| DC50007 |
Etoposide
Featured
|
>98%,Standard References |
|
| DC50008 |
Colchicine
Featured
|
Colchicine is a potent therapeutic tool against COVID-19. Colchicine is a tricyclic alkaloid that is extracted from the plant Colchicum autumnale. Colchicine acts as a potent inhibitor of tubulin polymerization. |
|
| DC50010 |
ICCB280
Featured
|
ICCB280 is a potent inducer of C/EBPα. ICCB280 exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis through activation of C/EBPα and affecting its downstream targets (such as C/EBPε, G-CSFR and c-Myc). |
|
| DC50011 |
CCCP
Featured
|
CCCP is an oxidative phosphorylation (OXPHOS) uncoupler. CCCP induces activation of PINK1 leading to Parkin Ser65 phosphorylation. |
|
| DC50012 |
TLR7/8 agonist 1 dihydrochloride
Featured
|
TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline. |
|
| DC50013 |
BC1618
Featured
|
BC1618 is a novel Fbxo48 inhibitor and prevent pAmpkα degradation with MEC (minimal efficacious concentration) of 0.6 μM. |
|
| DC50020 |
Pirtobrutinib (LOXO-305)
Featured
|
LOXO-305 is an investigational, novel, selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. LOXO-305 was designed to reversibly bind BTK, preserve activity in the presence of the acquired resistance, and avoid off-target kinases that have complicated the development of both covalent and investigational non-covalent BTK inhibitors.LOXO-305 is a highly selective, non-covalent BTKi that inhibits both wild type (WT) and C481-mutated BTK with equal low nM potency was developed. |
|
| DC50021 |
JMX0493
Featured
|
JMX0493 is a potent inhibitor of human adenoviruses (HAdVs) with IC50 of 0.78 μM and displays high selectivity index (SI>100) and 2.5-fold virus yield reduction compared to niclosamide. JMX0493 targets the HAdV entry pathway that prevents viral particle disassembly and subsequent release from the endosome. |
|
| DC50022 |
ACH-000143
Featured
|
ACH-000143 is a novel potent melatonin receptor agonist with EC50 of 0.06 nM/0.32 nM against MT1/MT2. ACH-000143 leads to a reduction in body weight gain similar to dapagliflozin with superior results on hepatic steatosis and triglyceride levels in high-fat diet rats. |
|
| DC50023 |
Compound 5i
Featured
|
Compound 5i is a novel and brain-penetrant O-GlcNAcase inhibitor with IC50 of 46 nM. |
|
| DC50025 |
Deruxtecan
Featured
|
Deruxtecan, a topoisomerase I inhibitor, is an exatecan derivative (DX-8951 derivative) with a cleavable pepetide linker and a maleimide group. The maleimide group in Deruxtecan can react with antibody to form antibody-drug conguates (ADC) such as Trastuzumab deruxtecan (DS-8201a), which is a HER2-targeting antibody–drug conjugate. |
|
| DC50026 |
GSK-114
Featured
|
GSK-114 is a potent and selective selective TNNI3K inhibitor (TNNI3 IC50 = 25nM; B-RafV600E IC50 = 1000 nM). GSK-114 displays significant bias (40-fold) for TNNI3K over B-Raf, exceptional broad spectrum kinase selectivity, and adequate oral exposure to en |
|
| DC50027 |
ENMD-2076 L-(+)-Tartaric acid
Featured
|
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively. |
|
| DC50028 |
Laninamivir Octanoate
Featured
|
Laninamivir (L174000) prodrug; a novel long-acting neuraminidase inhibitor. |
|
| DC50030 |
GRL-1720
Featured
|
GRL-1720 is an irreversible, covalent inhibitor of SARS-CoV-2 main protease (Mpro) with EC50 of 15 µM. |
|
| DC50032 |
CU-CPT17e
Featured
|
CU-CPT17e shows strong NF-κB activation in TLR3, TLR8 and TLR9 HEK293 cells with EC50 values of 4.80±0.73, 13.5±0.58 and 5.66±0.17 μM, respectively. CU-CPT17e significantly improves the activity with 13.9±0.9 fold of NF-κB activation and an EC50 value of 4.8±0.7 μM. CU-CPT17e inhibits the proliferation of HeLa cancer cells by triggering apoptosis and arresting the cell cycle at the S phase. The induction of apoptosis by CU-CPT17e in HeLa cells is investigated. HeLa cells are cultured with increasing concentrations of CU-CPT17e or poly I:C or blank control (DMSO) for 24 h. Treatment with CU-CPT17e for 24 h at different concentrations (10 to 40 μM) results in an elevation of apoptotic cell population ranging from 10% to 17%, which is more effective than poly I:C at 5 μg/mL. These results suggest that the antiproliferative activity of CU-CPT17e against HeLa cells might result from its ability to directly induce apoptosis[1]. |
