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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC80801 H-Ile-Ala-OH
H-Ile-Ala-OH (Ile-Ala; L-Isoleucyl-L-alanine) is a linear aliphatic dipeptide and self-reactive cyclization reagent that self-assembles into amorphous films or spherical structures from specific solvents. H-Ile-Ala-OH also serves as a precursor for the synthesis of the cyclic peptide cyclo (L-isoleucyl-L-alanine). H-Ile-Ala-OH undergoes solid-state cyclization when heated above 206 °C, and its initiation temperature is closely related to the size of side-chain substituents.
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DC80800 HIF-PHD-IN-5
HIF-PHD-IN-5 (Compound A4) is a hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD) inhibitor. HIF-PHD-IN-5 can be used for the research of neurological disease.
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DC80799 HIF-1α-IN-10
HIF-1α-IN-10 is a ligands for target protein for PROTAC (HIF-1α). HIF-1α-IN-10 can be used to synthesize PROTAC HIF-1α degrader-2.
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DC80798 HI-280
HI-280 is a human immunodeficiency virus type 1 (HIV-1) reverse transcriptase inhibitor. HI-280 can be used for the research of infection.
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DC80797 HGF-IN-1
HGF-IN-1 ((the compound on the left in the second line of page 77) is a HGF inhibitor. HGF-IN-1 can be used in cancer research.
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DC80796 Hexoprenaline sulfate
Hexoprenaline sulfate is an orally active and selective β-adrenergic receptor agonist. Hexoprenaline sulfate can dilate the bronchi. Hexoprenaline sulfate can activate adenylate cyclase and increases 14C-Aminopyrine uptake. Hexoprenaline sulfate exhibits anti-infection and anti-inflammmation effect. Hexoprenaline sulfate can increase placental weight and blood flow. Hexoprenaline sulfate can be used for the researches of inflammation, immunology, infection, endocrinology and neurological disease, such as asthma, chronic bronchitis, sepsis and intoxication of organophosphorus compounds.
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DC80795 Hexaprofen
Hexaprofen is a 2-arylpropionic acid derivative. Hexaprofen inhibits CXCL8-induced chemotaxis, while no activity is detected against CXCL1-induced chemotaxis.
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DC80794 Hexane-2,5-dione
Hexane-2,5-dione (2,5-HD) is a cytotoxic agent. Hexane-2,5-dione causes an accumulation of neurofilaments within axons in rats that may lead to their degeneration. Hexane-2,5-dione is promising for research of neurodegenerative diseases (e.g., Alzheimer's, Parkinson's).
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DC80793 Herbicide safener-1
Herbicide safener-1 (II-Q001) is a crop protection and safety agent. Herbicide safener-1 can protect crops from the damage caused by pesticides (such as herbicides and fungicides).
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DC80792 Herbicidal agent 15
Herbicidal agent 15 is a uracilpyridine herbicide. Herbicidal agent 15 controls harmful plants and acts on plants, their seeds, and their habitat to manage unwanted vegetation.
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DC80791 HER2-IN-23
HER2-IN-23 is a selective HER2 inhibitor. HER2-IN-23 reduces in total HER2 expression rather than in phosphorylated HER2 (p-HER2). HER2-IN-23 reduces cyclin D1 level and stimulates PARP cleavage. HER2-IN-23 can be used for the study of HER2-positive breast cancer.
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DC80790 Heptenophos
Heptenophos is an inhibitor of AChE and plasma carboxylesterase (CES). By inhibiting AChE activity, Heptenophos causes the accumulation of acetylcholine at cholinergic synapses, thereby triggering typical symptoms of organophosphate poisoning. Heptenophos exhibits rapid lethal toxicity in male albino mice, but its toxic effects are effectively antagonized by obidoxime, and Memantine further enhances the detoxification efficacy of obidoxime. Therefore, Heptenophos is commonly used in studies related to the mechanism of organophosphate poisoning and detoxification strategies.
