Chromatin/Epigenetics

Ilginatinib (NS-018) is a highly active and orally bioavailable inhibitor of JAK2.

AES-135 is a potent HDAC inhibitor, inhibits HDAC3, HDAC6, HDAC11 (IC50s: 654, 190, and 636 nM) with anti-tumor activity.

BMS-986158: BET inhibitor, IC50 of 6.6 nM in SCLC, 5 nM in TNBC cells.

FIDAS-5 is an orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. Cost-effective and quality-assured.

Tranylcypromine (2-PCPA) HCl, a MAO inhibitor, treats major, dysthymic, and atypical depression.

BRD-6929, a brain-targeted HDAC1/2 inhibitor (IC50 1/8 nM), enhances gnidimacrin's anti-HIV effect, useful in mood behavior studies.

LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM.

Fenbendazole (Fenbendazol) is an antinematodal benzimidazole used in veterinary medicine.

MK8722 is an effective and systemic activator of pan-AMPK.

Tinengotinib is a multikinase inhibitor that targets a series of kinases , including Aurora kinases A/B, JAK1/2, FGFR1/2/3, VEGFRs, and many other kinases.

ODM-207 (BET-IN-4) is a potent BRD4 inhibitor.

Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity.

Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable inhibitor of JAK2.

Nefiracetam (DM9384), in Phase 2 trials, enhances GABA, choline, monoamine systems, and treats Ro 5-4864 convulsions.

Indoprofen ((±)-Indoprofe) is a non-steroidal anti-inflammatory drug.

MAK683 is an inhibitor of embryonic ectoderm development (EED) (IC50s: 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay).

EHP-101 is a PPARγ/CB2 dual agonist with anti-inflammatory properties, inhibits fat formation, and combats diet-related obesity.

Uzansertib phosphate (INCB053914 phosphate) is an orally active, ATP-competitive inhibitor of pan-PIM kinase, inhibiting PIM1, PIM2 and PIM3.

JAK2 Inhibitor V (JAK2 Inhibitor V Z3) is a novel specific inhibitor of Jak2, inhibiting Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner.

MAT2A inhibitor 2 is an inhibitor of methionine adenosyltransferase 2A (MAT2A).

Amifostine (Ethyol) anhydrous is a cytoprotective agent, acts as a free radical scavenging activity.

Fluorescein NAD+ is a non-radioactive PARP assay substrate, enabling direct enzyme measurement by fluorescence. Comes as 81μg in 250μl water.

(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

SJ10542: potent JAK2/3-targeting PG-PROTAC; DC50s: JAK2 - 14 nM, JAK3 - 11 nM, JAK2-fusion ALL - 24 nM; CRBN recruiter.

AUR1545 is a selective KAT2A/KAT2B degradator, inhibitory against AML, SCLC, and NEPC, and suppressing tumour growth in the NCI-H1048 xenograft model.

CARM1/IKZF3 ligand 1 functions as an inhibitor of CARM1 and serves as a target protein ligand for the synthesis of PROTAC CARM1/IKZF3 degrader-1.

PROTAC BRD4 Degrader-5 is a PROTAC that degrades BRD4 in HER2 positive and negative breast cancer cell lines.

TCIP3 is a bivalent molecular glue (molecular glue) that can simultaneously bind to both p300/CBP and BCL6. It redirects p300 and CBP to activate programmed cell death genes, which are typically repressed by the oncogenic driver BCL6. TCIP3 is useful for studying diffuse large B-cell lymphoma (DLBCL) and is not toxic to untransformed tonsil lymphocytes or fibroblasts.

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.

Protein Kinase C (19-31), a PKC inhibitor derived from PKCa, has a serine at position 25 and tests PKC activity.

PROTAC HDAC6 degrader4 (Compound 17c) is a PROTAC that targets and degrades HDAC6, with a DC50 of 14 nM. It exhibits inhibitory activity against HDAC1, HDAC2, HDAC3, and HDAC6, with IC50 values of 2.2, 2.37, 0.61, and 0.295 μM, respectively. [Pink: ligand for target protein HDAC6 ligand-3; Black: linker; Blue: ligand for cereblon E3 ligase]

Compound 8b, a dual-ligand PROTAC, targets VHL & BRD4, degrades BRD4 in PC3 cells; conjugates with STEAP1/CLL1, DC50: 1.3/18 nM.

