| DC65292 |
RK-582
Featured
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RK-582 is an orally efficacious spiroindolinone-based tankyrase inhibitor for the treatment of colon cancer. It exhibits a markedly improved robust tumor growth inhibition in a COLO-320DM mouse xenograft model when orally administered. |
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| DC65293 |
IACS-9439
Featured
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IACS-9439 is a potent, highly selective,and orally bioavailable CSF1R inhibitor. Treatment with IACS-9439 led to a dose-dependent reduction in macrophages,promoted macrophage polarization toward the M1 phenotype, and led to tumor growth inhibition in MC38 and PANC02 syngeneic tumor models. |
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| DC65294 |
MG-6267
Featured
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MG-6267 is the first dual inhibitor of AChE and microRNA-15b biogenesis, protecting SH-SY5Y neuroblastoma cells from amyloid-beta (Aβ)-induced cytotoxicity |
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| DC65295 |
SSK1
Featured
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SSK1 is a senolytic prodrug, which was designed from gemcitabine, by chem. modifying gemcitabin to incorporate a site cleavable by SA-β-gal following delivery of the prodrug in vivo, to release the active parent drug gemcitabine. SSK1 can be used to reduce one or more symptoms associated with a Senescence-associated disease or disorder in a subject. SSK1 is specifically activated by β-gal and eliminates mouse and human senescent cells independently of senescence inducers and cell types. In aged mice, SSK1 effectively cleared senescent cells in different tissues, decreased the senescence- and age-associated gene signatures, attenuated low-grade local and systemic inflammation, and restored physical function. |
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| DC65296 |
Ropsacitinib
Featured
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ropsacitinib, also known as PF-06826647 and Tyk2-IN-8, is an orally administered, tyrosine kinase 2 (TYK2) inhibitor, that is in development with Pfizer for the treatment of plaque psoriasis and inflammatory bowel disease. |
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| DC65297 |
OP-5244
Featured
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OP-5244 is a potent and orally bioavailable CD73 inhibitor. |
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| DC65298 |
Peptide5
Featured
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Peptide5 is a connexin43 mimetic peptide. Peptide5 reduces swelling, astrogliosis, neuroinflammation and neuronal cell death following spinal cord injury ex vivo and in vivo. Peptide5 exhibits analgesic effects in models of neuropathic pain. |
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| DC65299 |
SPR519
Featured
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SPR519 is a potent dual inhibitor of PI3Kα and mTOR kinases with IC50 (PI3Kalpha) = 30 nM and IC50 (mTOR) = 10 nM. SPR519 exhibits an EC50 of low sub-micromolar range among various tested cancer cell lines such as A2780 (0.23 μM), PC3 (0.48 μM), and SKOV3 (0.50 μM). |
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| DC65300 |
Lenacapavir(GS-6207)
Featured
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Lenacapavir, also known as GS-6207, is a HIV-1 capsid inhibitor. Lenacapavir shows anti-HIV activity. Lenacapavir displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs). Lenacapavir demonstrated picomolar potency in vitro with no cross resistance to existing antiretroviral classes and potent antiviral activity in persons with HIV-1. In persons with HIV-1, there was no preexisting resistance to lenacapavir regardless of treatment history. |
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| DC65301 |
C5-RIBOTAC
Featured
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C5-RIBOTAC is a RIBOTAC degrader, targeting the SARS-CoV-2 RNA genome |
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| DC65302 |
CG416
Featured
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CG416 is a tropomyosin receptor kinase (TRK) degrader that targets the intracellular kinase domain of TRK. CG416 reduced levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colorectal carcinoma cells and inhibited downstream PLCγ1 signaling at sub-nanomolar concentrations. CG416 also degraded human wild-type TRKA. |
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| DC65303 |
BI730357
Featured
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BI 730357 is a RORγ Antagonist for the treatment of autoimmune diseases. |
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| DC65304 |
PIPE-359
Featured
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PIPE-359 is a brain-penetrant and selective antagonist of the muscarinic acetylcholine receptor subtype 1. |
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| DC65305 |
KGN-00429
Featured
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KGN-00429 is a novel selective bromodomain and extra-terminal domain (BET) protein family inhibitor (BETi ), inducing an ‘activated’ keratinocyte transcriptional profile with reversal of chronic wound biomarkers in human skin ex vivo. This product has no formal name. For the convenience of scientific communication, we named it by combining its InChi Key (3 letters from the first letter of each section) with the last 5 digit of its CAS#) according to MedKoo Chemical Nomenclature (https://www.medkoo.com/page/naming). |
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| DC65306 |
DS79932728
Featured
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DS79932728 is a Potent, Orally Available G9a/GLP Inhibitor for Treating β‑Thalassemia and Sickle Cell Disease. |
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| DC65307 |
MI-09
Featured
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MI-09 is a SARS-CoV-2 Protease inhibitor (IC50 = 15.2 nM). In a transgenic mouse model of SARS-CoV-2 infection, oral or intraperitoneal treatment with MI-09 significantly reduced lung viral loads and lung lesions.
