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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC23789 AK778 Featured
AK778 (Col001) is a small-molecule compound that inhibits the interaction of Hsp47 with collagen, competitively inhibits the interaction and causes the inhibition of collagen secretion by destabilizing the collagen triple helix. .
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DC20439 LXRβ agonist 17 Featured
LXRβ agonist 17 is a novel, potent, orally active liver X receptor β (LXRβ) agonist with Ki/EC50 of 3/21 nM, displays 27-fold selectivity over LXRα; also exhibits excellent selectivity against other nuclear hormone receptors (>3,000-fold); induces the expression of LXR target genes in vitro and in vivo.
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DC58042 MRTX-282 Featured
MRTX-282 is a novel KRas G12D inhibitor.
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DC60042 YKP-3089 Featured
Cenobamate, a sodium channel blocker, enhances GABAergic transmission and has the potential to be a versatile CNS drug.
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DC11386 NNZ-2591 Featured
NNZ2591 (cyclo-L-glycyl-L-2-allylproline)1 is an investigational synthetic analog of cyclic glycine-proline (cGP), a breakdown product of human insulin-like growth factor 1 (IGF-1), that has been chemically modified to increase its half-life, stability, and oral bioavailability.
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DC70599 miR-21 inhibitor 12 Featured
miR-21 inhibitor 12 (miR-21-IN-12) is a small molecule inhibitor of microRNA-21 expression and inhibit miR-21 transcription.miR-21-IN-12 inhibited transcription of the miR-21 gene resulting in significant reductions in primary and mature miR-21 levels.miR-21-IN-12 demonstrated cytotoxicity in a cervical cancer cell line via induction of apoptosis and was capable of reducing microtumor formation in a long-term clonogenic assay.miR-21-IN-12 shows some level of selectivity for miR-21 and is not a general miRNA pathway inhibitor.
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DC70374 DYRK2 inhibitor C17 Featured
DYRK2 inhibitor C17 is a potent, selective DYRK2 inhibitor with IC50 of 9 nM, weakly inhibits DYRK3 (IC50=68 nM), and does not inhibit DYRK1A/1B (IC50>2000 nM).C17 showed outstanding selectivity for the human kinome containing 467 other human kinases.C17 showed synergistic 4E-BP1 phosphorylation suppression combined with AKT and MEK inhibitors.C17 impeded the store-operated calcium entry process (ORAI1 channel).
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DC74365 RMC-4998 Featured
RMC-4998 (RMC4998) is a tricomplex inhibitor that targets the active state or GTP-bound state of KRAS G12C, selectively inhibits the proliferation of KRASG12C mutant cells with mean IC50 of 0.28 nM.
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DC70783 SJ432 Featured
SJ432 (SJ-432) is a potent, highly selective BET BD2 inhibitor with Kd of 6/2 nM (BRD2-BD2/BRD4-BD2), displays 80/152-fold selectivity over BD1, respectively.SJ432 is more water soluble than SJ018 (40 uM vs <0.1 uM).SJ432 potently inhibits MV4-11 cell growth with GI50 of 8 nM, is more effective than JQ1 at reducing levels of MYC protein in NB cell lines, upregulated p21& GADD45H and downregulated CCND2 & ODC1, C-MYC target genes.SJ432 (15 mg/kg, i.p.) significantluy reduced tumor volumes in pediatric NB xenograft SK-N-AS, with essentially no loss in body weight.
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DC60191 Tenofovir Alafenamide Impurity 1 Featured
DC46349 ALS-I Featured
ALS-I, an acid-Liable surfactant, is adopted for in-solution enzymatic digestions, can help to solubilize hydrophobic proteins. ALS-I is significantly enhanced peptide recovery for mass spectrometry (MS) mapping in the study of the proteomes of regenerating rat retina and mouse brain.
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DC7806 Geldanamycin (NSC122750)
Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.
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DC70805 SSCI-2 Featured
SSCI-2 is a highly potent, selective NaV1.7 inhibitor with IC50 of 9 and 17 nM on human and rhesus Nav1.7 channels, respectively.SSCI-2 showed robust selectivity over other human and rhesus Nav channel paralogs, with the exception of Nav1.2 channels (IC50 183 nM for hNaV1.2), shows no other channels and receptors in 114 enzymatic, radioligand binding, and cellular assays.SSCI-2 also exhibits high potency in manual patch clamp experiments (IC50=24/62 nM for huma/rhesus Nav1.7 channels).SSCI-2 inhibits withdrawal responses to noxious heat in rhesus monkeys.
