Chromatin/Epigenetics

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

cisVH 298 is a negative control for VH 298. Exhibits no detectable binding of VHL.

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

TP-472N serves as a negative control probe for TP-472, which is a specific and effective BRD7/9 probe.

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

HDAC6 degrader-3: potent, selective, degrades HDAC6 at 19.4 nM, weakens HDAC1 at 0.647 μM, induces α-tubulin hyperacetylation.

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.

dBRD9 is a PROTAC.

PROTACBRD4 Degrader-26 (PROTAC-2) is a photo-regulated PROTAC designed to degrade BRD4, achieving 80% degradation efficiency at a concentration of 1 μM. This compound can be inactivated by ultraviolet light.

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.

PROTAC BRD4 Degrader-15 targets von Hippel-Lindau and BRD4 with IC50s 7.2/8.1 nM and degrades BRD4 in cancer cells.

DNMT2-IN-2 is a selective inhibitor of DNA methyltransferase 2 (DNMT2) with a KD value of 3.04 μM. It targets a concealed allosteric binding site of DNMT2 and reduces m5C levels in tRNA of MOLM-13 cells. This compound works synergistically with Doxorubicin to impair cell viability and is applicable in cancer research, including studies of cervical cancer and leukemia.

N-Myristoyl-Lys-Arg-Thr-Leu-Arg: PKC inhibitor, IC50=75μM, blocks IL-2 in Jurkat cells.

XYD190 (Compound 14g) is an orally active degrader of CBP/p300. It inhibits the bromodomain of CBP/p300 with an IC50 of 483.7 nM and demonstrates antitumor activity against acute myeloid leukemia.

PRMT5-IN-9 is a novel PRMT5 inhibitor for treating cancer, with an IC 50 of 0.01 μM.

CP2 is a useful organic compound for research related to life sciences and the catalog number is T35338.

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

PRMT5-IN-36 (compound 4), an orally active PRMT5 inhibitor, is utilized in cancer research studies.

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

Cell-permeable peptide blocking Pim-1 kinase, halts DU145 cell growth, causes G1 arrest and apoptosis, inert to RPWE-1 cells at 10-20 μM.

Anemonin, a furanone dimer from Buttercups, may help manage melanocytes and osteoarthritis.

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

MS8511 HCl is a G9a/GLP inhibitor with anticancer activity that can be used in the study of a variety of cancers including brain cancer.

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

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

GSK232 is a highly selective and cellularly penetrant inhibitor of CECR2 with outstanding physicochemical properties.

PRMT5-IN-4 (compound AAA-1) is a PRMT5 inhibitor.

Kiss2 peptide acetate is the acetate form of Kiss2 peptide, serving as a positive regulator of reproduction. It binds to its homologous receptor Kiss2R (GPR54) in COS-7 cells, activating the PKA and PKC signaling pathways through Gas and Gaq proteins. This activation enhances the activity of both cAMP response element-dependent luciferase (CRE-luc) and serum response element-dependent luciferase (SRE-luc).

AS2553627 is a JAK inhibitor. AS2553627 prevents chronic rejection in rat cardiac allografts.

PROTAC BRD9 binder moiety 5 selectively binds BRD9 with IC50 4.20μM, used in PROTAC synthesis, shows cancer cell antiproliferative activity.

PARP1-IN-38 (compound ent-6_P) is a potent PARP1 inhibitor with an IC50 value of 10 μM. It exhibits selective cytotoxic activity in BRCA-mutant cancer cells.

Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is an orally active pan-PKC inhibitor that inhibits PKCα, PKCβI, PKCβII, and PKCγ.

BI01826025 (pArg-JQ1), a BRDT BD1 bromodomain PROTAC degrader, tests ClpC2's effect on ClpC1P1P2 protease.

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.

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

Strong PRMT5 inhibitor with 4 nM IC50, surpassing other PRMTs; halts MCL growth in lab tests.

Compound 38-S is an orally active CB1R/AMPK modulator with a K i of 0.81 nM and an IC50 of 3.9 nM for CB1R.

PROTAC TYK2 degrader-1 (CPD-155) functions as a selective degrader of TYK2, demonstrating a degradation maximum (D max) greater than 60%. This compound effectively targets TYK2 for degradation, utilizing a linker to connect the TYK2 ligand with the VHL ligand Thalidomide, each color-coded for identification.

