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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC74642 Mtb ATP synthase-IN-1
Mtb ATP synthase-IN-1 is a potent Mycobacterium tuberculosis (Mtb) ATP synthase inhibitor, with MIC of 0.452-0.499 μg/mL against Mtb.
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DC74636 Bromo-PADAP
Bromo-PADAP is a dye agent for research use. Bromo-PADAP was reported for the spectrophotometric determination of uranium(VI). Bromo-PADAP is highly sensitive towards uranium, the uranyl complex having a molar absorptivity of 74,000 at 578 nm and pH 7.6. In the presence of a mixed masking solution only a few ions interfere seriously, and the method can be made specific for uranium by a preliminary extraction of uranium into tri-n-octylphosphine oxide, and direct development of the bromo-PADAP colour in the organic phase. Details are given for the determination of uranium in waters, ores, phosphoric acid and phosphate rocks, thorium oxide, and zirconium oxide.
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DC74635 ATH434 mesylate
ATH434, also known as PBT434, is a novel, brain-penetrant, inhibitor of α-synuclein aggregation. In transgenic animal models of Parkinson disease (A53T) and MSA (PLP-α-Syn), PBT434 reduced α-synuclein aggregation, preserved neurons and improved motor function. Glial cell inclusions were also reduced in a murine MSA model. PBT434 is thought to act by redistributing reactive iron across membranes, thereby blocking intracellular protein aggregation and oxidative stress. The affinity of PBT434 for iron is greater than that of α-synuclein but lower than that of iron trafficking proteins, e.g., ferritin.
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DC74633 TCMDC-137332
TCMDC-137332 is a compound that exhibits antimalarial activity against Plasmodium falciparum with an IC50 value of 7 nM.
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DC74632 Dimethylamiloride
Dimethylamiloride is a Na(+)-H+ exchange inhibitor.
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DC74631 JAK-IN-21
JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor.
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DC74630 Antiviral agent 17
Antiviral agent 17 is an anti-infection agent.
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DC12262 H-Val-Pro-Pro-OH TFA Featured
H-Val-Pro-Pro-OH (TFA) is a trifluoroacetate (TFA) salt form of the tripeptide H-Val-Pro-Pro-OH, which is derived from milk proteins. This peptide is known for its ability to inhibit Angiotensin I Converting Enzyme (ACE), a key enzyme in the renin-angiotensin system (RAS) that regulates blood pressure. The TFA salt form is commonly used in research and pharmaceutical applications to improve the solubility and stability of the peptide.
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DC20081 H-Val-Pro-Pro-OH Featured
H-Val-Pro-Pro-OH is a tripeptide derived from milk proteins, specifically a proline-rich peptide, and is known for its inhibitory activity against Angiotensin I Converting Enzyme (ACE). ACE is a key enzyme in the renin-angiotensin system (RAS), which regulates blood pressure by converting angiotensin I to angiotensin II, a potent vasoconstrictor. Inhibition of ACE leads to reduced angiotensin II levels, resulting in vasodilation and lowered blood pressure.
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DC9482 17-AAG Featured
17-AAG (17-N-Allylamino-17-demethoxygeldanamycin), also known by its NSC number 330507 and CP number 127374, is a well-studied inhibitor of Heat Shock Protein 90 (HSP90). HSP90 is a molecular chaperone that plays a critical role in the stabilization and activation of a wide range of client proteins, many of which are involved in oncogenic processes. By inhibiting HSP90, 17-AAG disrupts the function of these client proteins, leading to the degradation of oncogenic proteins and ultimately inhibiting cancer cell growth and survival.
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DC72871 FHP01 Featured
FHP01 (BA103) is a potent, small molecule inhibitor of DDX3X helicase activity with IC50 of 0.3 uM in in vitro enzyme assays, exhibits very effective antiproliferative and killing activity against different breast cancer cell types (IC50=3.058 and 3.21 μM in MDA MB 468 and MDA MB 231, respectively). FHP01 does not inhibit the ATPase activity of DDX3X and the helicase activity of DDX1 (IC50>100 uM). FHP01 also inhibited WNT signaling, a key tumorigenic pathway already correlated to DDX3X functions in breast cancer model cell lines. FHP01 inhibits ER+/PR+ (IC50 = 12.43 and 10.62 μM in MCF7 and T47D cells, respectively) and HER2+ (IC50 = 13.46 μM in SKBR3) cells, but lower in control MCF10A cells (IC50 = 28.71 μM). FHP01 (45 mg/kg, i.p. injection) suppresses rowth of MDA MB 231 tumor xenografts in nude mice.
