XPW1 is a potent and selective CDK9 inhibitor with excellent anti-ccRCC activity and low toxicity.

YPN-005 (YPN005) is a highly potent, selective inhibitor of cyclin-dependent kinase 7 (CDK7) with IC50 of 31 nM, with low inhibition for CDK2 and CDK5.

ZNL-05-044 is a potent, selective CDK11 inhibitor with Kd of 69 nM (CDK11A), shows significantly kinome-wide selectivity. ZNL-05-044 treatment leads to G2/M cell cycle arrest, impacts CDK11-dependent mRNA splicing in cells.

ZSQ836 (ZSQ 836) is a potent, selective and orally bioavailable CDK12/CDK13 covalent inhibitor with IC50 of 32 nM (CDK12), covalently interacts with Cys1039 of CDK12.

OBI-3424 S-isomer (TH-3424, OBI 3424) is a highly potent DNA alkylating prodrug that is converted by AKR1C3 to a potent DNA-alkylating agent.

CDEAH is a monofunctional alkylating agent that selectively kills PARP1- and xeroderma pigmentosum A-deficient cells.

NSC373981 (NSC 373981) is a CARD11 G-quadruplex (G4) stabilizing small molecule that downregulates CARD11 gene expression in DLBCL cells.

QBS10072S is a novel dual-function, BBB permeable chemotherapeutic agent with alkylating moiety and a selective large neutral amino acid transporter 1 (LAT1, SLC7A5) substrate, shows excellent BBB penetration and promising efficacy in vitro (U251 cell IC5

H3B-960 is a potent, selective and covalent inhibitor of Werner syndrome protein (WRN) helicase activity with IC50 of 60 nM.

H3B-968 is a potent, selective and covalent inhibitor of Werner syndrome protein (WRN) helicase activity with IC50 of 41 and 13 nM in ADP-Glo assay DNA unwinding assay, respectively.

HRO761 is a potent, selective, allosteric WRN inhibitor with IC50 of 100 nM (ATPase assay) and GI50 of 40 nM (SW48 cells), respectively. HRO761 binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation.

KY386 is a potent, selective inhibitor of RNA helicase DHX33 with IC50 of 19 nM.

SU0448 is a specific, cell-permeable small molecule activator of the DNA repair enzyme Human MutT Homolog 1 (MTH1) with AC50 value of 5.5 uM, inhibits cell viability of HCC1806 cells with IC50 of 36.1 uM.

Fraisinib is a specific and effective inhibitor of glycyl-tRNA synthetase 1 (GARS1), suppresses the synthesis of Ap4A by GARS1 and displays strong anti-tumoral potential.

RBI2 (Ribosome biogenesis inhibitor 2) is a small molecule inhibitor of ribosome biogenesis inhibitor, potently inhibits pre-rRNA levels in A375 with IC50 of 169 nM.

Ku-DBi 245 is a novel DNA-PK inhibitor with a unique mechanism of action, blocking the Ku 70/80 heterodimer interaction with DNA.

SN38023 is a bioreductive prodrug of DNA-dependent protein kinase inhibitor IC87361 (Cat# PC-62995), SN38023 is metabolised to a potent DNA-PKi (IC87361) selectively in radioresistant hypoxic cells.

ZL-2201 mesylate (ZL2201) is a highly potent, selective and orally bioavailable inhibitor of DNA-dependent protein kinase (DNA-PK) with IC50 of 1.1 nM.

CCT241950 (CCT 241950) is a small molecule NEK2 inhibitor, induces Tyr70Nek2 to jut into the ADP-binding pocket.

T-1101 tosylate (TAI-95 tosylate) is a potent, orally abioavailable Hec1 inhibitor that disrupts Hec1-Nek2 protein interaction wide anti-cancer spectrum (GI50=14.29-73.65 nM, breast cancer cell lines).

SYL1073 is a potent, selective and covalent Threonine tyrosine kinase (TTK) inhibitor with IC50 of of 16 nM.

DI-87 ((R)-DI-87) is a highly potent, specific, orally bioavailable deoxycytidine kinase (dCK) inhibitor with IC50 of 3.15 nM.

F-aza-T-dCyd (NSC801845) is a novel cytidine analog and is more efficacious than aza-T-dCyd in cell culture and mouse xenograft studies in HCT-116 human colon carcinoma.

JLT048 is a small molecule inhibitor of tyrosyl-DNA-phosphodiesterases 1 and 2 (TDP1 and TDP2) with IC50 of 7.7 and 32 uM, respectively.

PSB-071 (PSB071) is a small molecule inhibitor of nucleoside triphosphate diphosphohydrolases (NTPDase).

PSB-0952 (PSB0952) is a potent, selective ecto-5'-Nucleotidase (eN, CD73) inhibitor with Ki of 260 nM, >150-fold selectivity over NTPDases and P2Y receptor subtypes P2Y2, P2Y4, P2Y6, and P2Y12.

