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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC76302 S234984
S234984 (Compound 13) is a molecular glue enhancer can specifically bind to KBTBD4 and HDAC2 to form a stable ternary complex. S234984 can be used for anti-cancer study.
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DC76301 LSQ-28
LSQ-28 is an orally active HDAC3 inhibitor with an IC50 of 42 nM, and exhibits potent anticancer, antiproliferative, antimigratory, anti-invasive, and antiwound healing activities. LSQ-28 can be utilized in cancer research.
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DC76300 KT32
KT32 (10c) is a potent dual inhibitor of HDAC and Topo II α. KT32 induces cell death through apoptosis.
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DC76299 HDSI-18
HDSI-18 is an orally active HDAC6 selective inhibitor (IC50: 1.6 nM). HDSI-18 is cytotoxic to K562, MV4-11, MOLM-13, THP-1, and Jurkat cells (IC50: 0.48, 0.58, 0.91, 1.79, and 4.31 μM, respectively). HDSI-18 activates Caspase-3, induces mitochondrial depolarization and apoptosis, and has antitumor activity.
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DC76298 Fibrostat
Fibrostat (Compound 5n) is a selective HDAC6 inhibitor that exerts antifibrotic effects by inhibiting HDAC6 activity, with an IC50 value of 63 nM. It also exhibits good selectivity over HDAC1, HDAC3, HDAC5, HDAC8, HDAC10, and HDAC11. Fibrostat significantly downregulates fibrotic markers (fibronectin and collagen 1) in fibroblasts. Additionally, Fibrostat demonstrated no toxicity in rat-perfused heart and zebrafish larvae models. Fibrostat shows potential for research into fibrosis-related diseases.
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DC76297 FF2039
FF2039 (compound 1j) is a specific HDAC1, HDAC6, and HDAC isoforms of class I, IIa and IIb PROTAC degrader. FF2039 demonstrates s significant antiproliferative activity against both hematological and solid cancer cell lines, driven by cell cycle arrest and Apoptosis induction. FF2039 inhibits HDAC isoform of HDAC1, HDAC2, HDAC4 and HDAC6 with IC50s of 1.03, 2.15, 12.4 and 0.053 μM, respectively. FF2039 shows antiproliferative activity against different tumor entities of MM.1S, MDA-MB-231 and U-87MG with EC50s of 2.8, 28 and 30 μM, respectively.
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DC76296 DS-103
DS-103 is an inhibitor for HDAC that inhibits HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8 with IC50s of 0.029, 0.123, 0.022, 0.367 and 9.26 μM, respectively. DS-103 inhibits Plasmodium falciparum 3D7 with IC50 of 5.08 μM. DS-103 exhibits cytotoxicity in cells A2780 and Cal27 with IC50 of 1.48 μM and 1.47 μM, reverses Cisplatin resistance in A2780 and Cal27 with IC50 of 4.62 μM and 2.23 μM. DS-103 exhibits synergistic effect with Cisplatin, enhances Cisplatin-induced apoptosis.
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DC76295 CS4
CS4 is a selective HDAC inhibitor with the IC50 values of 38 nM, 12 nM, 5.8 μM, 19 μM and 61 μM against of HDAC1, HDAC6, HDAC8, HDAC4 and HDAC11, respectively. CS4 promotes α-tubulin and histone 3 acetylation. CS4 activates PPARγ and blocks glycolysis. CS4 induces cell cycle arrest at G2 phase and apoptosis, and shows anticancer effect both in vivo and in vitro.
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DC76294 CHDI-00484077
CHDI-00484077 (Compound 12) is a CNS-penetrant class IIa HDAC inhibitor, with IC50s of 0.01 μM (HDAC4), 0.02 μM(HDAC5), 0.02 μM (HDAC7), 0.03 μM (HDAC9) respectively. CHDI-00484077 can be used for research of huntington’s disease.
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DC76293 C1A
C1A is a class I/II HDACs and sirtuin inhibitor with an IC50 of 479 nM for HDAC6. C1A induces sustained acetylation of HDAC6 substrates, α-tubulin and HSP90. C1A shows srtong anticancer effcts, and induces apoptosis in cancer cells.
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DC76292 Butyrylhydroxamic acid
Butyrylhydroxamic acid (N-Hydroxybutanamide) is a potent inhibitor of histone deacetylase (HDAC). Butyrylhydroxamic acid enhances memory in behavioral models of rodents and can be used as memory enhancers, mood stabilizers, and β-chain hemoglobin disease studies.
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DC76291 Bavarostat
Bavarostat (EKZ-001) is a BBB-penetrable and selective HDAC6 inhibitor (IC50: 0.06 μM). Bavarostat modulates tubulin acetylation selectively over histone acetylation. Bavarostat can be used for research of cancers and central nervous system (CNS) disorders.