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.

CD532 hydrochloride, potent Aurora A inhibitor (IC50=45 nM), hampers MYCN protein, changes AURKA's shape, aids cancer research.

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%.

NP213 is a rapidly acting synthetic antimicrobial peptide (AMP).

HDAC6-IN-53 (Compound W28) is an inhibitor targeting histone deacetylase 6 (HDAC6) with an IC50 of 19.65 nM. It reduces the idiopathic pulmonary fibrosis (IPF) phenotype by inhibiting TGF-β1-induced collagen expression and demonstrates therapeutic efficacy in a bleomycin-induced mouse model of pulmonary fibrosis. HDAC6-IN-53 is applicable for research in idiopathic pulmonary fibrosis and related pulmonary fibrotic diseases.

SAMS peptide is a specific substrate for the AMP-activated protein kinase (AMPK).

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.

ZL0590 is an effective and selective inhibitor of BD1-BRD4 (IC50 = 90 nM) with anti-inflammatory activities.

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.

CBP/p300-IN-8 strongly inhibits CBP/P300 bromodomains; CBP IC50=0.01-0.1μM, BRD4 IC50=1-1000μM.

Hyp-dBET1 is a PROTAC degrader targeting BRD4, with an IC50 value of 3.4 μM in MDA-MB-231 cells. Under hypoxic conditions, Hyp-dBET1 becomes active, recruiting E3 ubiquitin ligase, and facilitates the degradation of BRD4 via the ubiquitin-proteasome system. Hyp-dBET1 is applicable in anti-cancer research.

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%.

Uzansertib (INCB053914) is a potent pan-PIM kinase inhibitor with low IC50s: 0.24, 30, 0.12 nM for PIM1, 2, 3; hinders hematologic tumor growth.

SMD-3040 TFA is a selective SMARCA2 degrader comprising SMARCA2/4 ligands, a linker, and VHL ligands, utilized in PROTAC drug synthesis.

PROTAC BRD4 Degrader-19 (compound 176) is a proteolysis-targeting chimera (PROTAC) designed to specifically degrade the BRD4 protein, offering potential utility

GSK040: Potent BET BD2 inhibitor, pIC50 8.3, 5000x selectivity over BD1, for oncology & immunology research.

GSK8573 is an inactive control compound for GSK2801. GSK8573 has binding activity to BRD9 (Kd of 1.04 μM).

Vanicoside A is a protein kinase C( PKC ) inhibitor from Polygonum pensylvanicum [1] .

MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology(Kd of 4 nM for Brd4BD2)

HIF-1 alpha (556-574) is a 19-mer fragment vital for gene expression in low oxygen; it binds VHL with critical proline 564 for stability.

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.

Namoline, a γ-pyrone, inhibits LSD1 with a 51 μM IC50, blocking cell growth and showing potential in prostate cancer studies.

BRD7-IN-1, a BI7273 derivative, transforms into PROTAC VZ185 (targets BRD7/9 with 4.5/1.8 nM DC50s) via a VHL linker.

KB02-JQ1: potent BRD4-degrading PROTAC, stable, specific; doesn't affect BRD2/3, modifies DCAF16 for action.

NSC 370284 inhibits STAT3/5, reducing AML cell viability with TET1 overexpression in vitro/in vivo.

MS9024 is a degrader of DNA methyltransferase 1 (DNMT1), facilitating its degradation in HCT116 cells via the ubiquitin-proteasome pathway, with a DC50 of 35 nM (DC50 values are 254 nM in MDA-MB-468 and 101 nM in H1299). Additionally, MS9024 inhibits DNMT1 with an IC50 of 0.43 μM.

CDD-1102 HCl is a novel BRDT-BD4 / BRD2-BD1302 selective inhibitor that shows non-hormonal contraceptive potential in ex vivo experiments.

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.

PRO-HD3 is a cell-specific, PROTAC-based degrader targeting HDAC6 [1].