PSB-0963 (PSB0963) is a potent, selective ecto-5'-Nucleotidase (eN, CD73) inhibitor with Ki of 150 nM, >100-fold selectivity over NTPDases.

TH6342 (TH-6342) is a specific small-molecule inhibitor against the dNTP triphosphohydrolase (dNTPase) SAMHD1, inhibits the enzymatic activities of SAMHD1 against dGTP, Cl-F-ara-ATP, and ara-CTP with IC50 of 9.6, 11.0 and 5.8 uM, respectively.

TH7528 (TH-7528) is a specific small-molecule inhibitor against the dNTP triphosphohydrolase (dNTPase) SAMHD1, inhibits the enzymatic activities of SAMHD1 against dGTP, Cl-F-ara-ATP, and ara-CTP with IC50 of 4.5, 2.8 and 2.6 uM, respectively.

AMXI-5001 (AMXI 5001) is a novel, highly potent, orally active dual PARP1/2 (IC50 5/0.05 nM) and microtubule polymerization inhibitor, inhibits intracellular PAR formation with IC50 of 7 nM.

G-631 is a potent and selective TNKS1/2 inhibitor with IC50 of 7 nM in biochemical assays of tankyrase auto-PARsylation activity, and cellular potency of 8 nM (HEK293).

KMR-206 (KMR206) is a potent, selective PARP7 inhibitor with IC50 of 13.7 nM, displays 75-fold selectivity for PARP7 over PARP2 and does not inhibit PARP1 up to 3 uM.

kt-3283 is a novel bi-functional PARP-HDAC inhibitor with IC50 of 0.338 nM, 2.19 nM and 1.89 uM for PARP1, PARP2 and HDACs, respectively.

Mortaparib is a dual inhibitor of mortalin-PARP1 interaction, and a p53 activating cytotoxic compound, induces activation of growth arrest and apoptosis signaling in cancer cells in vitro and in vivo.

Morataprib Plus is a novel anticancer small molecule that disrupts mortalin-p53 interaction, prevents the interaction of mortalin with p53 resulting in the activation of growth arrest and apoptosis mediated by activation of p21WAF1 or BAX and PUMA signall

HC-5404 (LY-4) is a potent, selective and orally active inhibitor of PKR-like endoplasmic reticulum kinase (PERK, EIF2AK3) with IC50 of 1 nM.

Allopole is the first allosteric, specfic and cell-permeable inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1), Allopole is the prodrug of Allopole-A.

Allopole-A is the first allosteric, specfic inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1) with IC50 of 2.5 nM in FP-based assays, Allopole-A is the active form of Allopole.

PLK1 inhibitor SBE13 is a potent, selective PLK1 inhibitor with IC50 of 0.2 nM, with little to no inhibition against PLK2/PLK3 (IC50, 65 uM/875 nM).

(R)-BA-1049 is a potent, orally-available ROCK2-selective inhibitor with IC50 of 0.24 uM, 16-fold selectivity over ROCK-1.

(S)-BA-1049 is a potent, orally-available ROCK2-selective inhibitor with IC50 of 0.24 uM, 16-fold selectivity over ROCK-1.

C3TD879 is a potent, selective first-in-class Citron kinase (CITK) chemical inhibitor with biochemical IC50 of 12 nM.

ITRI-E-(S)4046 (E(S)4046) is a potent, highly specific, dual synergistic inhibitor of myosin light chain kinase 4 (MYLK4) and Rho-related protein kinase (ROCK) with IC50 of 3.2 nM and 25.6 nM for ROCK1 and MYLK4, respectively.

Netarsudil (AR-13324) is a potent, selective ROCK inhibitor with Ki of 4.2 nM for ROCK2.

DIZ-3 is a dimeric aryl-substituted imidazole as a selective multimeric G-quadruplex (G4) ligand, intercalates into the G4-G4 interface, induces cell cycle arrest and apoptosis, and inhibits cell proliferation in alternative lengthening of telomere (ALT)

Teloxantron (Telomerase inhibitor TXT4) is a potent small molecule inhibitor of telomerase activity with IC50 of 9.61 uM, 7-fold lower than BIBR1532 (Cat# PC-45170), inhibits the processivity of telomerase with preferential DNA damage on telomeres.

LMP744 (MJ-III-65, NSC706744) is a small molecule TOP1 inhibitor antitumoral activity.

SD133 (Sd-133) is a drug-like small molecule inhibitor of adhesion molecule cadherin 11 (CDH11), binds specifically to the CDH11 binding pocket with KD of 25.2 uM in SPR assays.

GB1490 is a potent, selective and orally available galectin-1 (gal-1) inhibitor with Kd value of 0.4 uM and 0.23 uM for human and mouse galectin-1, respectively.

