| DC47939 |
NBI-921352
Featured
|
NBI921352 is a Nav1.6 inhibitor with an IC50 value of 3.765 μM. |
|
| DC47944 |
MRT-81
Featured
|
MRT-81 is a potent antagonist of human and rodent smoothened Smo receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer. |
|
| DC47957 |
LSN3318839
Featured
|
LSN3318839 is an orally efficacious positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R). |
|
| DC47969 |
JADA82
Featured
|
JADA82 (PCK82) is a potent KDM5A (lysine demethylase 5A) inhibitor. From patent WO2020033377A1. |
|
| DC47977 |
I-BET567
Featured
|
I-BET567 is a potent and oral active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation. |
|
| DC47980 |
HIF-2α-IN-4
Featured
|
HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing. |
|
| DC47985 |
GNE-9815
Featured
|
GNE-9815 is among the most highly kinase-selective RAF inhibitors targeting KRAS mutant cancers via combination treatment. |
|
| DC47989 |
FPFT-2216
Featured
|
FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease. |
|
| DC48014 |
CXCR7 antagonist-1
Featured
|
CXCR7 antagonist-1 is an inhibitor of the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR. CXCR7 antagonist-1 prevents tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases (extracted from patent WO2014085490A1, compound 1.128). |
|
| DC48021 |
CL097
Featured
|
CL097, a potent TLR7/8 agonist, induces pro-inflammatory cytokines in macrophages. CL097 induces NADPH oxidase priming, resulting in an increase of the fMLF-stimulated ROS production. |
|
| DC48024 |
cGAMP diammonium
Featured
|
cGAMP (Cyclic GMP-AMPP) diammonium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators. |
|
| DC48025 |
Cevidoplenib dimesylate
Featured
|
Cevidoplenib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities. |
|
| DC48043 |
BIIB091
Featured
|
BIIB091 is a novel reversible, selective, potent BTK inhibitor with Kd of 0.07 nM. |
|
| DC48046 |
AZD-5672
Featured
|
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis. |
|
| DC48075 |
SGC-SMARCA-BRDVIII
Featured
|
SGC-SMARCA-BRDVIII is a potent and selective SMARCA2/4 BRD inhibitor. |
|
| DC48081 |
MINA53 inhibitor (Compound 10)
Featured
|
MINA53 inhibitor (Compound 10) is a first-in-class inhibitor of the ribosomal oxygenase MINA53 with an IC50 of 1.5 μM in vitro. |
|
| DC59002 |
ssPalmO-Phe(SS-OP)
Featured
|
ssPalmO-Phe(SS-OP) is a self-degradable material for the delivery of oligonucleotides. ssPalmO-Phe is a self-degradable derivative of ssPalm that is self-degraded in the intraparticle space by a specific hydrolytic reaction. ssPalmO-Phe is beneficial for overcoming the plasma/endosomal membrane, LNP-ssPalmO-Phe can be used to deliver both nucleic acids. |
|
| DC60201 |
SR 18662
Featured
|
SR18662 is an optimized anticancel agent based on ML264. SR18662 Efficiently Inhibits the Growth of Colorectal Cancer In Vitro and In Vivo. SR18662 showed improved efficacy in reducing the viability of multiple colorectal cancer cell lines. Flow cytometry analysis following SR18662 treatment showed an increase in cells captured in either S or G2-M phases of the cell cycle and a significant increase in the number of apoptotic cells, the latter a unique property compared with ML264 or SR15006. SR18662 treatment also reduces the expression of cyclins and components of the MAPK and WNT signaling pathways. |
|
| DC59005 |
Ozanimod hydrochloride
Featured
|
Ozanimod is a potent and selective S1P1 and S1P5 receptor agonist with EC50s of 410±160 pM and 11±4.3 nM in [35S]-GTPγS binding, respectively. |
|
| DC59006 |
AEOL-10150 (pentachloride)
Featured
|
AEOL-10150 pentachloride is a metalloporphyrin catalytic antioxidant and is a superoxide dismutase mimetic, and protects lungs from radiation-induced injury[1]. |
|
| DC59010 |
C14-4 (C14-494,Lipid B-4,Lipid B4)
Featured
|
C14-4 (C14-494,Lipid B-4,Lipid B4) is a novel ionizable lipid with the highest T-cell transfection efficiency and low cytotoxicity.The C14-4 ionizable lipid has been explored for CAR-T therapy.To screen the excellent formulations for mRNA delivery, a
lipid library of 24 ionizable lipids was constructed to make
iLNPs, which were used to deliver luciferase mRNA into
Jurkat cells.[115] The optimal iLNPs formulation was C14-4
iLNPs (C14-4 ionizable lipid, DOPE, chol, and PEG at a molar
ratio of 35%, 16%, 46.5%, and 2.5%) (Figure 6c). The optimal
dose of luciferase mRNA for C14-4 iLNPs was 30 ng.