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DC72877 PF-114 Featured
Vamotinib (PF-114) is a potent, selective and orally available inhibitor of native (IC50=0.49 nM) and mutated BCR/ABL (IC50=0.7-4 nM, ABL (T315I) IC50=0.78 nM). PF-114 potently inhibits ABL2, DDR1, DDR2, FMS, FRK, LCK, LYN and PDGFR kinases, but did not inhibit c-SRC, CSK, or c-KIT.
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DC70908 Xeruborbactam
Xeruborbactam (QPX7728) is an ultrabroad-spectrum beta-lactamase inhibitor with remarkable activity against a wide range of beta-lactamases, including those that are typically resistant to other inhibitors.
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DC74017 HTL0041178 Featured
HTL0041178 is a potent GPR52 agonist with EC50 of 27.5 nM (human or rat GPR52).
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DC22392 BRD-4592 Featured
BRD4592 is a small-molecule allosteric inhibitor that targets the tryptophan synthase (TrpAB) of Mycobacterium tuberculosis. TrpAB is a bifunctional enzyme composed of α and β subunits, which catalyzes the final steps of tryptophan biosynthesis. BRD4592 binds at the interface of the α and β subunits, disrupting the enzyme's function.
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DC47030 Ilunocitinib Featured
Ilunocitinib (compound 27) is a JAK inhibitor (extracted from patent WO2009114512A1).
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DC23181 (R)-GNE-140 Featured
(R)-GNE-140 (GNE-140) is a novel potent, selective lactate dehydrogenase (LDH) inhibitor with IC50 of 3, 5, and 5 nM for LDHA, LDHB, and LDHC, respectively.
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DC8746 NSC319726 Featured
NSC319726 is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.
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DCC1260 CBL0137 hydrochloride Featured
CBL0137 (CBL-0137) activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex).
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DC70728 RA608 Featured
RA608 (RA-608) is a potent, selective, ATP-competitive, orally available CaMKII inhibitor, inhibits human CaMKIIδ, CaMKIIγ, CaMKIIα, and CaMKIIβ with IC50 of 22, 51, 121, and 1135 nM, respectively.RA608 displays a good selectivity profile against a broad panel of 304 human recombinant kinases.RA608 significantly reduces SR Ca leak in human atrial cardiomyocytes, reduces diastolic tension of human atrial trabeculae, does not affect action potential characteristics; attenuates heart failure in the murine HF model induced by TAC.
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DC70444 GS-680 Featured
GS-680 (GS680) is a novel selective and ATP-competitive CaMKII inhibitor with biochemical IC50 of 2.3 and 15.9 nM against CaMKIIδ and CaMKIIα, respectively.GS-680 inhibited phospholamban phosphorylation in NRVM with an EC50 of 98.9 nM.GS-680 inhibits premature atrial contractions.GS-680 significantly reduced CaMKII autophosphorylation.GS-680 inhibits pro-arrhythmic activity in human atrium and improves contractility in failing human ventricle.
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DC74339 HRX-0233 Featured
HRX-0233 (HRX0233) is a potent and selective inhibitor of MAP2K4 (MKK4), a kinase involved in the stress-activated protein kinase (SAPK) signaling pathway. MAP2K4 plays a role in regulating cellular responses to stress, apoptosis, and tumorigenesis. HRX-0233 has shown particular promise in KRAS-mutant cancers, where it exhibits synergistic effects with RAS inhibitors, making it a potential candidate for combination therapy in these difficult-to-treat cancers.