6-B345TTQ is a small molecule inhibitor of the α4 integrin-paxillin interaction, impairs the interaction of native paxillin with α4 integrin, decreases α4-mediated cell migration.

Alintegimod (7HP349) is a small molecule activator of the integrins αLβ2 (LFA-1) and α4β1 (VLA-4). 7HP349 directly activates integrin cell adhesion receptors crucial for the generation of an immune response.

A7B7C7 (11-A7B7C7) is a potent Paxillin-α4 integrin binding antagonist with IC50 of 300 nM in vitro, decreases α4β1-mediated T cell migration.

AXT107 (AXT-107) mimetic peptide derived from collagen IV, binds integrins αvβ3 and α5β1 (Kd=1.29 and 2.21 nM), disrupts VEGFR2-β3 complex formation.

GSK3335103 is a highly potent and orally bioavailable nonpeptidic αvβ6 integrin inhibitor with pIC50 of 8.0. GSK3335103 shows high desirable oral pharmacokinetic profiles in rat, dog, and minipig, with low to moderate clearance, moderate volumes of distributio, high to complete oral bioavailabilities and high solubility in all physiological media.

GW559090 is a potent, selective, competitive and high-affinity α4β1 integrin (VLA-4) antagonist with Kd of 0.19/1.04 nM for huamn/rat α4β1, respectively.

IVL745 (IVL-745) is a small molecule very late antigen (VLA-4) antagonist with IC50 of 20 nM and 2 nM for adhesion to VCAM-1 and fibronectin, respectively.

MSR03 is a potent, pure small molecule αVβ3 antagonist with IC50 of 1.5 uM for inhibition of adhesion of cells expressing human αVβ3 to immobilized fibrinogen.

TBC 4746 (AVA4746) is a small molecule mimetic of VCAM-1 that binds VLA-4 on B-ALL cells with high affinity and efficiently blocks ligand-binding with VCAM-1 with EC50 of 38.52 nM.

AM-1882 (AM1882) is a potent, selective mitotic kinesin KIF18A inhibitor with IC50 of 230 nM in kinesin-8 microtubule (MT)-ATPase motor assays.

AM-9022 (AM9022) is a potent, selective and orally active mitotic kinesin KIF18A inhibitor with IC50 of 47 nM in kinesin-8 microtubule (MT)-ATPase motor assays.

ALM201 is a small 23 amino acid peptide derived from the FK506 binding protein FKBPL, a targeted microtubule binding agent which exhibits potent anti-angiogenic activity in vitro and in vivo.

CH-2-77 is a potent colchicine-binding site inhibitor (CBSI) targeting tubulin, shows potent anti-proliferative activity against a panel of cancer cells in vitro and efficacious anti-tumor effects in vivo.

CH-2-77 analogue 60c is a potent colchicine-binding site tubulin inhibitor, inhibits tubulin polymerization and is effective against P-glycoprotein-mediated multiple drug resistance and taxol resistance.

EAPB02303 (EAPB 02303) is a novel microtubule-disrupting agent with in-vivo activity in PDAC and in-vitro synergy with Paclitaxel, inhibits A375 melanoma cell line with IC50 of 3 nM.

FiVe1 is a vimentin binding small molecule that promotes vimentin disorganization and phosphorylation during metaphase, causes mitotic catastrophe, multinucleation, and the loss of stemness in cancer cells.

KGP591 is a small molecule inhibitor of tubulin polymerization with IC50 of 0.57 uM, exhibits cytotoxicity against the MCF-7 and MDA-MB-231 human breast cancer cell lines with GI50 of 320 and 102 nM, respectively.

KGP618 is the phosphate prodrug salt of KGP591, which is a small molecule inhibitor of tubulin polymerization with IC50 of 0.57 uM.

An orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo.

R-huezole is a phase-separating small molecule that forms liquid droplets to selectively sequester tubulin, enters cultured human cells and prevents cell mitosis by forming tubulin-concentrating condensates in cells.

TN-2 is a potent, dual tubulin/NRP1-targeting inhibitor with IC50 of 0.71 uM (tubulin polymerization) and 0.85 uM (NRP-1), inhibits proliferation and angiogenesis of tumor cells.

BBC1115 is a novel chemotype inhibitor of bromodomain and extra-terminal motif (BET) proteins, displays broad binding across BDs of BET proteins.

BI 1702135 (Compound 4) is a potent SMARCA2 binder for targeted protein degradation (PROTAC) design as BI 1810284 (ACBI2, Cat. PC-20464).

BI-4827 (BI 4827) is the negative control compound of BI-7190, which is a potent, selective chemical probe targeting the bromodomain of BPTF.

BI-7190 (BI 7190) is a potent, selective chemical probe targeting the bromodomain of BPTF with binding Kd of 3.5 nM.