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| DC65308 |
Pleurotine
Featured
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| DC65310 |
SR-1114
Featured
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SR-1114 is a first-in-class ENL PROTAC. |
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| DC65311 |
SMU-C80
Featured
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SMU-C80 is a TLR2 agonist (EC50 = 31.02 ± 1.01 nM). SMU-C80, through TLR1/2, recruits the adaptor protein MyD88 and triggers the NF-κB pathway to release cytokines such as TNF-α and IL-1β from human, but not murine, cells. To the best of our knowledge, it is the first species-specific TLR1/2 agonist reported until now. Moreover, SMU-C80 increased the percentage of T, B, and NK cells ex vivo and activated the immune cells, which suppressed cancer cell growth in vitro. |
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| DC65312 |
Icenticaftor(QBW251)
Featured
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Icenticaftor, also known as QBW251 is a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease. |
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| DC65313 |
GSK743
Featured
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GSK743 is a Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitor. |
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| DC65314 |
SKLB-C2807
Featured
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SKLB-C2807 is an AR-DBD binder. |
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| DC65315 |
LC28
Featured
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LC28 is a novel inhibitor of STAT3 signaling, suppressing survival of cisplatin-resistant ovarian cancer cells. |
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| DC65316 |
MMPP
Featured
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MMPP is a novel potent inhibitor of pro-inflammatory responses by inhibiting in vitro STAT3 activation and its downstream signalling in murine macrophages and human synoviocytes from patients with RA. |
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| DC65317 |
VPC-70063
Featured
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VPC-70063 is a Myc-Max inhibitor. VPC-70067 is a close analog of the previously identified Myc inhibitor 10058-F4. VPC-70063, of a chemically different scaffold, was the best performer in a panel of in vitro assays, and the forerunner for future hit-to-lead optimization efforts. |
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| DC65318 |
IACS-9779
Featured
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IACS-9779 is a Potent IDO1 Inhibitor Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme. IACS-9779 with a predicted human efficacious once daily dose below 1 mg/kg to sustain >90% inhibition of IDO1 displayed an acceptable safety margin in rodent toxicology and dog cardiovascular studies to support advancement into preclinical safety evaluation for human development. |
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| DC72833 |
Muscarine
Featured
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Muscarine ((+)-Muscarine) is a toxin that can stimulate the parasympathetic nervous system. Muscarine is an agonist of muscarinic acetylcholine receptor (mAChR). |
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| DC72848 |
Leniolisib phosphate
Featured
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Leniolisib (CDZ173) phosphate is a potent and selective PI3Kδ inhibitor. Leniolisib phosphate has the potential for immunodeficiency disorders treatment. |
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| DC72862 |
Formamide
Featured
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Formamide (Methanamide; Formimidic acid) is a clear liquid amide derived from formic acid. It allows for the denaturation and renaturation of nucleic acids at room temperature. Formamide-induced DNA denaturation when combined with detection of denatured DNA with a monoclonal antibody (MAb) makes it possible to specifically identify the apoptotic cells. |
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| DC72871 |
FHP01
Featured
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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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