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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC73266 EA-89-YM35
BRD9 inhibitor EA-89 is a potent and selective inhibitor that binds to BRD9 in a novel way.
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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.
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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.
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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.
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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).
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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.
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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)).
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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).
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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.
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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.
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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.
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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.
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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).
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DC73253 BBC1115
BBC1115 is a novel chemotype inhibitor of bromodomain and extra-terminal motif (BET) proteins, displays broad binding across BDs of BET proteins.
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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.
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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.
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DC73250 Lexibulin
An orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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