CDD-787 is a highly potent, selective BET bromodomain 1 (BET BD1) inhibitor with IC50 of 2.1 and 3.3 nM for BRDT-BD1 and BRD4-BD1, respectively, with high selectivity (>3,000-fold) over BET BD2 proteins.

CDD-956 is a highly potent, selective BET bromodomain 1 (BET BD1) inhibitor with IC50 of 2.1 and 4.4 nM for BRDT-BD1 and BRD4-BD1 respectively, with high selectivity (>500-fold) over BET BD2 proteins.

CG13250 (CG 13250, CG250) is a potent, selective and orally bioavailable BET bromodomain inhibitor with Kd of 44 nM (BRD4), IC50 of 1.1 uM (BRD4 BD1+BD2).

CG223 (CG14223) is a potent and specific inhibitor of BET proteins with Kd of 45 nM for the C-terminal bromodomain of BRD3 (i.e. BRD3(2)) to 370 nM for the N-terminal bromodomain of BRDT (i.e. BRDT(1)).

CN210 is a quinazoline-based BET family inhibitor with Kd value of 70 nM for BRD4 (BD1,2) and IC50 of 0.94 uM in MV4-11 viability assay.

DDO-8926 is a potent selective inhibitor of bromodomain and extra-terminal (BET) proteins with Ki values of 15 nM (BRD4 BD1) and 9.5 nM (BRD4 BD2).

Dual PI3K/BET 18DS is a potent, chimeric dual PI3K/BET bromodomain inhibitor, demonstrates high selectivity, nanomolar range cellular potency, and compelling in vivo efficacy.

DUAL946 is a sub-micromolar inhibitor of both BET and class I & IIb HDAC proteins with IC50 of 0.05/0.25/0.42/14.13/34.89 uM for BRD4/HDAC1/HDAC2/HDAC5/HDAC7/HDAC9, respectively.

DW-71177 (DW71177) is a potent and BD1-selective BET inhibitor with ITC KD of 6.7 nM (BRD4-BD1), 20-fold selective over BRD4-BD2, exhibits strong antileukemic activity.

BRD9 inhibitor EA-89 is a potent and selective inhibitor that binds to BRD9 in a novel way.

FHT-2344 (FHT2344) is a potent, selective inhibitor of SMARCA4 and SMARCA2 (BRG1 and BRM) with IC50 of 26 and 13 nM respectively, the ATPase component of the BAF complex.

GNE-234 is the negative control compound of the selective PBRM1(2) inhibitor GNE-235.

GNE-235 (GNE235) is a potent, selective inhibitor of the second bromodomain of polybromo-1 (PBRM1; BAF180; PB1) with KD value of 0.28 uM in BROMOscan assays.

GSK023 is a potent, selective BET BD1 domain inhibitor with pIC50 of 7.8 against BRD4 BD1, >100-fold selective over BD2.

GSK761 (GSK-761) is the first small molecule inhibitor of bromodomain-containing protein SP140, inhibits macrophage inflammatory function.

HPI-1 is a high affinity BET bromodomain binder with low nM Kd for BRD2/3/4 and about 10-fold lower affinity for BRDT. HPI-1 shows much higher affinity to BD2 of BRD2 (17 nM), than to BD1 (540 nM), no apparent selectivity between BRD2/3/4.

iBRD4-BD1 is a potent, selective inhibitor of the first BRD4 bromodomain with IC50 of 12 nM, shows 23- to 6200-fold intra-BET selectivity.

IV-255 is a next-generation selective inhibitor of BRG1 bromodomain, inhibits SWI/SNF complex and enhances DNA damage and cell death in glioblastoma.

IV-275 is a next-generation inhibitor of BRG1 and BRM bromodomains, inhibits SWI/SNF complex and enhances DNA damage and cell death in glioblastoma.

PFI-6 is a selective small-molecule chemical probe inhibitor for the YEATS domain of MLLT1 and MLLT3 with IC50 of 140 nM and 160 nM, respectively.

SJ1461 (SJ-1461) is a potent and orally bioavailable BET inhibitor with IC50 of 6.8/0.2 nM for BRD4 BD1/BD2, and 1.3/0.1 nM for BRD2 BD1/BD2, respectively.

TDI-11055 (TDI 11055) is a potent, selective and orally bioavailable inhibitor of the acyl-lysine reader ENL/AF9 YEATS domain with IC50 of 0.05 and 0.07 uM, respectively.

XL-126 (XL126) is a potent BD1-selective BET inhibitor with SPR binding KD value of 8.9 nM, has 185-fold BD1/BD2 selectivity.

YEATS4 binder 4d is a potent, selective small-molecule epigenetic reader YEATS4 binder with Ki of 33 nM, >10-fold selectivity over YEATS1, 2 and 3.

