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Cat. No. Product name CAS No.
DC73214 kt-3283

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.

DC73215 Mortaparib

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.

139393-50-3
DC73216 Mortaparib Plus

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

727701-39-5
DC73218 HC-5404

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.

2247396-91-2
DC73219 Allopole Featured

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.

DC73220 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.

DC73221 SBE13

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).

775294-82-1
DC73222 (R)-BA-1049

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

1973494-16-4
DC73223 (S)-BA-1049

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

2146097-17-6
DC73224 C3TD879

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

2850259-33-3
DC73225 ITRI-E-(S)4046

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.

2661229-35-0
DC73226 Netarsudil

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

1254032-66-0
DC73227 DIZ-3

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)

2675490-72-7
DC73228 Teloxantron

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.

2016813-83-3
DC73229 LMP744

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

308246-52-8
DC73230 SD133

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.

1239467-61-8
DC73231 GB1490

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.

2172866-22-5
DC73232 6-B345TTQ

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.

297157-87-0
DC73233 7HP349

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.

1378535-08-0
DC73234 A7B7C7

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

495402-33-0
DC73235 AXT107

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.

DC73236 GSK3335103 Featured

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.

1893340-21-0
DC73237 GW559090

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.

278598-52-0
DC73238 IVL745

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.

229627-58-1
DC73239 MSR03

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.

DC73240 TBC4746

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.

422268-99-3
DC73241 AM-1882 Featured

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

2600559-12-2
DC73242 AM-9022 Featured

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.

2446872-46-2
DC73243 ALM201

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.

959961-27-4
DC73244 CH-2-77

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.

2408642-05-5
DC73245 CH-2-77 analogue 60c

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.

2757188-21-7
DC73246 EAPB02303

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.

1958290-51-1
DC73247 FiVe1 Featured

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.

932359-76-7
DC73248 KGP591

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.

DC73249 KGP618

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

DC73250 Lexibulin

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

DC73251 R-huezole

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.

DC73252 TN-2

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.

2983719-82-8
DC73253 BBC1115

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

DC73254 BI 1702135

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

2906881-71-6
DC73255 BI-4827

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

2001082-00-2
DC73256 BI-7190

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

2001082-11-5
DC73257 CDD-787

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.

2822750-93-4
DC73258 CDD-956

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.

2994671-53-1
DC73259 CG13250

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).

1629873-75-1
DC73260 CG223

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)).

1629873-79-5
DC73261 CN210

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.

2098715-58-1
DC73262 DDO-8926

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).

DC73263 Dual PI3K/BET 18DS

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.

2750361-19-2
DC73264 DUAL946

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.

1868180-45-3
DC73265 DW-71177

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.

2241311-72-6
DC73266 EA-89-YM35

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

DC73267 FHT-2344

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.

2468058-90-2
DC73268 GNE-234

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

DC73269 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.

DC73270 GSK023

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

DC73271 GSK761

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

DC73272 HP-4833

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.

DC73273 iBRD4-BD1

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.

2839318-17-9
DC73274 IV-255

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

DC73275 IV-275

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.

DC73276 PFI-6

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.

2675452-91-0
DC73277 SJ1461

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.

DC73278 TDI-11055

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.

2657651-10-8
DC73279 XL-126

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.

DC73280 YEATS4 binder 4d

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.

DC73281 YEATS4 binder 4e

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.

DC73282 ZEN-3694

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.

DC73283 2,4-lutidine

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.

108-47-4
DC73284 F1957-0088

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

65541-95-9
DC73285 GSK3482364 Featured

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.

2170136-65-7
DC73287 A452

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

798543-42-7
DC73288 CM-1758

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

2256079-39-5
DC73289 GH8HA01

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

DC73290 HO53

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.

DC73291 HR488B

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

DC73292 KH-259

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).

DC73293 KPZ560

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

2397562-43-3
DC73294 Mz325

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

DC73295 NBM-T-L-BMX-OS01

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

1246952-34-0
DC73296 NN-429

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.

2490284-32-5
DC73297 NT160

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.

