| DC72873 |
MTK458
Featured
|
MTK458 (MTK-458) is a potent, selective and brain penetrant PINK1 activator, MTK-458 promotes the first step in mitophagy.
MTK458 selectively activates PINK1 by stimulating dimerization and stabilization of the PINK1/TOM complex.
MTK458 binds to PINK1 and stabilizes an active heterocomplex, thereby increasing mitophagy.
MTK458 reduces the PINK1 substrate pS65-Ubiquitin (pUb) in primary neurons and in vivo.
MTK458 drives clearance of pathologic α-synuclein in vitro and in vivo, decreases pS129 α-synuclein aggregates and normalized both brain and corresponding plasma pUb levels in both cellular and animal models of α-synuclein aggregation (PD-like pathology). |
|
| DC65319 |
UNC7145
Featured
|
UNC7145 is a negative control for UNC6934 (GLXC-22088). |
|
| DC65320 |
Mandipropamid
Featured
|
|
|
| DC65321 |
BAY-297
Featured
|
BAY-297 is a potent and selective PIP4K2A inhibitor. BAY-297 can serve as valuable chemical probes to study PIP4K2A signaling and its involvement in pathophysiological conditions such as cancer. |
|
| DC65322 |
BT8009
Featured
|
BT8009 is a Nectin-4 targeting toxin conjugate with a Kd value of 2.5 nmol/L for human Nectin-4 (hNectin-4) extra-cellular domain (ECD). BT8009 consists of a Nectin-4-binding bicyclic peptide, a cleavable linker system and monomethylauristatin E (MMAE). BT8009 can be used for the research of advanced and metastatic urothelial cancer. |
|
| DC65323 |
Nerandomilast (Synonyms: BI 1015550)
Featured
|
Nerandomilast (BI 1015550) is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD). |
|
| DC65324 |
NX-2127
Featured
|
NX-2127 is a potent, selective, and orally bioavailable BTK degrader with Kd of 18 nM (for WT BTK), 45 nM (BTK C481S), 18 nM (BTK T474I), 44 nM (BTK M437R), 97 nM (BTK V416L), and 88 nM (BTK L528W), respectively. NX-2127 efficiently engages the intracellular ubiquitin-proteasome system to simultaneously bind both BTK and the CRBN E3 ubiquitin ligase complex, inducing polyubiquitination and proteasome-dependent degradation of BTK, IKZF1, and IKZF3. |
|
| DC65325 |
MK-0616
Featured
|
MK-0616 is a potent, oral macrocyclic peptide inhibitor of PCSK9 that is not only able to reduce LDL-cholesterol, non-HDL-cholesterol, and apoB, but can also lower Lp(a). |
|
| DC65327 |
306-N16B (Disulpax)
Featured
|
306-N16B is a lipidnanoparticle, and allows systemic codelivery of Cas9 mRNA and sgRNA. 306-N16B can transport mRNA to the pulmonaryendothelial cell. 306-N16B can be used for research of genome editing-based therapies. Based on the same lipid libraries with 306-O12B, the researchers also found that N-series ionizable lipids were able to selectively deliver mRNA to the lungs of mice. Compared with the liver-targeted O-series ionizable lipids which contained ester bond in lipid tail found in previous work, such as 306-O12B, the N-series ionizable lipids with
the lipid tail containing amide bond prefer to deliver mRNA to the lung. As a N-series ionizable lipid, the chemical structure of the 306-N16B is shown in Figure 4a,b. The difference of organ targeting may be due to their adsorption
of different protein coronas during blood circulation caused
by their different structures mentioned earlier.It has
shown that the second major protein of the protein
corona adsorbed by liver-targeting 306-O12B iLNPs was apolipoprotein
E (ApoE), while the three dominant proteins in the
protein corona adsorbed by lung-targeting 306-N16B iLNPs
were serum albumin, fibrinogen beta chain, and fibrinogen
gamma chain. However, the 306-N16B iLNPs showed less
organ selectivity when systematically codelivered Cas9