YEATS4 binder 4e is a potent, selective small-molecule epigenetic reader YEATS4 binder with Ki of 37 nM, >15-fold selectivity over YEATS1, 2 and 3.

ZEN-3694 is a novel potent, orally bioavailable BET bromodomain inhibitor, selectively binds to both bromodomains of the BET proteins, inhibiting the interaction of acetylated histone peptide with IC50 values in low nM range.

2,4-lutidine is a small molecule targeting the UHRF1 tandem Tudor domain (TTD) with TR-FRET (His6-TTD vs. H3K9me3) EC50E of 29.2 uM.

F1957-0088 is a small molecule targeting the UHRF1 tandem Tudor domain (TTD) with TR-FRET (TTD vs. H3K9me3) EC50 of 45.1 uM.

GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity.

A452 is a potent and selective HDAC6 inhibitor, effectively inhibits the cell growth and viability of various cancer cell types, irrespective of p53 status.

CM-1758 is a novel histone deacetylase (HDAC) inhibitor with IC50 of 5 nM and 126 nM for HDAC1 and HDAC6, respectively.

GH8HA01 is a highly potent, selective HDAC8 inhibitor with Ki of 0.67 nM, highly selective against HDAC8 compared to other HDACs.

HO53 is a small moecule inducer of cathelicidin antimicrobial peptide gene (CAMP) expression in bronchial epithelium cells, HO53 is a histone deacetylase (HDAC) inhibitor, interacts directly with HDAC3.

HR488B is a potent, selective HDAC1 inhibitor with IC50 of 1.24 uM, effectively inhibits the proliferation of CRC cells.

KH-259 is a potent, isozyme-selective and CNS-penetrant HDAC6 inhibitor with IC50 of 260 nM, shows weak activity against HDAC1 and HDAC4 (IC50>6 uM).

KPZ560 is a potent, HDAC1/2-selective inhibitor with IC50 of 12/68 nM, respectively.

Mz325 is a potent, selective, dual inhibitor of Sirt2/HDAC6 with IC50 of 320/43 nM, respectively.

NBM-T-L-BMX-OS01 (BMX, HDAC8 inhibitor) is a potent, selective and BB penetrant HDAC8 inhibitor with IC50 of 831 nM.

NN-429 (NN429) is a potent, selective second-generation inhibitor of HDAC6 with IC50 of 3.2 nM, >312-fold selectivityt over all HDAC isoforms.

NT160 is a high affinity, selective class-IIa histone deacetylase (HDAC) inhibitor with IC50 of 80 nM (HDAC4), 600-fold selectivity over HDAC2 and 27-fold selectivity over HDAC8.

PB118 is a potent, selective HDAC6 inhibitor with IC50 of 5.6 nM, shows >1000 times selectively towards HDAC1, reduces alzheimer's disease neuropathology.

Purinostat is a potent, highly selective class I and IIb HDAC inhibitor with IC50 of 0.81, 1.4, 1.7, and 3.8 nM for class I HDAC1, 2, 3, and 8, and 11.5, 1.1 nM for class IIb HDAC 6 and 10, respectively.

RBC1HI is a novel small molecule HDAC1/HDAC2 inhibitor, attenuates behavioral manifestations of oxycodone withdrawal, especially in mice with neuropathic pain.

RGFP963 (RGFP 963) is a potent, selective class I HDAC inhibitor with IC50 of 1.51 uM, 0.75 and 0.096 uM for HDAC1, HDAC2, and HDAC3, respectively.

SBI-46 (SBI 46) is an antiandrogen-equipped histone deacetylase (HDAC) inhibitor, strongly binds to androgen receptor (AR, IC50=8.4 nM) and potently inhibited HDACs and the proliferation of AR+ CRPC.

SP-2-225 is a potent, selective HDAC6 inhibitor, improves antitumor immune responses and prevent tumor relapse after radiotherapy.

TTA03-107 is a potent, selective HDAC1 inhibitor with Ki of 3.22 and 17.6 nM for HDAC1/2, respectively.

TYA-018 (TYA018) is a potent, isoform-selective inhibitor of HDAC6 with IC50 of 10 nM, inhibits tubulin acetylation (Ac-Tubulin) with EC50 of 120 nM in cell-based assay in induced pluripotent stem cell-derived cardiomyocytes (iPSC-CMs).

YAK540 is a potent, highly selective class IIa HDAC inhibitor with IC50 of 114 nM (HDAC4), displays excellent selectivity against HDAC2 (265-fold), HDAC6 (100-fold), and HDAC8 (82-fold).

Yanostat (KH16) is a novel potent HDAC inhibitor with low nanomolar in vitro activity against class I HDACs (HDAC1/2/3 IC50=13/34/6 nM).

