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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
17 Results for "
VCP Inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (17)
17 Results for "VCP Inhibitors" in MCE Product Catalog:
53
53 Publications Verification
CB-5083 is a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC50 of 11 nM .
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MSC1094308 is a non-competitive and reversible VPS4B/p97 (VCP) (I/II type AAA ATPase) allosteric inhibitor, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively . MSC1094308 inhibits the D2 ATPase activity by binding to a agentable hotspot of p97. MSC1094308 can be used in study of cancer .
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1 Cited Publications
Cat. No.: HY-139606
CAS No.: 2630950-38-6
VCP/p97 inhibitor-1 is a potent inhibitor of VCP/p97 (also called Cdc48, CDC-. 48, or Ter94) with an IC50 of 54.7 nM. VCP/p97 inhibitor-1 causes the dysregulation of protein homeostasis and disturbs the degradation of misfolded polypeptides by the ubiquitin-proteasome system (UPS) .
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Mal-PEG2-VCP-Eribulin consists the ADCs linker (Mal-PEG2-VCP) and Eribulin (HY-13442). Eribulin is a mechanistically unique microtubule inhibitor and Eribulin inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules. Mal-PEG2-VCP-Eribulin is an Eribulin-based agent for antibody conjugates .
Cat. No.: HY-128871
CAS No.: 2130869-17-7
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VCP-Eribulin is a bioactive molecule-linker conjugate designed for ADCs (Drug-Linker Conjugates for ADC), formed by conjugating an ADC linker (VCP) with Eribulin (HY-13442). Eribulin is a unique microtubule inhibitor exhibiting antitumor activity. VCP-Eribulin can be utilized for antibody conjugation .
NPD8733 is an inhibitor of cancer cell-enhanced fibroblast migration. NPD8733 specifically binds to valosin-containing protein (VCP)/p97, a member of the ATPase-associated with diverse cellular activities (AAA+) protein family. NPD8733 has the potential for the research of cancer diseases .
Cat. No.: HY-148122
CAS No.: 2749599-78-6
NW 1028 is a potent VCP/p97 inhibitor. NW 1028 targets the ND1L domain of p97 and inhibits the degradation of a p97-dependent reporter. NW 1028 has good binding affinity with Kd values of 100 and 285 nM for ND1L and full length p97, respectively. NW 1028 has the function of regulating the mitotic spindle of cells .
Cat. No.: HY-174984
CAS No.: 3098437-66-9
VCP/p97 IN-3 is a VCP/p97 allosteric inhibitor. VCP/p97 IN-3 shows the inhibitory activity against the VCP proteins with an IC50 of 9 nM and the mutant VCP proteins with IC50 of 12 nM (N660K) and 19 nM (V474A/D649A). VCP/p97 IN-3 increases K48-linked ubiquitination and the level of cleaved caspase-3. VCP/p97 IN-3 activates ER-stress and the UPR. VCP/p97 IN-3 inhibits tumor growth in RPMI-8226 cell subcutaneous xenograft mouse models. VCP/p97 IN-3 can be used for the study of multiple myeloma .
Cat. No.: HY-174847
CAS No.: 3007658-94-5
VCP/p97 IN-2 (Compound V13) is a VCP/p97 inhibitor with IC50 of 32 nM for p97. VCP/p97 IN-2 has excellent antitumor activities and significantly inhibits tumor growth in Molm-13 xenograft mice model. VCP/p97 IN-2 can be used for acute myeloid leukemia (AML) research .
Cat. No.: HY-177414
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BB-1701 is an anti-HER2 antibody-drug conjugate (ADC). BB-1701 consists of a humanized anti-HER2 antibody (Trastuzumab) (HY-P9907), a linker (Mal-PEG2-VCP), and a microtubule inhibitor (Eribulin) (HY-13442), with the drug-linker conjugate of the ADC being Mal-PEG2-VCP-Eribulin (HY-128870). BB-1701 exhibits potent cytotoxicity against various cancer cells, shows a remarkable bystander effect, and induces immunogenic cell death (upregulated cell surface expression of calreticulin, release of ATP/HMGB1, macrophage infiltration) and apoptosis. BB-1701 potently inhibits tumor growth in T-DM1/T-DXd-resistant tumor models. BB-1701 can be used in studies related to breast cancer, gastric cancer, non-small cell lung cancer, and heterogeneous mixed tumors .
Cat. No.: HY-177549
CAS No.: 2841688-52-4
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Fmoc-PEG6-VCP-Eribulin is the derivative of Eribulin (HY-13442). Eribulin (E7389) is a microtubule targeting agent that is used for the research of metastatic breast cancer. Eribulin inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules .
Cat. No.: HY-168007
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NSC804515 is an inhibitor of wild-type and R155H mutant p97/VCP ATPase, with an IC50 of about 15 nM for both targets. NSC804515 acts as an antiproliferative agent, disrupts the function of the ubiquitin-proteasome system, induces UbG76V-GFP accumulation, and shows reduced inhibitory potency against p97 variants carrying P510S, K512N, N616F and F618S mutations. NSC804515 can be used in research related to cancer, inclusion body myopathy with early-onset Paget's disease and frontotemporal dementia, as well as familial amyotrophic lateral sclerosis .
Cat. No.: HY-184291
CAS No.: 3114314-82-5
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VCP/p97 IN-4 is a p97/VCP inhibitor (Kd=14.99 μM) targeting the allosteric site of the D1-D2 domain. VCP/p97 IN-4 inhibits the ATPase activity of VCP/p97 in an ATP concentration-independent manner. VCP/p97 IN-4 induces apoptosis, autophagy, mitochondrial stress and mitochondrial membrane depolarization. VCP/p97 IN-4 inhibits the growth of patient-derived colorectal cancer organoids and exhibits in vivo efficacy in a colorectal cancer xenograft mouse model. VCP/p97 IN-4 can be used for the research of colorectal cancer .
Cat. No.: HY-118460
CAS No.: 1135195-64-0
Synonyms: VCP/p97-IN-PPA
ACJI-99C (VCP/p97-IN-PPA) is a selective covalent p97/VCP ATPase inhibitor with an IC50 value of 0.6 μM. ACJI-99C binds with p97 active site residues to block ATPase activity. ACJI-99C irreversibly blocks degradation of p97-dependent protein in cells. ACJI-99C inhibits proliferation of cancer cells, including p97 inhibitor-resistant lines. ACJI-99C can be used for the research of colorectal cancer .
Cat. No.: HY-183257
CAS No.: 1242983-93-2
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ATI-1 is an autophagy initiation inhibitor. ATI-1 targets valosin-containing protein (VCP/p97, disrupts its interaction with UFL1, impairs UFMylation homeostasis associated with VCP, promotes polyubiquitination and degradation of Beclin1, and blocks the formation of early autophagosomes. ATI-1 induces synergistic death of autophagy-dependent malignant tumor cells under nutrient deprivation conditions, accompanied by decreased mitochondrial membrane potential, reduced ROS levels and lysosomal stress. ATI-1 exhibits anti-tumor efficacy in a pancreatic adenocarcinoma xenograft mouse model. ATI-1 can be used for the research of pancreatic adenocarcinoma and lung cancer .
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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