mRNA and sgRNA in vivo, which could simultaneously
activate tdTomato expression in the liver and lung of Ai14
mice, whereas single mRNA delivery could almost
exclusively deliver mRNA to the lungs. This surprising phenomenon
requires further investigation. Both the change of
iLNPs charge and the change of lipids functional group
can influence the distribution of iLNPs in vivo due to
the altering of protein corona composition. Therefore,
it is possible to control the organ targeting of iLNPs by
controlling the composition of the outer protein corona of
iLNPs. |
|
| DC65329 |
ALC-0315 analogue-2
Featured
|
ALC-0315 analogue-2 is an analogue of ALC-0315. ALC-0315 is an ionisable aminolipid that is responsible for mRNA compaction and aids mRNA cellular delivery and its cytoplasmic release through suspected endosomal destabilization. ALC-0315 can be used to form lipid nanoparticle (LNP) delivery vehicles. Lipid-Nanoparticles have been used in the research of mRNA COVID-19 vaccine. |
|
| DC65331 |
LNP Lipid-1
Featured
|
LNP Lipid-1 (Method B) is a lipid compound. LNP Lipid-1 is involved in the synthesis of lipid nanoparticles compositions. LNP Lipid-1 has potential applications in the transport of biologically active substances such as small molecule drugs, proteins, and nucleic acids. |
|
| DC65333 |
A2-Iso5-4DC19
Featured
|
A2-Iso5-4DC19 is a lipidoid compound. A2-Iso5-4DC19 is an effective carrier for the delivery of an agent such as a polynucleotide to a cell. |
|
| DC65334 |
Lipid 15
Featured
|
Lipid 15 is an ionizable amino lipid used for the generation of Lipid nanoparticles . |
|
| DC65335 |
LNP Lipid-5
Featured
|
LNP Lipid-5 (Compound Lipid 2) is an ionizable lipid (amino lipid). LNP Lipid-5 can be used to prepare lipid nanoparticles . |
|
| DC65336 |
PSMA-1007
Featured
|
PSMA-1007 is a novel Glu-Ureido-based prostate-specific membrane antigen (PSMA) inhibitor designed for use in positron emission tomography (PET) imaging of prostate cancer. It belongs to the class of small-molecule PSMA inhibitors that specifically target PSMA, a transmembrane protein highly expressed in prostate cancer cells and the neovasculature of other solid tumors. PSMA-1007 is particularly notable for its favorable pharmacokinetic properties, including high tumor uptake and low urinary excretion, making it an excellent tool for prostate cancer diagnosis and staging. |
.gif)
|
| DC65337 |
DUPA(OtBu)-OH
Featured
|
DUPA(OtBu)-OH is a DUPA precursor. DUPA is used as the targeting moiety to actively deliver Docetaxel (DTX) for treatment of Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer. |
|
| DC65338 |
Pentixafor(CPCR4-2)
Featured
|
Pentixafor is a synthetic, cyclic pentapeptide analog of stromal cell-derived factor-1 (SDF-1 or CXCL12), which is the natural ligand for the C-X-C chemokine receptor type 4 (CXCR4). CXCR4 is a chemokine receptor that plays a critical role in tumor growth, progression, invasiveness, and metastasis. Pentixafor is designed to target CXCR4, which is overexpressed in various cancers and is associated with poor differentiation and aggressive disease. |
|
| DC65339 |
HBED-CC-tris（tBu) ester
Featured
|
|
|
| DC65340 |
UAMC1110-NH2
Featured
|
UAMC1110-NH2 is a derivative of UAMC1110 (SP-13786) with an aminobutoxy group, making it a useful intermediate for synthesizing UAMC1110 conjugates. UAMC1110 is a potent and selective FAP inhibitor with low nanomolar potency and high specificity over related proteases. Together, UAMC1110-NH2 and UAMC1110 have significant potential for advancing FAP-targeted therapies, imaging agents, and research tools, particularly in cancer and fibrotic diseases.