|
| DC50035 |
PF00835231
Featured
|
PF00835231(SARS-CoV-2 inhibitor 5h) is areversible-covalent inhibitor of SARS-CoV-2 main protease (Mpro) with EC50 of 4.2 µM. Compound 5h blocks the infectivity and cytopathicity of the virus with high potency and without any detectable cytotoxicity even at 200 µM.PF-00835231 is a potent inhibitor of CoV-2 3CLpro with IC50 of 4 nM and shows suitable pharmaceutical properties to warrant further development as an intravenous treatment for COVID-19. |
|
| DC50036 |
RAD-150
Featured
|
RAD150 is a nonsteroidal androgen receptor modulator (IC50 = 130 nM) and benzoate ester derivative of the selective androgen receptor modulator (SARM) RAD140. |
|
| DC50038 |
PROTAC SGK3 degrader-1
Featured
|
PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on PROTAC. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate). |
|
| DC50039 |
3'3'-cGAMP (sodium salt)
Featured
|
3’3’-cGAMP Fluorinated (c-[2'FdGMP]-[2'FdAMP]) is a synthetic analog of cyclic guanosine monophosphate- adenosine monophosphate (cyclic GMP-AMP, cGAMP) with a fluorine atom at 2’ position of the nucleosides. 3’3’-cGAMP is a cyclic di-nucleotide produced by bacteria. It is also referred to as "canonical" cGAMP due the presence of the classical 3’-5’ phosphodiester linkages between the guanosine and the adenosine. It has been reported that cGAMP binds STING (stimulator of IFN genes) and subsequently induces TBK1-IRF3-dependent production of IFN-β [1].
The incorporation of fluorine into biologically active molecules is commonly used in medicinal chemistry to improve their metabolic stability or to modulate physicochemical properties such as lipophilicity [2, 3]. Moreover, the introduction of a fluorine atom can change the biological activities of a molecule. Interestingly, when used at low concentrations in various cellular assays, 3’3’-cGAMP Fluorinated induces higher levels of type I IFNs than does cGAMP.
STING ligands such as cGAMP induce type I IFNs and activate interferon stimulated genes (ISG) through IRFs. To facilitate their study, InvivoGen has developed stable reporter cells in two well established immune cell models: THP-1 human monocytes and RAW 264.7 murine macrophages. These cells express a reporter gene (SEAP or Lucia luciferase), under control of an IRF-inducible promoter. |
|
| DC50040 |
GNF-PF-3777 (8-Nitrotryptanthrin)
Featured
|
GNF-PF-3777 (8-Nitrotryptanthrin) is a potent human indoleamine 2,3-dioxygenase 2 (hIDO2) inhibitor which significantly reduces IDO2 activity with Ki of 0.97 μM. |
|
| DC50051 |
Emavusertib(CA-4948)
Featured
|
CA-4948 is a potent IRAK4/FLT3 inhibtor with anti-tumor activity[1].CA-4948 is over 500-fold more selective for IRAK-4 compared to IRAK-1. CA-4948 reduces TNF-α, IL-1β, IL-6 and IL-8 release from TLR-Stimulated THP-1 Cells with an IC50 <250 nM. CA-4948 al |
|
| DC50052 |
9-(2-Deoxy-2-fluoroarabinofuranosyl)guanine
Featured
|
9-(2-Deoxy-2-fluoroarabinofuranosyl)guanine|2'-FANA-G |
|
| DC50053 |
E3 Ligase Ligand-Linker Conjugates 20
Featured
|
Thalidomide-O-amido-C8-NH2 (Cereblon Ligand-Linker Conjugates 2), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs. |
|
| DC50055 |
Thalidomide-NH-C6-NH2
Featured
|
Thalidomide-NH-C6-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology. |
|
| DC50056 |
Thalidomide-PEG2-C2-NH2
Featured
|
Thalidomide-PEG2-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology. |
|
| DC50057 |
E3 ligase Ligand-Linker Conjugates 30
Featured
|
E3 ligase Ligand-Linker Conjugates 30 incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a PROTAC linker. E3 ligase Ligand-Linker Conjugates 30 can be used to design PROTAC MDM2 degrader[1]. |
|
| DC50058 |
VH032-C3-NH2((S,R,S)-AHPC-C3-NH2)
Featured
|
(S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852. UNC6852 is an EED-targeted bivalent chemical degrader[1]. |
.png)
|
| DC50059 |
(S,R,S)-AHPC-C4-NH2
Featured
|
(S,R,S)-AHPC-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC[1].
|
|
| DC50060 |
(S,R,S)-AHPC-C2-NH2 dihydrochloride
Featured
|
(S,R,S)-AHPC-C2-NH2 dihydrochloride incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-OH can be used in the synthesis of a series of PROTACs[1]. |
|
