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PROTACs

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Cat. No. Product Name Field of Application Chemical Structure
DC80860 iNOs-IN-7
iNOs-IN-7 (example 4) is an inducible nitric oxide synthase (NOS) inhibitor. iNOs-IN-7 can be used for the study of inflammatory disease and pain.
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DC80853 iMQT_020
iMQT_020 is a selective allosteric SLC1A5_var inhibitor. iMQT_020 disrupts the trimeric assembly of SLC1A5_var, causing metabolic crisis in cancer cells and selectively suppressing their growth. iMQT_020 reduces glutamine anaplerosis and oxidative phosphorylation, resulting in a broad disruption of cancer metabolism. iMQT_020 reduces GSH levels and increases cellular ROS and mitochondrial ROS. iMQT_020 induces apoptosis and ferroptosis. iMQT_020 can epigenetically upregulate PD-L1 expression. iMQT_020 can be used for the study of pancreatic cancer, lung cancer, and colon cancer.
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DC80851 Im-m7GDP
Im-m7GDP is the cap reagent that can be used for nucleic acid synthesis.
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DC80847 IL-17-IN-5
IL-17-IN-5 (Compound 3) is an IL-17 inhibitor with an IC50 of <0.1 μM. IL-17-IN-5 can be used in the research of inflammatory diseases.
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DC80846 IL-17-IN-4
IL-17-IN-4 (Compound 3) is an IL-17 inhibitor with an IC50 of less than 0.1 μM. IL-17-IN-4 can be used for the study of inflammatory diseases.
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DC80840 IK-595
IK-595 is a MEK1/MEK2 inhibitor with high affinity (7.39 nM).IK-595 blocks EGF-induced ERK1/2 phosphorylation in AsPC-1 cells with IC50 value of 0.1 nM. IK-595 has oral activity and blood-brain barrier penetration. IK-595 can be used for the research of Ras/MAPK pathway-altered cancers.
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DC80831 ICI 198615
ICI 198615 is a lipoxygenase inhibitor. ICI 198615 inhibits the activity of lipoxygenases involved in eicosanoid metabolism. ICI 198615 attenuates the early phase of bronchoconstriction induced by ET-1.
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DC80830 ICI 185282
ICI 185282 is a potent, selective, orally active thromboxane A2 (TXA₂) receptor antagonist. ICI 185282 causes dose-dependent inhibition of U-46619-induced platelet aggregation ex-vivo in guinea-pig. ICI 185,282 inhibits bronchospasm induced by U-46619, PGD2, PGF2α, arachidonic acid, LTD4 and PAF in vivo. ICI 185282 can be used for bronchial asthma research.
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DC80826 IAXO-101 iodide
IAXO-101 iodide is a TLR4/CD14 blocker. IAXO-101 iodide can inhibit the innate immune pathway of CD14. IAXO-101 iodide is capable of improving the recording performance of intracortical microelectrodes in mice. IAXO-101 iodide can also partially alleviate fetal growth restriction, placental vascular damage, and reduce the level of the inflammatory factor TNF-α in pregnant mice infected with malaria. IAXO-101 iodide can be used in the research of gestational malaria and inflammatory diseases.
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DC80820 Hsp90-IN-46
Hsp90-IN-46 is a Hsp90 inhibitor. Hsp90-IN-46 exhibits broad-spectrum antiproliferative activity against tumor cell lines. Hsp90-IN-46 inhibits breast cancer cell proliferation by reducing colony formation and downregulating the proliferation marker Ki-67. Hsp90-IN-46 inhibits Hsp90 and its ATPase activity, downregulates the downstream substrate oncoproteins HER2 and CDK4, and moderately induces the heat shock response. Hsp90-IN-46 shows significant antitumor activity in a mouse model of triple-negative breast cancer tumor xenografts. Hsp90-IN-46 can be used for research on various cancers including triple-negative breast cancer, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer.
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DC80819 Hsp90-IN-44
Hsp90-IN-44 (compound 16) is a Hsp90 inhibitor with an IC50 of 9.8 µM. Hsp90-IN-44 can be used for cancer research.
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DC80817 HSP90-IN-28
HSP90-IN-28 (compound 12 h) is a potent and selective Hsp90 inhibitor with an IC50 of 0.46 μM for Hsp90α. HSP90-IN-28 exhibits ~48 fold selectivity versus other Hsp90β (IC50 = 22.28 μM).
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DC80814 HPK1-IN-64
HPK1-IN-64 is a potent, selective, and orally active HPK1 inhibitor with an IC50 value of 1.9 nM. HPK1-IN-64 exhibits selectivity exceeding 100-fold, 80-fold, 300-fold, and 350-fold against off-target kinases such as GLK, MAP4K5, TBK1, and TNIK, respectively. HPK1-IN-64 inhibits SLP76 protein phosphorylation and IL-2 secretion. HPK1-IN-64 may be used in cancer research, such as for colorectal cancer.
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DC80811 HO 221
HO 221 is an orally active benzoylphenylurea derivative with antitumor activity. HO 221 can inhibit the activity of mammalian DNA polymerase alpha. HO 221 can induce G1 phase arrest. HO 221 can be used for the research of cancer, such as leukemia.
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DC80808 HK2-IN-3
HK2-IN-3 (compound 12) is a potent hexokinase 2 (HK2) inhibitor with an IC50 of 56.4 nM. HK2-IN-3 reduces glucose uptake and downregulated GLUT1/GLUT4 in oral squamous cell carcinoma (OSCC). HK2-IN-3 induces mitophagy and apoptosis. HK2-IN-3 suppresses tumor growth and angiogenesis in OSCC xenograft mouse models. HK2-IN-3 can be used for OSCC research.
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DC80806 HIV-1-IN-88
HIV-1-IN-88 (compound 20a) is a potent HIV‑1 protease inhibitor (IC50 = 10 pM) with an antiviral EC50 of 10.4 nM. HIV-1-IN-88 exhibits potency against the multidrug-resistant variants HIV-1Muta and HIV-1I50V with EC50 values of 30.0 and 34.3 nM, respectively. HIV-1-IN-88 can be used for HIV research.
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DC80804 HIV RT-IN-1
HIV RT-IN-1 is an inhibitor of HIV integrase and HIV reverse transcriptase-associated ribonuclease H. HIV RT-IN-1 is applicable to research related to HIV-1 infection.
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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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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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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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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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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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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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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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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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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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DC80770 HDAC1 activator-1
HDAC1 activator-1 is a specific HDAC1 activator with orally activity, exerting no significant effects on other HDAC family members. HDAC1 activator-1 exhibits neuroprotective activity, ameliorates cognitive and motor function deficits by reducing neuronal loss and gliosis. HDAC1 activator-1 specifically activates HDAC1 in SH-SY5Y cells and exerts regulatory effects on aberrant cell cycle and DNA damage. HDAC1 activator-1 can be used for the research of TDP-43 proteinopat1-related neurodegenerative diseases including Amyotrophic Lateral Sclerosis (ALS) and cerebral ischemia-related neurological injury.
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