1418293-40-9
DC73298 PB118

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

DC73299 Purinostat

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.

1929583-17-4
DC73300 RBC1HI

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

2121516-13-8
DC73301 RGFP963

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.

1396720-98-1
DC73302 SBI-46

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.

DC73303 SP-2-225

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

2364448-93-9
DC73304 TTA03-107

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

2397562-25-1
DC73305 TYA-018 Featured

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).

2653254-31-8
DC73306 YAK540

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).

DC73307 Yanostat

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).

DC73308 YSL-109

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.

2578957-91-0
DC73309 YSR734

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).

DC73310 JG-2016

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

2887480-87-5
DC73311 MC4171

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.

DC73312 CBA-1

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

333318-69-7
DC73313 EPZ020809

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

956723-02-7
DC73314 FTO-43

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).

2640366-38-5
DC73315 iPHF8

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.

1574530-99-6
DC73316 WS-384

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

2247544-03-0
DC73317 ZY0511

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.

2058310-24-8
DC73318 BBDDL2059

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.

2691174-27-1
DC73319 BN104

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).

2938995-50-5
DC73320 C220

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.

1989620-03-2
DC73321 CDIBA

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.

479422-22-5
DC73322 DP308 Featured

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.

685884-37-1
DC73323 DS-1594a

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.

2440018-29-9
DC73324 EML1219

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

DC73325 EML734

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.

DC73326 EPIC-0307

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.

894949-88-3
DC73327 EPZ028862

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

1887082-53-2
DC73328 EPZ-031686

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

1808011-22-4
DC73329 HKMTI-1-005

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).

1932653-80-9
DC73330 IHMT-337 Featured

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

DC73331 iPRMT1

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

DC73332 JS1310

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).

2247753-73-5
DC73333 KMI169

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.

DC73334 KTX-1001

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

2604513-16-6
DC73335 M-808

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.

2377335-74-3
DC73336 MS-049

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

1502816-23-0
DC73337 MS1262

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

DC73338 PF-06821497 S enantiomer

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.

1844849-11-1
DC73339 PFI-2

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

1627676-59-8
DC73340 PRT382

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.

2242790-05-0
DC73341 PRT543

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

DC73342 SETDB1 activator (R,R)-59

(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

2755823-12-0
DC73343 SKLB-03220

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

2852050-29-2
DC73344 UNC7648

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.

DC73345 UNC9512

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.

DC73346 TGP-29b-066

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

349429-86-3
DC73347 2800Z

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.

1048966-16-0
DC73348 40569Z

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.

2640673-56-7
DC73349 FLS-359

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.

2309398-79-4
DC73350 JYQ-42 Featured

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.

2838025-41-3
DC73351 MC 2494

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.

DC73352 MC3138

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

1844889-12-8
DC73353 MC3482

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..

2922280-86-0
DC73354 MDL-811

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).

2275619-98-0
DC73355 SCIC2.1

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

923763-29-5
DC73356 SirReal1.1

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

1862238-00-3
DC73357 UBCS373

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

DC73358 UBCS385

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

DC73359 25B-NBOMe

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).

1026511-90-9
DC73360 AS2030680

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.

2170562-35-1
DC73361 AS2674723

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.

1392819-23-6
DC73362 ASP5736

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.

1264206-74-7
DC73363 CSTI-300

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).

DC73364 E-6801

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.

528859-04-3
DC73365 NH300094

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.

2647419-63-2
DC73366 NU-1223

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.

2415092-49-6
DC73367 PZ-1922

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.

1648745-65-6
DC73368 TZB-30878

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.

864385-95-5
DC73369 VU6047534

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

DC73370 BnOCPA

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.

872693-38-4
DC73371 I-ABOPX

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.

112533-64-9
DC73372 KF-26777

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

206129-88-6
DC73373 MRS7935

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

DC73374 OT-7999

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.

246031-23-2
DC73375 QAF-805 Featured

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

431040-19-6
DC73376 TRR469

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.

1394867-58-3
DC73377 AS408

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.