Compared with electroporated CAR T cells, the CAR T cells engineered
via C14-4 iLNPs showed potent cancer-killing activity
when they were cocultured with Nalm-6 acute lymphoblastic leukemia
cells. To obtain a safer and more effective CAR mRNA
delivery vehicle, the orthogonal design provided 256 potential
formulations, and 16 representative iLNPs formulations were
evaluated.Through evaluating the safety, delivery efficiency,
and transfection efficiency of 16 iLNPs, the formulation B10
(C14-4 ionizable lipid, DOPE, chol, PEG at a molar ratio of
40%, 30%, 25%, and 2.5%) was screened out as the optimal performing formulation. The luciferase expression based on B10
formulation was increased threefold than the initial formulation.
Reducing the accumulation and clearance of iLNPs in the liver
can increase the expression of CAR mRNA in T cells, further
improving the therapeutic effect of CAR-T. Studies have shown
that cholesterol analogs can alter the mechanisms of intracellular
circulation and enhance the delivery of mRNA, which may be
related to the reduced recognition of iLNPs by the Niemann
Pick C1 (NPC1) enzyme.The addition of a hydroxyl
group to various locations in the cholesterol molecule can alter
the binding kinetics between the modified cholesterol and NPC1,
and reduced NPC1 recognition of cholesterol. The results
showed that replacement of 25% and 50% 7 α-hydroxycholesterol
for cholesterol in iLNPs improved mRNA delivery to
primary human T cells in vitro by 1.8-fold and twofold,
respectively.C14-4 is one of the ionizable lipids to efficiently deliver mRNA
to Jurkat cells or primary human T cells. It will effectively promote
the development of mRNA delivery by iLNPs for CAR-T
therapy. |
|
| DC59012 |
Org41841
Featured
|
Org-41841 is an agonist for the luteinizing hormone/chorionic gonadotropin receptor (LHCGR) and partial agonist for TSHR. |
|
| DC59015 |
BI-0115
Featured
|
BI-0115 is a selective small molecule inhibitor of LOX-1 that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain. The structure of LOX-1 bound to BI-0115 shows that inter-ligand interactions at the receptor interfaces are key to the formation of the receptor tetramer thereby blocking oxLDL binding. |
|
| DC59016 |
Ensitrelvir (S-217622)
Featured
|
S-217622 is the first oral non-covalent, non-peptidic SARS-CoV-2 3CL protease inhibitor with IC50 of 0.096 μM. S-217622 displays antiviral activity in vitro towards a range of SARS-CoV-2 variants and coronavirus families, favorable drug metabolism and pha |
|
| DC59018 |
PLX5622 hemifumarate
Featured
|
PLX-5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals. |
|
| DC59120 |
BTSA1.2
Featured
|
BTSA1.2 is a rationalized BTSA1 analog with improved binding to BAX, cellular cytotoxicity, and better toleratence in vivo. Combination of BTSA1.2 with Navitoclax demonstrates synergistic efficacy in apoptosis-resistant cancer cells, xenografts, and patient-derived tumors while sparing healthy tissues. |
|
| DC48099 |
Fipravirimat
Featured
|
Fipravirimat is a potent HIV-1 inhibitor. Fipravirimat has the potential for HIV and AIDS research. |
|
| DC48107 |
Ensitrelvir fumarate
Featured
|
Ensitrelvir (S-217622) fumarate is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM). |
|
| DC48112 |
Ac-YVAD-cmk
Featured
|
Ac-YVAD-cmk (Caspase-1 Inhibitor II) is a selective caspase-1 (IL-1beta converting enzyme, ICE)) inhibitor with neuroprotective and anti-inflammatory effects. Ac-YVAD-cmk effectively suppresses the expression of IL-1β and IL-18. Ac-YVAD-cmk inhibits pyroptosis in many diseases. |
|
| DC48117 |
EB-42486
Featured
|
EB-42486 is a novel, potent, and highly selective G2019S-LRRK2 inhibitor (IC50 < 0.2 nM). |
|