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DC80789 Hepoxilin A3
Hepoxilin A3 (HXA3) is a neutrophil chemo-attractant, synthesized by activating the PLA2-12-LOX pathway. Hepoxilin A3 can guide neutrophils to cross the epithelial barrier and migrate to the infection site (such as the alveolar cavity). The level of Hepoxilin A3 increases synchronously with neutrophil infiltration in mouse models. Hepoxilin A3 can be used to study inflammatory diseases (such as pneumonia, cystic fibrosis).
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DC80787 HDAC-IN-99
HDAC-IN-99 is a histone deacetylase (HDAC) inhibitor with an IC50 of 37.73 nM, and it exhibits potent inhibitory activity against HDAC1 (IC50 = 48.09 nM), HDAC2 (IC50 = 300.28 nM) and HDAC6 (IC50 = 9.16 nM). HDAC-IN-99 inhibits the enzymatic activity of HDAC and exerts broad-spectrum antiproliferative activity in various cancer cell lines. HDAC-IN-99 induces S-phase cell cycle arrest and apoptosis in colon cancer cells, increases the acetylation levels of histone H3, histone H4 and α-tubulin, and upregulates the expression of p21 as well as the cleavage of caspase-3. HDAC-IN-99 displays antitumor activity in colon cancer xenograft models. HDAC-IN-99 can be used for the research of colon cancer.
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DC80786 HDAC-IN-97
HDAC-IN-97 is a PROTAC HDAC6 degrader-6that can be used for synthesis of PROTACs, such as HDAC6 degrader-6. HDAC6 degrader-6 is a potent HDAC6 PROTAC degrader with anticancer activity.
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DC80785 HDAC-IN-96
HDAC-IN-96 (Compound 3f) is a selective HDAC1/2 inhibitor with IC50 values of 457.1 and 433.7 nM. HDAC-IN-96 has strong inhibitory activity against multiple hematological tumor cells (RS4;11, K562, RPMI-8226, U266), with IC50 values ranging from 2.11 to 5.35 μM. HDAC-IN-96 can induce cancer cells apoptosis and S phase arrest. HDAC-IN-96 can be used for the research of cancer, such as acute lymphoblastic leukemia.
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DC80784 HDAC-IN-95
HDAC-IN-95 (Compound 9) is a HDAC inhibitor. HDAC-IN-95 can be used for the study of non-small cell lung cancer (NSCLC).
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DC80783 HDAC8-IN-16
HDAC8-IN-16 is a selective histone deacetylase 8 (HDAC8) inhibitor with an IC50 of 0.16 μM. HDAC8-IN-16 induces cell apoptosis, triggers G2/M phase cell cycle arrest, and moderately inhibits cancer cell proliferation. HDAC8-IN-16 is applicable to relevant research on colorectal cancer.
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DC80782 HDAC6-IN-80
HDAC6-IN-80 is an orally active, selective HDAC6 inhibitor with an IC50 of 8.5 nM. HDAC6-IN-80 inhibits lipopolysaccharide-induced microglial activation, reduces the levels of iNOS, COX-2, TNF-α and IL-6, and alleviates sensory hypersensitivity behaviors. HDAC6-IN-80 can be used for the research of inflammatory pain and chemotherapy-induced peripheral neuropathy.
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DC80781 HDAC6-IN-78
HDAC6-IN-78 (Example 48) is a selective HDAC6 inhibitor with an IC50 of 24 nM. HDAC6-IN-78 shows no activity against other HDAC isoforms.
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DC80780 HDAC6-IN-77
HDAC6-IN-77 is a highly selective HDAC6 inhibitor with an IC50 of 7.0 nM.HDAC6-IN-77 induces neurite outgrowth.HDAC6-IN-77 exerts neuroprotective activity.HDAC6-IN-77 shows no significant toxicity on dopaminergic cells.HDAC6-IN-77 can be used for the research of Alzheimer's disease.
