human colon cancer cells), HDAC1-IN-9 significantly induces apoptosis. Additionally, HDAC1-IN-9 possesses antiangiogenic properties, reducing the expression levels of VEGFR-2 and phosphorylated VEGFR-2 (pVEGFR-2) by approximately 80%.

PRMT3-IN-4 (intermediate 15) is an inhibitor of Protein arginine methyltransferase 3 (PRMT3) and serves as the active control for SGC707. It can be utilized in the synthesis of PROTACs targeting PRMT3 and is applicable in research related to leukemia.

DDO-2093 inhibits MLL1-WDR5 interaction (IC50: 8.6 nM, Kd: 11.6 nM), with strong antitumor properties and selectivity.

<p>Pim-1 kinase inhibitor 11 (10f) is an inhibitor of PIM-1 with an IC50 value of 0.18 μM. It exhibits anticancer activity by inducing apoptosis and causing cell cycle arrest.</p>

CBP/p300-IN-14, patent WO2021213521A1's compound 27, inhibits CBP/EP300 with 3.3 nM IC50.

PROTACSMARCA2/4 degrader-36 (Compound 29) is a potent dual degrader targeting SMARCA2 and SMARCA4, exhibiting DC50 values of 0.22 nM and 0.85 nM, respectively. Additionally, PROTACSMARCA2/4 degrader-36 demonstrates antiproliferative activity.

CEM114 is a potent chemical compound known as a chemical epigenetic modifier (CEM).

RX-37, a potent BET inhibitor (Ki: 3.2-24.7 nM for BRD2/3/4), selectively hinders growth in leukemia cells with MLL1 gene rearrangement.

HLDA-221 is a heterobifunctional small molecule known as a Regulated Induced Proximity Targeting Chimera (RIPTAC).

A compound inhibits EZH2, overexpressed in cancers, affecting Treg activity and innate immunity.

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

VPC-70063 (Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)-) is an inhibitor of c-Myc-MAX.

UNC10142 (Compound 44) is a small-molecule antagonist of CHD1, with a binding IC50 value of 1.7 μM. It induces a dose-dependent reduction in the viability of PTEN-deficient prostate cancer cells.

TB22 is a non-nucleoside inhibitor of DOT1LR231Q with anticancer activity. It inhibits the malignant phenotype of lung cancer cells harboring the R231Q mutation via the MAPK/ERK signaling pathway, making it useful for lung cancer research.

PROTAC BRD4 Degrader-8: BRD4 inhibitor with IC50s of 1.1/1.4 nM for BD1/BD2, degrades BRD4 in PC3 cells.

Eldocasiran, a micro-RNA-193a-3p analogue, exhibits anticancer properties. It is utilized in cancer research [1].

SYY-B085-1 is a histone acetyltransferase (HAT) inhibitor.

iHAC is an inhibitor-HSP90 anchoring chimera that covalently binds to the BRD4 ligand (+)-JQ-1, targeting HSP90 and thereby inhibiting cancer cell proliferation. This compound also triggers an anti-tumor immune response and is effective in suppressing the recurrence and metastasis of 4T1 breast cancer in mouse models.

PRO-HD2 is a selective, PROTAC-based degrader of HDAC6 [1].

<p>SIRT1 activated by CAY10591, mimics caloric restriction, extends lifespan, inhibits apoptosis, suppresses TNF-α, and promotes fat mobilization.</p>

GSK9311 hydrochloride is a less active GSK6853 analog, serving as a negative control, inhibiting BRPF1/2 (pIC50: 6.0/4.3).

(R)-SKBG-1 is an inhibitor of the RNA-binding protein NONO, effectively downregulating androgen receptor expression by targeting both AR-FL mRNA and AR-V7 mRNA

CPI-268456 is a compound which has bioactive.

MAK683 hydrochloride is an inhibitor of embryonic ectoderm development (EED), with IC50 values of 59, 26nM measured in EED Alphascreen, ELISA.Cost-effective and quality-assured.

HSP90/LSD1-IN-1 (compound 6) is a dual inhibitor of HSP90 and LSD1. This compound effectively inhibits the proliferation of prostate cancer cell lines PC-3 and DU145, with GI50 values of 0.24 μM and 0.30 μM, respectively.

RJW100 is a potent LRH-1 & SF-1 agonist with pEC50 of 6.6 & 7.5, also activates miR-200c promoter.

<p>PROTAC BRD4 Degrader-28 (Compound 4) is a PROTAC degrader specifically targeting BRD4, and it holds potential for cancer research.</p>