2378521-26-5
DC73378 Difluorophenyl Quinazoline

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.

911678-60-9
DC73379 L-771688

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.

200050-59-5
DC73380 Medetomidine hydrochloride

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

86347-15-1
DC73381 Tasipimidine

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.

1465908-70-6
DC73382 ZD7114

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

129689-30-1
DC73383 Forasartan

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

145216-43-9
DC73384 DSO-5a

DSO-5a (Dimethyl shikonin oxime 5a) is a potent, selective agonist pf bombesin receptor subtype-3 (BB3, BRS-3) with pEC50 of 8.4 (IP-1 accumulation in hBB3-H1299 cells).

2765182-03-2
DC73385 (S)-AC-265347

(S)-AC-265347 is a potent, selective CaSR agonist and positive allosteric modulator (ago-PAM), 10- to 20-fold more potent than (R)-AC-265347.

1253901-30-2
DC73386 AM6527

AM6527 is a highly potent, selective cannabinoid CB1 receptor antagonist with binding Ki of 4.88 nM, 100-fold selective over CB2 receptors.

1797883-78-3
DC73387 JM-00266

JM-00266 is a novel non-brain penetrant cannabinoid receptor 1 (CB1R) inverse agonist.

2090325-46-3
DC73388 JWH133

JWH133 (JWH-133) is a potent and selective CB2 agonist with Ki of 3.4 nM, 200-fold selective over CB1 receptors, inhibits glioma growth in vivo.

259869-55-1
DC73389 LEI-102

LEI-102 (LEI 102) is a potent, selective cannabinoid CB2 receptor agonist with binding pKi of 8.0, 1000-fold selectivity over CB1R.

1228659-40-2
DC73390 URB447

URB447 (URB-447) is a peripherally restricted CB(1) antagonist/CB(2) agonist with IC50 of 313 nM (rat CB1) and 41 nM (human CB2).

1132922-57-6
DC73391 BMS-694153

BMS-694153 is a potent, selective calcitonin gene-related peptide (CGRP) receptor antagonist with Ki of 0.013 nM for hCGRP (inhibition of 125I-CGRP binding in SK-N-MC cell membranes).

1050381-35-5
DC73392 ACT-672125

ACT-672125 (ACT672125) is a potent, selective CXCR3 antagonist with IC50 of 239 nM in human blood.

1449367-94-5
DC73393 alpha-NETA

alpha-NETA (α-NETA) is a small molecule antagonist of chemerin receptor chemokine-like receptor 1 (CMKLR1), inhibits chemerin-stimulated β-arrestin2 association with CMKLR1 with IC50 of 4.9 uM.

115066-04-1
DC73394 AZ12436092

AZ12436092 (AZ 12436092) is a potent, selective CCR3 antagonist with binding pKi value of 9.2.

921204-43-5
DC73395 AZD3778

AZD3778 (AZD-3778) is a dual CCR3 and H1-receptor antagonistwith Ki of 54 nM for guinea-pig H1-receptor, inhibits binding of CR3 radioligand 125I-eotaxin to human CCR3-receptor expressed on CHO-cells with IC50 of 8 nM.

485391-80-8
DC73396 BPRCX714

BPRCX714 (BPRCX 714) is a highly selective and potent CXCR4 antagonist with binding IC50 of 34.2 nM, effectively inhibits CXCL12-induced movement of CCRF-CEM cells with EC50 of 13.7 nM.

1892574-13-8
DC73397 BPRCX807

BPRCX807 (BPRCX-807) is a highly selective and potent CXCR4 antagonist with binding IC50 of 40.4 nM and EC50 of 48.1 nM for cell-mobility activity in the chemotaxis assays, inhibits CXCL12-mediated cell signaling pathway.

2236595-58-5
DC73398 CCX2553

A potent and specific CCR6 antagonist.

DC73399 DF2755A

DF2755A is a selective, allosteric, orally acting inhibitor of CXCR1/2 (Kd=2.24/0.94 nM), inhibits human PMN (hPMN) migration induced by CXCL8 and CXCL1 with IC50 of 4.2 and 2.1 nM, respectively.

