| DC71625 |
Tivozanib hydrochloride hydrate
Featured
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Tivozanib hydrochloride hydrate is a potent and selective and orally active VEGFR tyrosine kinase inhibitor with IC50是of 0.21, 0.16, 0.24 nM for VEGFR-1, VEGFR-2, VEGFR-3, respectively. Tivozanib hydrochloride hydrate inhibits angiogenesis and vascular permeability in tumor tissues and shows antitumor activity. Tivozanib hydrochloride hydrate has the potential for the research of metastatic renal cell carcinoma (RCC) . |
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| DC71627 |
Ansornitinib
Featured
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Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases. |
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| DC71628 |
WAY-340935
Featured
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WAY-340935 (VEGFR2-IN-2) can inhibit the function of VEGFR2 and the anti-proliferative activity against the H460 cell line is produced partly by interaction of VEGFR protein. |
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| DC71650 |
BVDV IN-1
Featured
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BVDV IN-1 is a non-nucleoside inhibitor of bovine viral diarrhea virus (BVDV), with an EC50 of 1.8 μM. |
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| DC71661 |
Loxoprofenol-SRS tromethamine
Featured
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Loxoprofenol-SRS tromethamine (HR1405-01), an active metabolite of Loxoprofen, is a Safe intravenous non-steroidal anti-inflammatory drug (NSAID) with superior anti-inflammatory and analgesic activities. |
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| DC71664 |
Val-Cit-PAB-MMAF sodium
Featured
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Val-Cit-PAB-MMAF sodium is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAF sodium contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin polymerization inhibitor MMAF.
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| DC71665 |
Val-Cit-PAB-MMAF
Featured
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Val-Cit-PAB-MMAF is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAF contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin polymerization inhibitor MMAF.
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|
| DC71668 |
Iu1-248
Featured
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Iu1-248, a derivative of IU1, is a potent and selective ubiquitin specific peptidase 14 (USP14) inhibitor with an IC50 of 0.83 μM. |
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| DC71676 |
EZM0414
Featured
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EZM0414 is a potent, selective, and orally bioavailable inhibitor of Histone-lysine N-methyltransferase SETD2. |
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| DC71677 |
IMD-0560
Featured
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IMD-0560 is an Inhibitor of nuclear factor kappa-B kinase (IKK) which can suppress the production of inflammatory cytokines and chemokines. |
|
| DC71683 |
Lodenafil
Featured
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Lodenafil (Hydroxyhomosildenafil) is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED). |
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| DC71686 |
Decanoic acid, 2-hexyl-, 6-oxohexyl ester-1
Featured
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Decanoic acid, 2-hexyl-, 6-oxohexyl ester-1 is a lipid product can be used for drug delivery. |
|
| DC71689 |
K145
Featured
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K145 is a selective, substrate-competitive and orally active sphingosine kinase-2 (SphK2) inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM in biochemical assays. |
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| DC71690 |
Amgen-23
Featured
|
Amgen-23 (compound 23) is a potent sphingosine kinases (SPHK) inhibitor with IC50 values of 20 nM and 1.6 μM for SPHK1 and SPHK2, respectively. Amgen-23 can be used for researching anticancer. |
|
| DC71697 |
DHAPC
Featured
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DHAPC is a phospholipid that is very sensitive to oxidation. |
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| DC71699 |
DOIC
Featured
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DOIC is a cationic lipid that can be used for RNA vaccines. |
|
| DC80050 |
LIPID A6
Featured
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Ionizable lipid A6 (di(dec-3-yn-1-yl) 9-((4-(dimethylamino) butanoyl)oxy) heptadecanedioate) was developed by modifying
the backbone structure of Dlin-MC3-DMA through introducing alkynyl and ester groups into the lipid tails. Alkyne lipid A6 demonstrated a significant improvement in transfection efficiency (~8.5, ~2.0, and ~2.5-fold higher than the original MC3, C12-200 and cKK-E12 containing LNPs, respectively).The performance
of the A6 coprepared into iLNPs with other amine-containing
lipid materials (cKKE12) was evaluated, and the molar ratio of
the formulation was changed to 35:16.0:46.5:2.5 (A6/cKKE12:
DOPE: Chol: PEG). The results showed that these formulations
synergistically facilitated more effective mRNA delivery and
improved tolerability following single and repeated dosing. It
was confirmed that albumin-associated macrophage phagocytosis
and endocytosis is an apolipoprotein-independent cellular
internalization pathway of iLNPs in the liver.