|
|
| DC65341 |
[18F]PSMA-1007
Featured
|
[18F]PSMA-1007, a positron emission tomography (PET) tracer, specifically targets prostate-specific membrane antigen (PSMA), which is highly expressed in prostate cancer. PSMA-PET is effective especially for regional detection of biochemical recurrence, which significantly affects patient management. Herein, we established and optimized a one-step radiolabeling protocol to separate and purify [18F]PSMA-1007 with a CFN-MPS200 synthesizer for clinical application. |
|
| DC65342 |
Fmoc-Cit-PAB-OH
Featured
|
Fmoc-Cit-PABA is a peptide linker useful for drug conjugate synthesis or ADC synthesis.
|
|
| DC65343 |
SU-5616
Featured
|
SU-5616 is a biochemical reagent. SU 5616 potentially modulates tyrosine kinase signal transduction, and regulates abnormal cell proliferation. |
|
| DC65344 |
KWCN-41
Featured
|
KWCN-41 is a selective and efficient inhibitor of RIPK1 kinase with an IC50 value of 88 nM. KWCN-41, specifically inhibiting cell necroptosis but not apoptosis, protects cell survival by blocking the necroptotic pathway, which inhibits the phosphorylation of essential proteins of the necroptosis. It also prevented the development of inflammation and reduced the level of inflammatory factors in mice. KWCN-41 is expected to be a lead compound for further studies in inflammatory diseases.
|
|
| DC65345 |
TRV-7019
Featured
|
TRV-7019 is a BBB-penetrable radioligand for brain imaging that target butyrylcholinesterase. TRV-7019 can be used for the diagnosis of an amyloid disease, multiple sclerosis, a brain tumor, or butyrylcholinesterase activity. |
|
| DC65346 |
ZM-226600
Featured
|
ZM-226600 is a potent Kir6 (KATP) channel opener (EC50 = 0.5 μM), devoid of antiandrogen properties. ZM226600 is more active than oxybutynin in reducing bladder overactivity, and it is devoid of vascular side effects observed with pinacidil. Its short duration of action (about 1 h) is probably the main problem to solve, in order to consider this compound a valid alternative to antimuscarinics in the therapy of bladder overactivity. |
|
| DC65347 |
A-674563 HCl
Featured
|
A-674563 is a potent and selective Akt1 inhibitor with Ki of 11 nM. A-674563 suppressed the activation of the NLRP3 inflammasome in cardiomyocytes following β-adrenoceptor activation, suggesting that AKT1 is a critical regulator molecule upstream of the NLRP3 inflammasome. A-674563 suppresses CDK2 activity, inhibits human NSCLC cell growth more effectively than the pan-AKT inhibitor, MK-2206 |
|
| DC72877 |
PF-114
Featured
|
Vamotinib (PF-114) is a potent, selective and orally available inhibitor of native (IC50=0.49 nM) and mutated BCR/ABL (IC50=0.7-4 nM, ABL (T315I) IC50=0.78 nM). PF-114 potently inhibits ABL2, DDR1, DDR2, FMS, FRK, LCK, LYN and PDGFR kinases, but did not inhibit c-SRC, CSK, or c-KIT. |
|
| DC72880 |
Norepinephrine hydrochloride
Featured
|
Norepinephrine (Levarterenol; L-Noradrenaline) hydrochloride is a potent agonist of adrenergic receptor (AR). Norepinephrine activates α1, α2, β1 receptors. |
|
| DC72885 |
Lirafugratinib
Featured
|
Lirafugratinib (RLY-4008) is an orally active and selective inhibitor of FGFR2. |
|
| DC72888 |
Z0933M
Featured
|
Z0933M is a potent S phase kinase-associated protein 1 (Skp1) inhibitor with Kd of 54 nM, potently inhibits Skp1-F-box protein-protein interactions with Ki value of 231 nM in FP-based in vitro competition assays. |
|