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

Ep300/CREBBP-IN-2: Potent, oral Ep300 & CREBBP inhibitor; IC50s: 0.052μM & 0.148μM; cancer research.

CREBtide is a synthetic substrate for PKA (Km=3.9 µM), which is based on the phosphorylation sequence in d-CREB (cAMP response element binding protein).

WQQ-345, a BCAT1 inhibitor, exhibits an IC50 of 10.8 mM. In 67R cells, it reduces α-KG levels and upregulates H3K27me3 expression while downregulating the expression of glycolytic enzymes (PFKP and LDHA), leading to impaired glycolytic activity. Additionally, WQQ-345 demonstrates tumor-suppressive activity in a 67R subcutaneous xenograft model.

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.

Novel inhibitor for PKMζ, halts synaptic potentiation and reverses LTP with IC50 of 1-2.5 μM, erasing spatial memory.

CBB1007 trihydrochloride is a selective, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).

EZH2/EPP inhibitor, Kd 320 nM. Reduces EZH2, H3K27me3; halts MLL-AF9 leukemia growth; drives monocyte-macrophage differentiation.

PROTAC EED degrader-1 is a PROTAC targeting EED (pKD = 9.02), is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.17.

JAK2-IN-10 (compound 5) is a potent inhibitor of JAK2v617f, with an IC50 value of ≤10 nM.

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

JPS036, a benzamide-based VHL E3-ligase PROTAC, potently degrades HDAC1/2, increasing gene expression and apoptosis in HCT116 cells.

PAD2-IN-2 (cis-isomer of 1) TFA is an inhibitor of protein arginine deiminase 2 (PAD2). This molecule features an azobenzene photoswitch, enabling the optical regulation of PAD activity. Additionally, PAD2-IN-2 TFA inhibits the citrullination of histone H3.

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.

PROTACBRD4 degrader-30 is an ISOX-DUAL-based PROTAC degrader, targeting BRD4 with an IC50 value of 65 nM. It is used in research studies related to c-Myc oncoproteins and the pathophysiology of cancer cells.

EXQ-2d is an inhibitor of tankyrase, effectively targeting TNKS1 and TNKS2 with IC50 values of 48.8 nM and 13.8 nM (pIC50=7.31 and 7.86), respectively. Additionally, EXQ-2d suppresses the WNT/β-catenin signaling pathway with an IC50 of 515 nM. It demonstrates antiproliferative activity in cancer cells COLO 320DM and RKO, with GI50 values of 4.9 μM and 77 μM, respectively.

Protein Kinase C (alpha) Peptide (TFA) is a PKC-α-associated peptide functioning as a lipid-dependent serine/threonine protein kinase.

JQ1-TCO, a BET inhibitor derivative, enables click chemistry for molecular probing in vivo and in vitro.

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.

INCB059872: potent, oral, selective LSD1 inhibitor for myeloid leukemia research.

PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins (IC50 of 9.6 nM ).

PROTAC SMARCA2/4-degrader-34 (compound 38) serves as an effective degrader of both SMARCA2 and SMARCA4. It demonstrates binding affinity to PXR with a DC50 value of 85.1 nM and reduces the protein expression of 3xFLAG-PXR.

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

1,4-DPCA is an inhibitor of prolyl-hydroxylase with an IC50 of 2.4 µM for collagen hydroxylation in human foreskin fibroblasts and 60 μM for factor inhibiting

TM11, a tanshinone analog, serves as an effective inhibitor of HuR, preventing the formation of HuR-RNA complexes. It also reduces LPS-induced inflammatory responses in murine macrophages.

Adenosine receptor modulator 1 acts as an inducer of collagen VII (C7). It enhances the expression of COL7A1 mRNA in donor-derived keratinocytes and, in synergy with Gentamicin, increases the overall levels of C7.

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%.

PROTAC BRD4 Degrader-12 targets BRD4 in PC3 cells; conjugates with STEAP1, CLL1; DC50: 0.39/0.24 nM.

PF-3166 (compound PF-3166) is a cell-active inhibitor of PAD2.

mUNO is a tumor-homing peptide (mUNO, sequence: "CSPGAK") that specifically binds to murine CD206, targeting tumor-associated macrophages that express CD206/MRC1. Additionally, mUNO can interact with human recombinant CD206.

MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. This compound delivers Verteporfin to CD206+ tumor-associated macrophages (TAM), thereby inhibiting the YAP/TAZ signaling pathway. It facilitates YAP exclusion from the nucleus, induces TAM polarization toward an anti-tumor phenotype, enhances phagocytosis and antigen presentation, and promotes T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models.

UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids.

TYK2activator-1 (16b) is a TYK2 activator with an EC50 value of 1.78 μM. It inhibits JAK2 and JAK3 with IC50 values of 6.8 μM and 6.3 μM, respectively.

HDAC/CD13-IN-1 (Compound 12) is an inhibitor of both HDAC and CD13, with IC50 values of 0.34 μM for hCD13, 0.53 μM for porcine CD13, and 0.03, 0.06, and 0.02 μM

ZINC000014708529 is a potent SIRT7 inhibitor exhibiting high affinity for SIRT7 and is utilized in cancer research [1].

Tert-butyl compound inhibits human EGLN-1; confirmed by spectrometry after 20 mins.

Cath-L-dBET1 is a PROTAC degrader targeting BRD4. It has an IC50 value of 2.8 μM in MDA-MB-231 cells. Activated by cathepsin L (Cath-L), Cath-L-dBET1 recruits E3 ubiquitin ligase to degrade BRD4 via the ubiquitin-proteasome system. Hyp-dBET1 is applicable for antitumor research.

2-PADQZ hydrochloride shows antiviral activity and targets influenza A virus RNA promoter.

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.

BAY-6035 is an inhibitor of SET and MYND domain-containing protein 3 (SMYD3). BAY-6035 has more than 100-fold selectivity over other histone methyltransferases.

Mz325 serves as a dual inhibitor of both HDAC and Sirt2, exhibiting an IC50 of 9.7 µM against Sirt2, which are implicated in the pathogenesis of cancer and

E67-2: Low-toxic, KIAA1718 inhibitor with IC50 of 3.4μM, targets H3K9/H3K4 demethylases.

WDR5ligand 2 is a ligand for WDR5 and can be utilized in the synthesis of PROTAC WDR5degrader 1.

SJ-106C, a SIRT inhibitor, exhibits IC50 values of 0.59, 0.12, and 0.49 μM against SIRT1/2/3, respectively. This compound specifically targets mitochondria and inhibits the growth of DLBCL tumors.

HDAC-IN-64 (Compound 13), an HDAC inhibitor, demonstrates potent inhibition of HDAC4/5/6/7/9 with IC50 values of 24, 45, 85, 31, and 37 nM, respectively.

Martinostat is an HDAC inhibitor that can be radiolabeled for quantitative imaging of HDACs within the central nervous system and major peripheral organs.

HIF1-IN-3 (Benzenepropanamide, N-[(8-hydroxy-7-quinolinyl)(4-methoxyphenyl)methyl]-) is an effective inhibitor of HIF-1 (EC50 = 0.9 μM) and can be used in

SAHA inhibits class I/II HDAC; c-SAHA, a fluorescent derivative, excites at 325 nm and emits at 400 nm.

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%.

Biotin-JQ1 is a bromodomain BRD4 binder; inhibits MM1.S cell growth with EC50 of 0.4μM.

Dihydrochlamydocin, an inhibitor of histone deacetylases (HDAC), exhibits potent cytostatic activity against mastocytoma cells.

iRucaparib-AP6: a specific, non-trapping PARP1 degrader; inhibits the enzyme's activity and scaffolding.

RK 286D is an indolocarbazole antibiotic.

KAT6A/KAT7-IN-2 (Example 177) is an inhibitor targeting KAT6A and KAT7, with an IC50 of 1 nM or less for both enzymes. It inhibits acetylation of H3K14 and H3K23 and also suppresses tumor cell proliferation, demonstrating an IC50 of 100 nM or less for CAMA-1 cells. This compound is applicable in cancer research.

SAMβA TFA, a selective antagonist of Mfn1-βIIPKC association conjugated to the cell permeable peptide TAT47-57, is a rationally designed inhibitor that improves

MNN-02-155 is a bivalent molecular glue that can simultaneously interact with both p300/CBP and BCL6. It effectively induces the activation of BCL6-targeted reporter genes and promotes cell death. This compound is used in the research of diffuse large B-cell lymphoma (DLBCL).

SARS-CoV-2-IN-87 (compound 138968421) is an effective inhibitor of the SARS-CoV-2 methyltransferases (nsp14 and nsp16).