According to the fusion kinetics, the lipids with highfrequency
tail protrusion and high lateral diffusion coefficient
can perturb and trigger membrane sprouting, which in turn promotes
membrane fusion. The application of iLNPs with those
lipids (such as A6) may be an effective method to further enhance
the release of mRNA in vivo. |
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| DC80052 |
H-D-Pro-Phe-Arg-pNA·2 HCl
Featured
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S-2302 is a Chromogenic substrate for plasma kallikrein, factor XIa and factor XIIa. |
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| DC80060 |
p-Tolyl-β-D-glucuronide
Featured
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p-Cresol glucuronide is a metabolite of p-cresol, a uremic toxin formed by bacterial fermentation of proteins in the large intestine. It is formed from p-cresol primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT1A6, but also by UGT1A9, in huma |
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| DC80065 |
113-O12B
Featured
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113-O12B is a disulfide bond-containing ionizable cationic lipidoid. 113-O12B LNP, an LN-targeting LNP delivery system, is developed for a mRNA cancer vaccine. The 113-O12B/mRNA shows enhanced expression in APCs compared with ALC-0315/mRNA, indicating the LN-specific targeting ability. |
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| DC80066 |
306Oi10
Featured
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306Oi10 is a branched-chain ionizable lipidoid that has shown significant promise in the generation of lipid nanoparticles (LNPs) for mRNA delivery. Its unique structural and functional properties make it a highly efficient delivery vehicle for mRNA-based therapeutics. |
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| DC80068 |
LIPID PL1
Featured
|
PL1 is a novel biomimetic phospholipid. PL1 nanoparticle delivery of costimulatory
receptor CD137 mRNA improved the immunotherapy with an
anti-CD137 Ab to some extent in both tumor models with better
results obtained in the B16F10 melanoma model as compared to
the A20 lymphoma model. |
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| DC80069 |
OF-DEG-LIN
Featured
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OF-Deg-Lin is a biodegradable lipid containing an ester group, developed from the nonbiodegradable, linoleic acid derived OF-02; mRNA-LNPs containing OF-Deg-Lin showed high expression in the spleen. The ionizable lipid Of-Deg-Lin was synthesized,
which possessed the similar chemical structure with OF-02.Both Of-Deg-Lin and OF-02 had diketopiperazine core and
doubly unsaturated tails, and the difference between them
was that Of-02 contained nondegradable 1,2-amino-alcohol linkages,
whereas Of-Deg-Lin contained degradable ester linkages The change of linker altered iLNPs distribution
and mRNA expression in vivo. Although the Of-Deg-Lin iLNPs
could accumulate in the liver and spleen, they induced the
expression of most functional proteins in B lymphocytes of
spleen (over 85% of the total protein), not in the liver.