Axl-IN-16, a dual Axl/HIF inhibitor, promotes Flammulina velutipes fruiting body formation and suppresses hypoxia-inducible factor activity along with receptor

XF067-68 is a PROTAC for targeted degradation of WD40 repeat domain protein 5 ( WDR5 )[1] .

JB300 is a PROTAC-based compound that serves as a highly selective degrader of Aurora A, with a DC50 of 30 nM. It is utilized in cancer research. JB300 comprises the PROTAC target protein ligand MK-5108 [pink part], E3 ligase ligand Thalidomide-O-COOH [blue part], and PROTAC Linker Boc-NH-PEG2-C2-NH2 [black part]. The conjugate of the E3 ubiquitin ligase ligand and linker is Thalidomide-O-COOH-NH2-C2-PEG2-NH-Boc.

SNIPER(BRD)-1 has LCL-161, (+)-JQ1 linked; degrades BRD4, cIAP1/2, XIAP; IC50s: 6.8, 17, 49nM.

PROTAC BET Degrader-3 is a potent degrader OF BET based on PROTAC.

PROTAC SMARCA2/4-degrader-28 (PROTAC 1) functions as a partial degrader of SMARCA2 and SMARCA4 through the PROTAC-based mechanism.

PF-04577806: potent & selective PKC inhibitor, ATP competitive, blocks PKCα/βI/βII/γ/θ (IC50: 2.4-45.9 nM), may reverse diabetic retinal leakage.

MNK/PIM-IN-1 is a novel dual inhibitor targeting both MNK and PIM pathways, characterized by its favorable pharmacokinetic profile.

HDAC11-IN-1 (Compound 14-NC6OH) is a macrocyclic inhibitor that selectively targets HDAC11 with a Ki of 40 nM. It demonstrates effective cell permeability and suppresses the expression of YAP1 and SOX2.

VinSpinIn is a probe for the Spin family proteins.

R 8605 is a third-generation retinoid.

GSK3735967: DNMT1 inhibitor, IC50 40 nM, dicyanopyridine core, binds hemimethylated CpG, interacts with H4K20me3.

ZMF-23, a PAK1/HDAC6 dual inhibitor, suppresses PAK1 and HDAC6-mediated aerobic glycolysis and cellular migration while inducing TNF-α-regulated necroptosis and

HDAC6ligand-3 serves as a ligand for HDAC6 and can be utilized as a target protein ligand in the synthesis of [PROTAC] HDAC6 degrader4.

HIV-1 protease-IN-10 (Compound 2), exhibiting HIV-1 latency reversing activity (IC50: 0.22 μM), selectively binds to the PKCδ C1b domain (IC50: 0.69 μM) and

Blocks HIF-1α/β dimerization, not HIF-2α; suppresses VEGF, CAIX in cancer cells; antiangiogenic in HUVECs (IC50 = 1.3 μM).

Sirtuin modulator 5 activates SIRT1 (<50 μM DC50), may extend cell lifespan, and could aid in researching various age/stress-related diseases.

SR-0813 is a potent and selective inhibitor of the YEATS domain in ENL/AF9.

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.

PROTAC BET Degrader-1 is a potent degrader of BET based on PROTAC.

GNE-987 is a potent chimeric BET degrader, binding BRD4 BD1/BD2 at IC50: 4.7/4.4 nM & has a DC50: 0.03 nM in EOL-1 AML cells.

PROTAC BRD4 Degrader-13 targets VHL and BRD4, degrading BRD4 with DC50 of 0.025/6.0 nM in PC3 cells when linked to STEAP1/CLL1 antibodies.

DS-103 is an HDAC inhibitor that targets HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 with IC50 values of 0.029, 0.123, 0.022, 0.367, and 9.26 μM, respectively. It also inhibits the malignant malaria parasite [Plasmodium falciparum 3D7] with an IC50 of 5.08 μM. In A2780 and Cal27 cells, DS-103 exhibits cytotoxicity with IC50 values of 1.48 μM and 1.47 μM, respectively, and reverses cisplatin resistance in these cells with IC50 values of 4.62 μM and 2.23 μM. DS-103 acts synergistically with cisplatin, enhancing apoptosis induced by cisplatin.