1218784-94-1
DC73400 GW782415W

GW782415W (GW782415) is a potent, specific CCR3 antagonist, inhibits chemotaxis of human and murine eosinophils pKi of 8.08 and 7.85, respectively.

408304-25-6
DC73401 Ki19003

Ki19003 (Ki 19003) is a potent, specific CCR3 antagonist, inhibits the CCL11-induced migration of CCR3-expressing L1.2 cells with IC50 of 20 nM.

444595-19-1
DC73402 LN6023

LN6023 (LN-6023) a potent, selective and first-in-class inhibitor of the atypical chemokine receptor 3 (ACKR3, CXCR7) with β-arrestin EC50 of 3.5 uM.

DC73403 NUCC-390 dihydrochloride

NUCC-390 dihydrochloride (NUCC390) is a small molecule agonist of CXCR4, recapitulates the activity of CXCL12α.

2749281-71-6
DC73404 RAP-103

RAP-103 is an orally active, stabilized pentapeptide analog of DAPTA (D-ala-peptide T-amide), and multi-chemokine receptor antagonist.

DC73405 SCH-479833

SCH-479833 is a potent, specific and orally active CXCR1 and CXCR2 antagonist with Ki of 0.17 and 7 nM, respectively.

473725-29-0
DC73406 UCB35625

UCB35625 is a potent, selective inhibitor of CCR1 and CCR3, inhibits MIP-1α-induced chemotaxis in CCR1 transfectants and eotaxin-induced chemotaxis in CCR3 transfectants with IC50 of 9.57 and 93.8 nM respectively.

202796-42-7
DC73407 UCUF-965

UCUF-965 (UCUF965) is a potent partial agonist and positive allosteric modulator of CXCR4 with EC50 of 0.02 uM, Emax=44% for CXCR4/CXCL12 signaling for β-arrestin-2 recruitment.

2965316-77-0
DC73408 VUF15485

VUF15485 is a small-molecule agonist of the atypical chemokine receptor ACKR3 with binding pIC50 of 8.3, and pEC50 of 7.6 in BRET-based β-arrestin2 recruitment assay.

2800877-68-1
DC73409 YM-344031 Featured

YM-344031 is a potent, selective, brain-penetrable CCR3 antagonist with binding IC50 of 3.0 nM, inhibits ligand-induced Ca(2+) flux with IC50 of 5.4 nM.

671204-98-1
DC73410 YM-344484

YM-344484 (YM344484) is a potent, selective dual antagonist of chemokine CCR3 receptor and histamine H1 receptor, potently inhibits both the CCL11-induced Ca2+ influx in human CCR3-expressing cells (Kb=1.8 nM) and histamine-induced Ca2+ influx in histamin

671205-14-4
DC73411 YM-355179

YM-355179 is a potent selective, and orally available antagonist of CC chemokine receptor 3 (CCR3) with binding IC50 of 7.6 nM (CCL5).

672957-37-8
DC73412 BMK-C205

BMK-C205 (BMK-C 205) is a potent, selective corticotropin-releasing hormone receptor 1 (CRF1R) antagonist with IC50 of 74 nM in calcium mobilization assays, blocks hypothalamus-pituitary-adrenal (HPA) axis activation.

2950971-22-7
DC73413 NBI-27914

NBI-27914 is a potent, selective antagonist of corticotropin-releasing factor 1 (CRF1) receptor with Ki of 1.7 nM, shows no activity at CRF2 receptors.

184241-44-9
DC73414 NBI-35965

NBI-35965 is a potent, selective antagonist of corticotropin-releasing factor 1 (CRF1) receptor with Ki of 4 nM, >1000-fold selective over CRF2.

268546-19-6
DC73415 (-)-GSK598809

GSK598809 (GSK-598809) is a potent, selective dopamine D(3) receptor antagonist with Ki value of 6.2 nM, >100-fold selectivity over D2 receptor.

863680-46-0
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