Of-Deg-Lin iLNPs can deliver mRNA and express functional
proteins in the spleen specifically, but the mechanism
is unclear. |
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| DC80070 |
A2-Iso5-2DC18
Featured
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A2-Iso5-2DC18 is a top-performing lipid for mRNA delivery in bone marrow-derived dendritic cells (BMDCs), BMDMs and HeLa cells. |
|
| DC80071 |
A18-ISO5-2DC18 (Pimidol)
Featured
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A18-Iso5-2DC18 that could not only deliver mRNA vaccines robustly but also activate the stimulator
of interferon genes (STING) pathway. A18-Iso5-2DC18 strongly binds to the stimulator of interferon genes (STING) and induces potent cytolytic T lymphocyte responses, resulting in substantial antitumor immunity (Miao et al. 2019). |
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| DC80072 |
306-O12B (Triscormin)
Featured
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306-O12B is a cationic lipidoid.306-O12B LNP is more efficient than MC-3 LNP in inducing loss-of-function mutations in Angptl3 through CRISPR-Cas9-based genome editing. It has been used in the generation of lipid nanoparticles (LNPs). Intravenous administration of LNPs containing 306-O12B and encapsulating an mRNA reporter accumulate specifically in the mouse liver. LNPs containing 306-O12B and encapsulating mRNA encoding the Cas9 nuclease (mCas9) and single-guide RNA targeting Angptl3 (sgAngptl3), the gene encoding angiopoietin-related protein 3, have been used to induce CRISPR-mediated gene knockdown in mice resulting in a reduction of serum Angptl3 protein, LDL, and triglyceride levels. A novel ionizable lipids library was constructed by a combinatory solvent-free Michael addition reaction between disulfide bondincorporated acrylate lipid tails and amine-containing heads. In this library, the tail-branched bioreducible ionizable lipid 306-O12B was screened out. Due to the presence of special ester bonds and branches in lipid tails, the accumulation of iLNPs in the liver was increased, and endosome escape was prompted. These iLNPs were used to deliver CRISPR-Cas9 mRNA and sgRNA targeting to angiopoietin-like 3 (Angptl3). Compared with FDA-approved MC3, 306-O12B induced more specific and efficient Angptl3 gene knockout in the liver, resulting in significant decrease in the levels of serum Angptl3 protein, low-density lipoprotein cholesterol (LDL-C), and triglyceride. According to the molecular shape hypothesis outlined several decades ago, the increase of branches can create ionizable lipids with more cone-shaped structure to enhance the destructiveness of the membrane structure of the endosome and increase mRNA release. However, it is unknown whether the structural stability of iLNPs will be sacrificed with the increase of branches. The optimal branches and chain length need to be further explored. |
|
| DC80080 |
OF-C4-Deg-Lin
Featured
|
OF-C4-Deg-Lin is a novel ionizable lipid for RNA delivery. OF-C4-Deg-Lin LNPs entrapping mRNA coding for luciferase induce the majority of protein expression in the spleen, with minimal translation in the liver, and negligible translation in other organs. OF-C4-Deg-Lin LNPs entrapping mRNA coding for luciferase induce the majority of protein expression in the spleen, with minimal translation in the liver, and negligible translation in other organs. To improve the mRNA delivery to extrahepatic tissues, a series of degradable diketopiperazine-based ionizable lipids were synthesized. Through evaluating the mRNA functional activity delivered by iLNPs, it was found that the ionizable lipids with
doubly unsaturated lipid tails and linkers containing a length of four carbon aliphatic chain (Of-C4-Deg-Lin) could deliver the mRNA more efficiently. Moreover, compared with cKK-E12 and Invivofectamine, Of-C4-Deg-Lin could specifically induce more than 85% of firefly luciferase expression in spleen,minimal expression in the liver, and insignificant expression in other tissues. |
|
| DC80073 |
Azido-PEG4-EV-Cit-PAB-MMAE
Featured
|
Azido-PEG4-EV-Cit-PAB-MMAE is a precursor of antibody drug conjugate. |
|
| DC60242 |
Florazone
Featured
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|
| DC60243 |
felezonexor（SL-801）
Featured
|
Felezonexor, also known as CBS9106, SL-801, and BMS566419, is a novel reversible oral CRM1 inhibitor with CRM1 degrading activity. CRM1 plays an important role in the nuclear export of cargo proteins bearing nuclear exporting signal sequences. CBS9106 inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells, including multiple myeloma cells. CBS9106 reduces CRM1 protein levels significantly without affecting CRM1 mRNA expression. Oral administration of CBS9106 significantly suppresses tumor growth and prolongs survival in mice bearing tumor xenograft without a significant loss in body weight. |
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