YSL-109 (YSL109) is a potent, highly selective small molecule inhibitor of HDAC6 with IC50 of 0.537 nM, >4000-fold selectivity over HDAC1 and HDAC8.

YSR734 is a first-in-class covalent HDACs inhibitor with IC50 of 0.109 uM, 0.154 uM and 0.143 uM for HDAC1, HDAC2, and HDAC3, sparing other deacetylases (HDAC4-HDAC10, IC50>10 uM).

JG-2016 is a small molecule inhibitor of histone acetyltransferase 1 (HAT1) with IC50 of 14.8 uM in the HAT1 acetylation assays.

MC4171 (KAT8 inhibitor 34) is a first-in-class, selective and reversible lysine acetyltransferase KAT8 inhibitor with IC50 of 8.1 uM and SPR Kd of 2.04 uM.

CBA-1 is a small molecule inhibitor of Wnt signaling, specifically targets Jumonji (JmjC) domain-containing demethylase KDM3A with IC50 of 3.9 uM.

EPZ020809 is a potent, specific KDM4C inhibitor with Ki of 31 nM, binds KDM4C in a 2-OG-competitive fashion.

FTO-43 (FTO-43 N) is a potent, selective inhibitor of the m6A demethylase fat mass- and obesity-associated protein (FTO) with IC50 of 1.0 uM, no significant acitivity against the homologous m6A RNA demethylase ALKBH5 (IC50>40 uM).

iPHF8 (inhibitor of PHF8) is a specific inhibitor of protein demethylase PHF8 with IC50 of 2.01 uM in Succinate-Glo JmjC demethylase assays, and SPR KD value of 240 nM.

WS-384 is a specific, small-molecule inhibitor dually targeting LSD1 (IC50=338.8 nM) and the DCN1-UBC12 interaction (IC50=14.8 uM).

ZY0511 is a highly selective and potent inhibitor of lysine-specific histone demethylase 1 (LSD1) with IC50 of 1.7 nM and SPR Kd of 2.42 nM.

BBDDL2059 (BBDDL 2059) is a potent, selective and covalent inhibitor of EZH2 with IC50 of 1.5 nM (EZH2-Y641F), targeting the Cys663 of EZH2.

BN104 (BNM-1192) is a potent, highly selective small molecule menin-MLL inhibitor, BNM-1192 is very potent against leukemia cell lines with MLL-fusion protein and NPM1 mutant (MV-4-11 (AF4 fusion), IC50=3.5 nM).

C220 (PRMT5 inhibitor C220) is a highly potent, selective and SAM cpmpetitive inhibitor of protein arginine methyltransferase 5 (PRMT5) with IC50 of 2.4 nM.

CDIBA is an allosteric inhibitors of m6A-RNA methyltransferase, METTL3 -14 complex with IC50 of 17.3 uM, also reported as a cytosolic phospholipase A2 (cPLA2) inhibitor.

DP308 is a novel and effective 53BP1 tandem Tudor domain (TTD) inhibitor, disrupts the binding between 53BP1 and H4K20me2 peptide with IC50 of 1.69 uM.

DS-1594a (Emilumenib) is a highly potent Menin-MLL1 inhibitor with IC50 of 1.4 nM in cell-free AlphaLISA assays, displays selective growth inhibition against AML and ALL cells with MLL1-r or NPM1c.

EML1219 is a selective small molecule inhibitor of protein arginine methyltransferase isoform PRMT9 with IC50 of 0.2 uM.

EML734 is a selective small molecule inhibitor of protein arginine methyltransferase isoforms, PRMT7 and PRMT9 with IC50 of 0.32 and 0.89 uM, respectively.

EPIC-0307 is a selective small-molecule inhibitor of PRADX-EZH2 interaction, inhibits GBM cell lines with IC50 of 12.13-17.69 uM, enhances temozolomide (TMZ) sensitivity to glioblastoma.

EPZ028862 is a potent, selective inhibitor of SMYD3 with biochemical IC50 of 1.8 nM, and function of cellular methylation IC50 of 32 nM.

EPZ-031686 (EPZ 031686) is a potent, selective, small molecule SMYD3 inhibitor (Biochem IC50=3 nM, Cell IC50= 36 nM).

HKMTI-1-005 is a potent, substrate-competitive dual inhibitor of EZH2 and the closely related G9A/GLP H3K9 methyltransferases with IC50 of 0.1 uM (EHMT2).

IHMT-337 (IHMT337) is a potent, highly selective and irreversible EZH2 inhibitor, specifically inhibits the methylation at H3K27.

iPRMT1 is a potent and selective PRMT1 inhibitor with IC50 of 270 nM, shows good selectivity over other PRMTs.

JS1310 (JS-1310) is a specific small-molecule PRMT7 inhibitor with IC50 of 5 uM (human PRMT7), displays no acitivity against type I PRMTs (PRMT1, 3, 4, 6, and 8, IC50 >100 uM) or the type II PRMT5 (IC50=50 uM).