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DC76290 (Rac)-Nanatinostat
(Rac)-Nanatinostat ((Rac)-CHR-3996, example 44) is a potent HDAC inhibitor with an IC50 of <330 nM. (Rac)-Nanatinostat has anticancer effects and can effectively inhibit the cell growth of HeLa, U937 and HUT cells.
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DC76289 Delocamten
Delocamten is the inhibitor for cardiac myosin with an IC50 of 1.1 μM. Delocamten can be used in researchs of hypertrophic cardiomyopathy, left ventricular hypertrophy and diastolic dysfunction.
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DC76288 Adhibin
Adhibin is an allosteric inhibitor for RhoGAP class IX myosin, that inhibits Myo9 ATPase in mammalian and invertebrate with IC50 of 2.5 µM and 2.6 µM. Adhibin binds to the ATPase of myosin, interfers with its motor function, blocks the RhoGTPase related signaling pathway, and affects the cell migration, adhesion and cell division. Adhibin can be used in research about cancer metastasis.
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DC76287 (S)-3'-Hydroxy blebbistatin
(S)-3'-Hydroxy blebbistatin is a myosin II inhibitor and is more water-soluble than Blebbistatin.
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DC76286 (S)-3'-Aminoblebbistatin
(S)-3'-Aminoblebbistatin is the derivative of Blebbistatin.
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DC76285 SPA107
SPA107 (Hemiasterlin methyl ester) is a Hemiasterlin.
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DC76284 Myoseverin B
Myoseverin B is a microtubule assembly inhibitor capable of inhibiting the polymerization of tubulin (IC50 = 2 μM) and exhibiting low cytotoxicity in most cell types. Myoseverin B can be used in research as an antitumor agent.
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DC76283 JC168
JC168 is a phenyl analog of peloruside and serves as a microtubule inhibitor, demonstrating antiproliferative and anticancer activities. JC168 promotes tubulin polymerization, thereby interfering with microtubule dynamics, and can be utilized in research related to microtubule-associated disorders.
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DC76282 Icafolin-methyl
Icafolin-methyl is a plant-specific herbicide and an inhibitor of tubulin polymerization. It is metabolized to carboxylic acid icafolin in plants, potentially inhibiting tubulin polymerization by binding to β-tubulin.
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DC76281 Ethaboxam
Ethaboxam is a β-tubulin inhibitor that can be used as anti-oomycete fungicide.
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DC76280 DPP-21
DPP-21 is an inhibitor of tubulin polymerization (IC50: 2.4 μM). DPP-21 shows anti-proliferative activity against cancer cell lines, with IC50s of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23) and 9.37 nM (HepG2) respectively. DPP-21 arrests the cell cycle in the G2/M phase of mitosis, subsequently inducing tumor cell apoptosis (decreases Bcl-2 but upregulates the pro-apoptotic protein Bax).
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DC76279 cis-9,10-Dehydroepothilone D
cis-9,10-Dehydroepothilone D (KOS-1584) is an epothilone derivative with antiproliferative activity and tubulin polymerization activity. cis-9,10-Dehydroepothilone D can be used for the study of lung cancer, colon cancer, prostate cancer and breast cancer.
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DC76278 BKS3031A
BKS3031A is the inhibitor for αβ-tubulin that binds to the colchicine binding site, and inhibits the microtubule assembly dynamics.
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DC76277 AB8939
AB8939 is an effective small moleculeMicrotubule/Tubulin polymerization inhibitor with anti-tumor activity (it inhibits tumor cell proliferation with an IC50 of less than 10 nM). AB8939 can effectively evade resistance mechanisms mediated by things like P-glycoprotein and myeloperoxidase. AB8939 can induce G2/M phase cell cycle arrest and apoptosis in cells.
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DC76276 7-Acetyl paclitaxel
7-Acetyl paclitaxel is a microtubule depolymerization inhibitor which inhibits calcium-induced microtubule depolymerization. 7-Acetyl paclitaxel reduces the growth of J774.2 macrophages (IC50 ~ 60 nM) and increases the levels of nitric oxide (NO) and TNF in isolated mouse peritoneal macrophages.
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DC76275 (S)-AM-9022
(S)-AM-9022 is the S-enantiomer of AM-9022. 2-Methylbiphenyl-oxadiazole-NH-Ph-CHO can be utilized in AUTAC synthesis.
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DC76274 K34c hydrochloride
K34c hydrochloride is a potent and selective α5β1 integrin antagonist. By inhibiting α5β1 integrin, K34c hydrochloride reduces chemotherapy-induced premature senescence and promotes apoptosis. K34c hydrochloride can be used in glioblastoma research.
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DC76273 EMD-132338
EMD-132338 is a GPIIb/IIIa (αIIbβ3) antagonist that inhibits platelet aggregation. EMD-132338 can be utilized in antithrombosis research.
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