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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
180 Results for "
chimera
" in MedChemExpress (MCE) Product Catalog:
Products (180)
180 Results for "chimera" in MCE Product Catalog:
15
15 Publications Verification
Target:
Research Areas:
AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .
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8 Cited Publications
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MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent . MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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7 Cited Publications
CCT128930 is a ATP-competitive and selective inhibitor of AKT (IC50=6 nM for AKT2). CCT128930 has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). Antitumor activity.
7
7 Cited Publications
CCT128930 hydrochloride is a potent and selective inhibitor of AKT (IC50=6 nM). CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. Antitumor activity .
5
5 Cited Publications
SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations .
4
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PhosTAC7 is a heterobifunctional molecule named as a Phosphorylation Targeting Chimera (PhosTAC). PhosTAC7 can dephosphorylate the PDCD4 protein, FOXO3a protein, and tau protein by recruiting serine/threonine protein phosphatase 2A (PP2A). PhosTAC7 offers the advantage of selectively modulating the phosphorylation state of individual target proteins, making it a promising tool for research in cancer and tau protein-related neurodegenerative diseases (Alzheimer's disease) .
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4 Cited Publications
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AUTAC4 is a mitochondria-targeting autophagy-targeting chimera (AUTAC). AUTAC4 downregulates cytosolic proteins and promotes targeted mitochondrial turnover via mitophagy .
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2
2 Cited Publications
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DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets .
1
1 Cited Publications
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PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM .
1
1
1 Cited Publications
AD4 is an artemisinin derivative that is a proteolytic targeting chimera (PROTAC) targeting PCLAF. AD4 can effectively degrade PCLAF in RS4;11 cells (IC50: 0.6 nM), thereby activating the p21/Rb axis and exerting anti-tumor activity. AD4 also prolonged survival of RS4;11-transplanted NOD/SCID mice, with in vivo efficacy .
1
1
1 Cited Publications
Cat. No.: HY-153713
Purity: 98.05%
MYC-RIBOTAC is a nucleic acid-targeting degrader (ribonuclease-targeting chimera, RIBOTAC) that targets the MYC internal ribosome entry site (IRES). MYC-RIBOTAC contains a MYC mRNA binding component and a small molecule that recruits and locally activates RNAse L1. MYC-RIBOTAC reduces MYC mRNA and protein expression levels, induces cell apoptosis, and can be used for antitumor research . MYC-RIBOTAC consists of pre-miR-155 binder Anticancer agent 167 (HY-156839), RNA binder NCI-B16 (HY-156215), and Linker Amino-PEG4-alcohol (HY-W008005).
1
1 Cited Publications
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MN551 is a covalent modulator of SOCS2 and CISH, with selectivity for SOCS2 and CISH over SOCS4. MN551 covalently modifies Cys111 in the SH2 domain of SOCS2 and Cys144 in the EF loop of the CISH SH2 domain, while only minimally modifying Cys471 in the BG loop of the SOCS6 SH2 domain. MN551 increases the thermal stability of the recombinant SOCS2-ElonginB-ElonginC complex and competitively blocks the binding of SOCS2 to its substrate; when delivered via the prodrug MN714, it blocks the intracellular recruitment of substrates by SOCS2. MN551 can serve as a chemical probe for investigating the biological functions of SOCS2 and its CRL5 complex, and also act as an E3 ligase-binding module in proteolysis-targeting chimeras (PROTACs) .
Tri-GalNAc(OAc)3 TFA is a trivalent N-acetylgalactosamine (GalNAc) derivative that can be used to synthesize GalNAc-LYTAC. Tri-GalNAc is a specific ligand targeting the asialoglycoprotein receptor (ASGPR), mediating the endocytosis and transport of cell surface proteins (such as EGFR, HER2) to lysosomes for degradation by lysosomal targeting chimeras (LYTACs). Tri-GalNAc significantly reduces the level of target proteins and inhibits downstream signaling pathways (such as EGFR-mediated Akt and MAPK signals). Tri-GalNAc(OAc)3 TFA can be used for hepatocyte targeting studies, and can degrade carcinogenic membrane proteins and inhibit tumor cell proliferation in liver cancer cell models .
tri-GalNAc-COOH is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research .
J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1 .
HaloAUTAC tt15 is an autophagy-targeting chimera (AUTAC), that targets the Halo Tag carrying proteins, and degrades via the autophagy mechanism .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