KMI169 (KMI-169) is a potent and selective lysine methyltransferase 9 (KMT9) inhibitor with ITC Kd of 25 nM and enzymatic IC50 of 50 nM.

KTX-1001 is a potent, selective histone methyltransferase NSD2 (WHSC1, MMSET) inhibitor targeting the catalytic SET domain.

M-808 (M808) is a highly potent, selective and covalent inhibitor of menin-MLL interaction with binding IC50 of 2.6 nM, forms a covalent bond with Cys329 in menin.

A potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50 of 34±10 nM and 43±7 nM, respectively.

MS1262 is a highly potent, selective and brain-penetrant inhibitor of G9a/GLP methylase with IC50 of 19/6 nM, respectively.

PF-06821497 S enantiomer is a novel potent, selective, orally bioavailable EZH2 inhibitor with Ki of <0.1 and 1.15 nM aginast both wt and mutant Y641N EZH2, respectively.

A first-in-class, potent and selective inhibitor of SETD7 methyltransferase with Ki app/IC50 of 0.33/2 nM.

PRT382 (PRT-382) is a potent, selective and SAM-competitive PRMT5 inhibitor with IC50 of 2.8 nM in filtration binding assays with recombinant human PRMT5/MEP50 and histone H2A as the protein substrate.

PRT543 is a highly potent, selective and SAM cpmpetitive inhibitor of protein arginine methyltransferase 5 (PRMT5) with IC50 of 10.8 nM.

(R,R)-59 is a small-molecule ligand activator for methyltransferase SETDB1 Triple Tudor Domain (3TD reader domain) with binding IC50 of 1.2 uM in TR-FRET assays, specifically promotes in vitro SETDB1-mediated methylation of lysine 64 of protein kinase Akt

SKLB-03220 (SKLB03220) is a potent, selective EZH2 covalent inhibitor with IC50 of 1.72 nM (EZH2 WT).

UNC7648 is a small molecule inhibitor of the methyl-lysine reader p53 binding protein 1 (53BP1) tandem Tudor domain (TTD) with TR-FRET IC50 of 8.6 uM.

UNC9512 is a selective methyl-lysine reader p53 binding protein 1 (53BP1) antagonist, binds the 53BP1 tandem Tudor domain (TTD) with TR-FRET IC50 of 0.46 uM, and SPR/ITC Kd vfalues of 0.17/0.41 uM respectively.

TGP-29b-066 (Targapremir-29b-066) is a specfic small-molecule miR-29b inhibitor that targets miR29b hairpin precursor (pre-miR-29b), selectivity and effectively decreases miR-29b expression levels in C2C12 myoblast, attenuates muscle atrophy in vitro and

2800Z is a specific SIRT7 inhibitor, significantly inhibits SIRT7 deacetylation activity without effects on SIRT1 and SIRT6 activities, induces apoptosis and increases chemosensitivity to sorafenib in human liver cancer.

40569Z is a specific SIRT7 inhibitor, significantly inhibits SIRT7 deacetylation activity without effects on SIRT1 and SIRT6 activities, induces apoptosis and increases chemosensitivity to sorafenib in human liver cancer.

FLS-359 (FLS-359) is a selective, allosteric inhibitor of sirtuin 2 (SIRT2) deacetylase activity with IC50 of 3 uM, shows no activity against SIRT1 and SIRT3, exhibits broad-spectrum antiviral activity.

JYQ-42 is a potent, selective SIRT6 allosteric inhibitor, effectively inhibits SIRT6 deacetylation with IC50 of 2.33 uM, inhibits the deacetylation activity of SIRT6 in pancreatic cancer cell lines.

MC 2494 is a nove potent, pan-Sirtuin (SirT) inhibitor, increases RIP1 acetylation in the death domain and induces bona fide tumour-restricted acetylated RIP1/caspase-8-mediated apoptosis.

MC3138 is a potent and selective small-molecule SIRT5 activator, inhibits proliferation in SIRT5-low PDAC cell lines and organoids.

MC3482 is a potent, specific SIRT5 inhibitor, increases the ammonia content in cells leading to autophagy and mitophagy, shows selective SIRT5 inhibition vs SIRT1-3..

MDL-811 (MDL811) is a potent, selective and allosteric SIRT6 activator with EC50 of 5.7 uM (activated SIRT6 deacetylation), two-fold greater activity than MDL-800 (EC50=12.3 uM, Cat# 35760).

SCIC2.1 is a potent small molecule SIRT1 activator (175%, AC50=36.8 uM), directly binds SIRT1 and protects SIRT1 from thermal degradation.

SirReal1.1 is a potent, selective inhibitor of Sirtuin 2 (Sirt2) with IC50 of 0.16 uM.

