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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC78664 NRG1271
NRG1271 is an orally active mitochondrial permeability transition pore (mPTP) inhibitor with blood-brain barrier penetration. NRG1271 can be used for the study of Neurological Disease.
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DC78663 AZD3839 fumarate
AZD3839 (fumarate) is an orally available, selective, reversible inhibitor of the β-site amyloid precursor protein cleaving enzyme BACE1 that can cross the blood-brain barrier. AZD3839 (fumarate) inhibits recombinant human BACE1 with a Ki=26.1 nM. AZD3839 (fumarate) inhibits A40 production in SH-SY5Y cells with an IC50 of 4.8 nM. AZD3839 (fumarate) binds to BACE1 and reduces the Aβ amyloid produced by the cleavage of amyloid precursor protein (APP) by BACE1 and γ-secretase. AZD3839 (fumarate) can be used in the field of Alzheimer's disease research.
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DC78662 R 1485 dihydrochloride
R 1485 is a 5-HT6 receptor antagonist.
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DC78661 LP-65
LP-65 is a dual inhibitor of MEK (IC50=83.2 nM) and mTOR (IC50=40.5 nM). LP-65 blocks MEK and mTOR signaling pathways and inhibits tumor cell proliferation and migration. LP-65 is promising for research of cancers.
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DC78660 HW091077
HW091077 is a highly selective P2X3 receptor antagonist with an IC50 of 17 nM. HW091077 blocks ATP-induced calcium influx and cell depolarization to inhibit cough reflex pathways. HW091077 is promising for research of chronic cough.
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DC78659 E3 ligase Ligand 75
E3 ligase Ligand 75 is an E3 ligase ligand. E3 ligase Ligand 75 can be used for synthesis PROTAC K-Ras Degrader-7.
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DC78658 Padoprazanum fumarate
Padoprazanum (Padoprazan) fumarate is a Proton Pump inhibitor.
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DC78657 Padoprazanum hydrochloride
Padoprazanum (Padoprazan) hydrochloride is a Proton Pump inhibitor.
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DC78656 Cleminorexton
Cleminorexton (Compound 67A) is an agonist of orexin-2 receptor (OX2R). Cleminorexton can be studied in research for narcolepsy and other disorders related to orexin insufficiency and/or excessive sleepness.
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DC78655 ARN21929
ARN21929 is a Topoisomerase II inhibitor with an IC50 of 4.5 μM. ARN21929 exhibits excellent kinetic and thermodynamic solubility as well as metabolic stability. However, ARN21929 shows poor antiproliferative activity against A549, DU145, MCF7, HeLa, and A375 cells. ARN21929 can be used in the study of cancer.
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DC78654 MARY1
MARY1 is a selective 5-HT2BR antagonist with an IC50 of 380 nM and a Ki of 764 nM (human 5-HT2BR). MARY1 induces renal mitochondrial biogenesis (MB) and enhances renal mitochondrial function by increasing mitochondrial respiratory capacity, mitochondrial protein levels, and mitochondrial number in renal proximal tubular cells (RPTCs). MARY1 induces MB through 5-HT2BR and dual PI3K/AKT and RAS/MEK/ERK cell signaling pathways in RPTCs. MARY1 can be used to study renal diseases associated with metabolic and mitochondrial dysfunction.
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DC78653 Androgen receptor ligand 1
Androgen receptor ligand 1 is an androgen receptor (AR) ligand. Androgen receptor ligand 1 binds to CRBN E3 ligase via a linker to form an AR PROTAC degrader. Androgen receptor ligand 1 can be used in the study of prostate cancer.
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DC78652 (S)-AZD0022
(S)-AZD0022 is an isomer of AZD0022, AZD0022 is a selective and orally active KRASG12D inhibitor. AZD0022 inhibits KRAS pathway suppression in the GP2D xenograft model.
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DC78651 N-Succinimidyl 3-maleimidopropionate
N-Succinimidyl 3-maleimidopropionate (Compound MC1) is a Glucuronide-Gemcitabine conjugate. N-Succinimidyl 3-maleimidopropionate can be used to synthesize ADCs (such as cAc10ec-MC1). N-Succinimidyl 3-maleimidopropionate can be used in Hodgkin's lymphoma research.
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DC78650 NVP-BQS481
NVP-BQS481 (Compound 1) is a selective Kinesin spindle protein-5 (Eg5) inhibitor with an IC50< 0.5 nM. NVP-BQS481 has significant antimitotic and antitumor activity (IC50: 0.0.9 nM for SK-OV-3ip cells). NVP-BQS481 can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs).