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DC80779 HDAC6-IN-76
HDAC6-IN-76 (Compound G25) is a selective HDAC6 inhibitor with an IC50 of 12 nM. HDAC6-IN-76 induces Autophagy in a p53-dependent manner. HDAC6-IN-76 induces Apoptosis in a p53-dependent manner. HDAC6-IN-76 exhibits anticancer activity against hematologic malignancies, including acute myeloid leukemia.
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DC80778 HDAC6-IN-75
HDAC6-IN-75 is a selective HDAC6 inhibitor with an IC50 of 0.17 nM against HDAC6. HDAC6-IN-75 induces the accumulation of acetylated α-tubulin in glioma cells. HDAC6-IN-75 triggers cell cycle changes, increases the SubG1 cell population, and promotes apoptosis in glioma cells and glioblastoma stem cells. HDAC6-IN-75 is applicable for glioma-related research.
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DC80777 HDAC6-IN-67
HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer.
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DC80776 HDAC6-IN-65
HDAC6-IN-65 is a selective HDAC6 inhibitor (IC50 = 0.9 nM) and also exhibits a certain suppressive effect on HDAC3 (IC50 = 39.4 nM). HDAC6-IN-65 can induce the accumulation of α-tubulin (ac-tubulin) and acetylated histone H3 (ac-histone H3, a class I HDAC inhibition marker) in Neuro-2a cells. HDAC6-IN-65 can be used for the study of melanoma.
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DC80775 HDAC6 ligand-7
HDAC6 ligand-7 (Compound 16a) is a positron emission tomography (PET) tracer for the deacetylase 6 (HDAC6) enzyme with a Kd value of 1.66 nM. HDAC6 ligand-7 exhibits excellent HDAC6 inhibitory activity, with IC50 values of 2.7 and 3.7 nM for hHDAC6 and mHDAC6, respectively, and has high selectivity for HDAC1/4/7/8. HDAC6 ligand-7 after being radioactively labeled with fluorine-18, [¹⁸F]HDAC6 ligand-7 shows varying degrees of radioactive uptake in PET, which can reflect the specific binding to HDAC6. HDAC6 ligand-7 can be used for the study of HDAC6 imaging.
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DC80774 HDAC3-IN-8
HDAC3-IN-8 is a selective inhibitor targeting HDAC1, HDAC2 and HDAC3, with IC50 values of 3.52 nM for HDAC1, 15.14 nM for HDAC2 and 0.38 nM for HDAC3. HDAC3-IN-8 shows high selectivity for HDAC3 and exerts its effect by inhibiting histone deacetylase activity. HDAC3-IN-8 can be used to construct HDAC3-targeted PROTAC degrader and is suitable for the research of acute myeloid leukemia (AML).
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DC80773 HDAC3 degrader-2
HDAC3 degrader-2 is a selective HDAC3 degrader. HDAC3 degrader-2 inhibits the activation of the NLRP3 inflammasome by degrading HDAC3, thereby reducing the maturation of IL-1β and caspase-1. HDAC3 degrader-2 exhibits anti-inflammatory activity. HDAC3 degrader-2 can be used in research related to endotoxin shock, colitis and gouty arthritis.
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DC80772 HDAC1-IN-10
HDAC1-IN-10 (Compound 2b) is a potent, selective and orally active HDAC1/2 inhibitor with IC50 values of 6 and 190 nM. HDAC1-IN-10 shows IC50 > 50 μM for HDAC3-8. HDAC1-IN-10 can inhibit tumor growth in HCT-116 colon xenograft nude mice model. HDAC1-IN-10 can be used for research of colon cancer.
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DC80771 HDAC1/3-IN-1
HDAC1/3-IN-1 is a selective HDAC1/3 inhibitor, with IC50 values of 256 nM and 340.3 nM against HDAC1 and HDAC3, respectively. HDAC1/3-IN-1 increases the SubG1 cell population and promotes apoptosis of glioma cells and glioblastoma stem cells. HDAC1/3-IN-1 can be used in studies related to glioblastoma.
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