UBCS373 (Sirt4 inhibitor 69) is a highly isoform selective inhibitor of mitochondrial deacylase Sirtuin 4 (Sirt4) with IC50 of 16 uM.

UBCS385 (Sirt4 inhibitor 60) is a potent, selective inhibitor of mitochondrial deacylase Sirtuin 4 (Sirt4) with IC50 of 0.9 uM.

25B-NBOMe is a highly selective 5-HT2A receptor agonist with Ki of 0.05 nM, 100-fold selective over 5-HT2C (Ki=4.6 nM).

AS2030680 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 0.58, 1.1 and 2.6 nM against human, rat, mouse 5-HT5A receptors, respectively.

AS2674723 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 0.75, 0.67 and 1.9 nM against human, rat, mouse 5-HT5A receptors, respectively.

AS5736 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 3.6, 1.7 and 4.4 nM against human, rat, mouse 5-HT5A receptors, respectively.

CSTI-300 (SMP-100) is a potent, selective 5-HT3 receptor partial agonist with high affinity for human and rat 5-HT3 receptor (Ki=2.0 nM).

E-6801 is a potent, selective 5-HT6 receptor partial agonist of 5-HT6 receptor with pKi of 8.46, cAMP formation EC50 of 8.02.

NH300094 is a potent antagonist of 5-HT receptors and dopamine receptors with IC50 of 0.47 nM, 1.04 nM, 11.71 nM and 31.55 nM for 5-HT2A, D2L, D2S and D3 receptors, respectively.

NU-1223 is a β carboline analog of alstonine and serotonin 5-HT2C receptor agonist, blocks phencyclidine and amphetamine-induced hyperactivity in subchronic phencyclidine mice.

PZ-1922 is a potent, triple-acting 5-HT6R/5-HT3R antagonist and MAO-B reversible inhibitor with Ki of 17/0.45 nM (5-HT6R/5-HT3R), and pIC50 of 8.93 for MAO-B.

TZB-30878 is a potent, selective, orally bioavailable 5-HT1A agonist and 5-HT3 antagonist, selectively binds to human 5-HT1A and 5-HT) receptors with Kd values of 0.68 and 8.90 nM, respectively.

VU6047534 is a selective, peripherally restricted 5-HT2B partial agonist with IC50 of 480 nM in radioligand binding assays.

BnOCPA is a potent and powerful analgesic and a highly selective and potent, full agonist at human adenosine A1 receptors (A1Rs) with pEC50 of 7.23 in a NanoBRET agonist binding assay.

I-ABOPX (BW-A522) is a potent, selective A3 adenosine receptor antagonist with high affinity for both the ovine (Ki=3 nM) and human (Ki=19 nM) A3 receptors.

KF-26777 (KF26777) is a potent and selective adenosine A3 receptor antagonist with Ki of 0.2 nM (human A3 receptor).

MRS7935 is a potent, selective positive allosteric modulator (PAM) of A1 adenosine receptor (A1AR) with EC50 of 1.43 uM.

OT-7999 (OT7999) is a potent and selective adenosine A3 receptor antagonist with Ki of 0.61 nM (human A3 receptor) in radioligand binding assays.

QAF-805 (QAF805) is a potent, dual adenosine-A2B receptor and adenosine-A3 receptor antagonist with Ki of 3.4 nM (A2B).

TRR469 is a potent, selective adenosine A1 receptor (A1AR) positive allosteric modulator with pKb of 5.36, exhibits anti-nociceptive properties in acute and neuropathic pain models in mice.

AS408 is a negative allosteric modulator of the β2-adrenergic receptor (β2AR) for both G-protein activation and arrestin recruitment (pKB=6.8, [35S]GTPγS binding assays), binds to a pocket formed by the membrane-facing surface of TM3 and TM5.

Difluorophenyl Quinazoline (DFPQ, AP-06-202) is a selective, biased, negative allosteric modulator of β-arrestin recruitment to the β2AR, without effect on on β2AR coupling to Gs.

L-771688 (L-771,688, SNAP 6383) is a potent and selective alpha1A (α1A)-adrenoceptor antagonist with binding Ki of 0.13 nM to α1-adrenoceptors in human prostate tissue.

A potent, highly selective α2-adrenoceptor agonist with Ki of 1.08 nM.

Tasipimidine is a potent, selective and orally active human α2A-adrenoceptor agonist with pEC50 of 7.57, >100-fold selectivity over α2B-and α2C-adrenoceptors and the rodent α2D-adrenoceptor.

ZD7114 (ICI D7114) is a potent, selective beta-adrenoceptor agonist, selectively stimulates brown fat and increases whole-body oxygen consumption.

Forasartan (SC-52458) is a potent, specific, competitive and reversible angiotensin II receptor (AT1 receptor) antagonist with binding Ki value of 2.9 nM.