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DCC5498 Biricodar(Vx-710) Featured
Biricodar (VX-710) is a multidrug resistance (MDR) modulator that targets two key drug efflux transporters: P-glycoprotein (Pgp) and multidrug resistance-associated protein 1 (MRP-1). These transporters are often overexpressed in cancer cells and contribute to multidrug resistance (MDR) by pumping chemotherapeutic drugs out of the cells, reducing their intracellular concentration and efficacy. Biricodar inhibits the function of Pgp and MRP-1, effectively chemosensitizing multidrug-resistant cancer cells and enhancing the effectiveness of chemotherapy agents. Its ability to reverse MDR makes it a promising candidate for improving cancer treatment outcomes.
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DC21257 LY2780301 Featured
The compound you are referring to is likely a dual inhibitor of p70S6K (S6K1) and Akt, two critical kinases in the PI3K/Akt/mTOR signaling pathway. This pathway is a central regulator of cell growth, proliferation, survival, and metabolism, and its dysregulation is frequently observed in cancers, including solid tumors and non-Hodgkin's lymphoma (NHL). A dual inhibitor targeting both p70S6K and Akt would offer a powerful therapeutic strategy to block this pathway at multiple nodes, potentially overcoming resistance mechanisms and improving treatment outcomes.
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DC42604 IFN-α/IFNAR-IN-1 hydrochloride Featured
IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor that specifically targets the interaction between interferon-alpha (IFN-α) and its receptor, interferon-alpha/beta receptor (IFNAR). This interaction is critical for initiating IFN-α signaling, which plays a key role in antiviral and immune responses. By blocking this interaction, IFN alpha-IFNAR-IN-1 hydrochloride inhibits IFN-α signaling and downstream responses, making it a valuable tool for studying IFN-α biology and its role in diseases such as autoimmune disorders and viral infections. It has demonstrated efficacy in inhibiting modified Vaccinia virus Ankara (MVA)-induced IFN-α responses in murine bone-marrow-derived, Flt3-L-differentiated plasmacytoid dendritic cell (pDC) cultures (BM-pDCs) with an IC50 of 2-8 µM.
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DC43400 Reversan Featured
Reversan (CBLC4H10) is a potent and nontoxic inhibitor of two major drug efflux transporters: multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp). These transporters are key players in multidrug resistance (MDR), a major obstacle in cancer chemotherapy, as they pump chemotherapeutic drugs out of cancer cells, reducing their intracellular concentration and efficacy. By inhibiting MRP1 and Pgp, Reversan can reverse drug resistance and enhance the effectiveness of chemotherapy agents. Its nontoxic profile makes it a promising candidate for overcoming MDR in cancer treatment.
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DC72592 Zelasudil Featured
Zelasudil is a Rho-associated coiled-coil kinase (ROCK) inhibitor with a specific binding affinity for ROCK2, a key enzyme in the Rho/ROCK signaling pathway. This pathway plays a critical role in regulating cellular processes such as cytoskeletal organization, cell motility, smooth muscle contraction, and gene expression. By selectively inhibiting ROCK2, Zelasudil modulates these processes, offering therapeutic potential for a variety of diseases characterized by fibrosis, inflammation, and vascular dysfunction, including pulmonary fibrosis, glaucoma, and cardiovascular diseases.
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DC21530 CMP-5 Featured
CMP-5 (PRMT5-IN-5) is a first-in-class, small-molecule inhibitor that specifically targets protein arginine methyltransferase 5 (PRMT5), an enzyme involved in epigenetic regulation and cellular signaling. PRMT5 catalyzes the symmetric dimethylation of arginine residues on histones and other proteins, playing a critical role in gene expression, cell proliferation, and survival. CMP-5 has shown remarkable specificity in blocking Epstein-Barr virus (EBV)-driven B-lymphocyte transformation and survival, while sparing normal B cells, making it a promising therapeutic candidate for EBV-associated cancers and other PRMT5-dependent diseases.
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DCC0970 Bi-1750 Featured
BI-1750 is a highly selective and stable fluorogenic substrate designed for Cathepsin C (CatC), a lysosomal cysteine protease involved in various physiological and pathological processes. Its unique properties make it a powerful tool for studying CatC activity in both research and drug development contexts.
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DC43898 CN009543V Featured
The statement suggests that CN009543V enhances tyrosine phosphorylation of the epidermal growth factor receptor (EGFR) through downstream signaling pathways.
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