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DC78649 Davalomilast
Davalomilast (Example 100) is an PDE4 inhibitor with anti-inflammatory property. Davalomilast can be studied in research for autoimmune diseases and dermatology research.
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DC78648 SM311
SM311 (Compound 10), a chemical probe, is a potent selective irreversible LIMK1 inhibitor (EC50=0.045 μM, >30-fold selective over LIMK2). SM311 blocks cofilin phosphorylation and actin cytoskeleton regulation. SM311 is promising for research of neurodegenerative diseases like Fragile X syndrome (FXS) and Alzheimer’s disease, as well as tumor invasion.
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DC78647 X-370
X-370 is a PI3Kδ inhibitor (IC50 = 7 nM). X-370 inhibits the survival of leukemia cells, inducing G1 arrest and apoptosis. X-370 blocks PDK1 binding and phosphorylation of MEK1/2, eliminating Akt and Erk1/2 signaling. X-370 can be used in research on B-cell acute lymphoblastic leukemia (B-ALL).
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DC78646 CP-800569
CP-800569 is an orally active cholesteryl ester transfer protein (CETP) inhibitor. CP-800569 can decrease low-density lipoprotein and postprandial triglyceride and increase high-density lipoprotein. CP-800569 can be used for the research of metabolic disease.
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DC78645 Davotifan
Davotifan (Compound A17) is a bicyclic compound. Davotifan is an inhibitor of HIF-2α. Davotifan can be studied in research for HIF-2α-related cancer.
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DC78644 Comtifator
Comtifator (Example 77) is a modulator of the integrated stress response pathway. Comtifator can be studied in research for diseases associated with integrated stress response.
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DC78643 SB-219994
SB-219994 is a peroxisome proliferator-activated receptors (PPARs) agonists. SB-219994 can inhibit airway neutrophilia and associated chemoattractants/survival factors. SB-219994 exhibits anti-inflammation effec.
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DC78642 17β-HSD5 inhibitor 2
17β-HSD5 inhibitor 2 (Compound 30) is an inhibitor for 17β-hydroxysteroid dehydrogenases 5 (17β-HSD 5) with IC50 of 40 nM.
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DC78641 BTX-6654 formate
BTX-6654 (formate) is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 (formate) reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations.
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DC78640 BRL-52656
BRL-52656 is a blood-brain barrier (BBB)-penetrable KOR receptor agonist that exhibits a biphasic effect. At low doses, BRL-52656 decreases blood pressure, whereas high doses have the opposite effect in spontaneously hypertensive rats. Additionally, BRL-52656 induces water diuresis by inhibiting the secretion of vasopressin (AVP).
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DC78639 CJ-17493
CJ-17493 is a neurokinin-1 (NK1) receptor antagonist, with a Ki of 0.2 nM. CJ-17493 shows moderate affinity for the verapamil-binding site of L-type Ca2+ channels (IC50 = 164 nM) and site 2 of sodium channels (IC50 = 48 nM). CJ-17493 can be used for the study of neurological diseases.
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DC78638 AR ligand 42
AR ligand 42 is a androgen receptor ligand. AR ligand 42 can be used to synthesize androgen receptor PROTAC degrader ITRI-90.
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DC78637 TFSeB
TFSeB is an orally active neuroprotective agent. TFSeB can reduce Streptozotocin (STZ)-induced MAO-B and AChE activity. TFSeB exerts neuroprotective effects by increasing the expression of BCL-2, BDNF, NRF2, and decreasing the expression of BAX. TFSeB can reduce lipid peroxidation (TBARS) and reactive oxygen species (ROS) levels. TFSeB can reduce neuroinflammation. TFSeB can be used for research on Alzheimer’s disease.
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DC78636 Gemigliptin hydrochloride
Gemigliptin (hydrochloride) is the hydrochloride salt of Gemigliptin. Gemigliptin (hydrochloride) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin (hydrochloride) exhibits potent anti-glycation properties. Gemigliptin (hydrochloride) can be used for the research of advanced glycation end products (AGE)-related diabetic complications.
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DC78635 Modzatinib
Modzatinib (ITK kinase-IN-1) (compound I) is an inhibitor targeting ITK kinase (IC50=8 nM, Jurkat cells) and can be used to study inflammatory diseases. Modzatinib has an IC50 of 23 nM for JAK3 in hPBMC cells (based on IL-2/pSTAT5 levels), wihout inhibitory effect against JAK2.
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