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DCC1706 Dd04107 Featured
Novel inhibitor of α-calcitonin gene-related peptide (α-CGRP) exocytotic release from primary sensory neurons, selectively interacting with Synaptotagmin 1
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DC46061 Antioxidant 1024 Featured
Antioxidant 1024 (MD 1024) is an antioxidant agent and metal deactivator.
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DC73981 DS68591889
DS68591889 (PTDSS1i) is a potent, selective phosphatidylserine synthase 1 (PTDSS1) inhibitor, highly sellective over PTDSS2, induces phospholipid imbalance in a wide range of cancer cells.
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DC20603 (5Z)-7-Oxozeaenol
(5Z)-7-Oxozeaenol is a potent and selective TAK1 inhibitor with IC50 of 8 nM, displays >33-fold and >62-fold selectivity over MEKK1 and MEKK4 respectively.
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DC49692 T-Type calcium channel inhibitor(TTA-P2) Featured
T-Type calcium channel inhibitor is a potent inhibitor of T-Type calcium channel. T-Type calcium channel inhibitor penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. T-Type calcium channel inhibitor has the potential for the research of neurology disease.
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DC22732 RU1968 Featured
RU1968 is a potent, cross-species sperm-specific Ca2+ channel CatSper inhibitor that is selective for CatSper over Slo3.
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DC73675 VU0546110 Featured
VU0546110 (VU 0546110) is a potent, selective inhibitor of the sperm-specific potassium channel SLO3 with IC50 of 1.29 uM, impairs sperm function.
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DC72326 Tabernanthalog Featured
Tabernanthalog is a water-soluble, non-hallucinogenic and non-toxic analogue of ibogaine. Tabernanthalog is a 5-HT2A agonist. Tabernanthalog is found to promote structural neural plasticity, reduce alcohol- and heroin-seeking behaviour, and produce antidepressant-like effects in rodents.
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DC22517 Exendin-4 acetate Featured
Exenatide acetate (Exendin-4 acetate) is the acetate of Exenatide, which is highly potent, long-acting glucagon-like peptide-1 receptor (GLP-1) agonist with IC50 of 3.22 nM..
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DC23916 Human growth hormone-releasing factor Featured
Human growth hormone-releasing factor stimulates GH production and release by binding to the GHRH Receptor (GHRHR) on cells in the anterior pituitary.
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DC42795 6R-FR054 Featured
6R-FR054 is a 6R-isomer of FR054. FR054 is an inhibitor of the Hexosamine Biosynthetic Pathway (HBP) enzyme PGM3, with a remarkable anti-breast cancer effect.
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DC82103 Ensifentrine Featured
Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research[1][2].
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DC72935 JSF-2414 Featured
JSF-2414 (JSF2414) is a potent, small molecule GyrB/ParE dual binding inhibitor, simultaneously binds to ATP binding regions of DNA gyrase (GyrB) and topoisomerase (ParE) and displays potent in vitro activity against strains of MRSA, VRSA and VISA.
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DC73421 ASP4345 Featured
ASP4345 (ASP-4345) is a potent, selective positive allosteric modulator of the dopamine type 1 (D1) receptor that selectively binds to, and enhances the activity of, D1 receptors.
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DC66546 R-Sirpiglenastat Featured
R-Sirpiglenastat is the R- isomer of Sirpiglenastat(DRP-104).Sirpiglenastat (DRP104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.
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DC73189 H3B-960 Featured
H3B-960 is a potent, selective and covalent inhibitor of Werner syndrome protein (WRN) helicase activity with IC50 of 60 nM.
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DC20316 Bantag-1 trifluoroacetate Featured
A potent, highly selective, peptide bombesin receptor subtype-3 (BRS-3) antagonist with IC50 of 2-8 nM for human and rodent BRS-3, displays 1000-fold selectivity over hNMBR and hGRPR, increases food intake and produces an obesity phenotype in mice..
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