| DC72242 |
CCT367766 formic |
CCT367766 formic is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 formic exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 formic reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 formic provides a potential chemical tool to study a largely unexplored protein. |
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| DC72267 |
dBRD4-BD1 |
dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1. |
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| DC72274 |
4-Azidobutylamine |
4-Azidobutylamine is a PROTAC linker, which refers to the alkyl chain composition. 4-Azidobutylamine can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins. |
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| DC72275 |
Biotin-PEG3-C3-NH2 |
Biotin-PEG3-C3-NH2 is a PEG-based PROTAC linker, with NH2 functional group, that can be used in the synthesis of PROTACs. |
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| DC72499 |
PZ703b TFA |
PZ703b TFA is a Bcl-xl PROTAC degradation agent that induces apoptosis and inhibits cancer cell proliferation for bladder cancer research. |
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| DC72500 |
MS15 |
MS15 is a potent and selective AKT PROTAC degrader. MS15 inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively. |
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| DC72501 |
ACBI2 |
ACBI2 is a highly potent and orally active VHL PROTAC (EC50: 7 nM), which selectively degrades SMARCA2 with a DC50 value of 1 nM in RKO cells. ACBI2 can be used in the research of lung cancer. |
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| DC72502 |
PZ703b hydrochloride |
PZ703b hydrochloride is a Bcl-xl PROTAC degrader that induces Apoptosis and inhibits cancer cell proliferation. PZ703b hydrochloride can be used for the research of bladder cancer research. |
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| DC72503 |
NU223612 |
NU223612 is a potent PROTAC (PROTACs) that degrades indoleamine 2,3-dioxygenase 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO)) with a Kd of 640 nM. NU223612 potently degrades the IDO1 protein through CRBN-mediated proteasomal degradation. NU223612 is bound to CRBN with an affinity of 290 nM. NU223612 can cross the blood-brain barrier (BBB). |
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| DC72504 |
SJ988497 |
SJ988497 is a PROTAC JAK2 degrader. SJ988497 potently inhibits CRLF2-rearranged (CRLF2r) cell proliferation and degrades the CRBN neosubstrate GSPT1. SJ988497 consists of a Ruxolitinib derivative, linker, and CRBN ligand Pomalidomide. SJ988497 can be used in the research of acute lymphoblastic leukemia (ALL). |
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| DC72505 |
SIAIS100 |
SIAIS100 is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. SIAIS100 can be used to research chronic myeloid leukemia (CML). |
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| DC72506 |
TD1092 |
TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. TD1092 activates Caspase 3/7, and promotes cancer cells Apoptosis via IAP degradation. TD1092 inhibits TNFα mediated NF-κB pathway and reduces the phosphorylation of IKK, IkBα, p65, and p38. TD1092 can act as PROTAC, and is used for cancer research. |
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| DC60361 |
DLin-K-DM4 |
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| DC72754 |
cis-MZ 1 |
cis-MZ 1 is a negative control of MZ 1. cis-MZ 1 is a PROTAC targeting to BRD4. |
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| DC72755 |
MS6105 |
MS6105 is an LDH protein hydrolysis-targeted chimera (PROTAC) that effectively degrades LDHA and LDHB in a time- and ubiquitin-proteasome system-dependent manner and has anticancer activity. |
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| DC72756 |
JQAD1
Featured
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JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer. |
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| DC60447 |
ARV-766
Featured
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ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations[1]. |
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| DC65207 |
CFT-8634
Featured
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CFT8634 is an oral activity degrader targeting BRD9 extracted from patent WO2021178920A1 compound 174. CFT8634 can be used for the research of synovial sarcoma and SMARCB1-deleted solid tumors. |
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| DC65210 |
CFT1946
Featured
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CFT1946 is an orally active and selective target ligand for BRAF kinase. |
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| DC65211 |
KT-474
Featured
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KT-474 is a highly active and selective, orally bioavailable IRAK4 degrader being developed for the treatment of toll-like receptor (TLR)/interleukin-1 receptor (IL-1R)-driven immune-inflammatory diseases. |
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| DC65324 |
NX-2127
Featured
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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. |
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| DC72887 |
ML 2-23 |
ML 2-23 is a potent PROTAC BCR-ABL degrader. ML 2-23 is selectively degrade BCR-ABL in a proteasome-dependent manner in leukemia cells. |
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| DC72888 |
Z0933M
Featured
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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. |
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| DC60470 |
TCIP1 |
TCIP1 is the most potent transcriptional/epigenetic CIP (chemical inducers of proximity) and specifically activates BCL6 target genes. TCIP1 kills diffuse large B cell lymphoma cell lines, including chemotherapy-resistant, TP53-mutant lines and exhibits cell-specific and tissue-specific effects. TCIP1 successfully killed large B cell lymphoma cell lines, including chemotherapy-resistant TP53-mutant lines and exhibited cell-specific and tissue-specific effects. The activation of apoptosis to cell death took place in just 72 hours.BCL6 is critical to the lymphatic system, and mice engineered without the BCL6 gene die of complex inflammatory reactions. BRD4 is heavily involved in genome function and stability across many processes. Concerns regarding utilizing these important gene expressions and how they might affect off-target healthy tissues were addressed in the study.TCIP1 acts in a context-specific manner requiring the expression of BRD4 and BCL6 to both be present in order to bind them and operate at a concentration that would occupy only a tiny fraction of the total BCL6 molecules.TCIP1 induced dramatic transcriptomic changes in the spleen, notably with an upregulation of the FOXO3 gene, which mirrored activity in the targeted cancer cells. Despite the significant transcriptomic changes in the spleen, TCIP1 was well tolerated without adverse effects, with no significant differences in mouse body weight and no noticeable abnormalities such as inflammatory infiltrates or apoptotic cells.
BCL6-BRD4 TCIP1 (TCIP1) is a potent BCL6-BRD4 transcriptional/epigenetic chemical inducer of proximity (TCIP) by covalently linking BCL6 binder BI-3812 to BRD4 ligand JQ1, selectively kills DLBCL cells with EC50 of 1.3 nM against KARPAS422 cell.
TCIP1 rapidly and robustly killed other DLBCL lines with high levels of BCL6, but JQ1 and BI3812 separately or together shows100–1,000-fold less-effective cell killing.
TCIP1 is 200–10,000-fold more potent in killing DLBCL cells than the degradation of BRD4 by dBET1 and/or degradation of BCL6 by BI3802.
TCIP1 induces a stable, cooperative protein-protein interaction between bromodomain 1 (BD1) of BRD4 and the BTB domain of BCL6.
TCIP1 shows affinity for intracellular ternary complex of BRD4 with Kd of 340 nM in TR-FRET assays.
TCIP1 induces G1/S and G2/M block in the cell cycle, TCIP1 (10 nM) represses MYC and its targets while activating pro-apoptotic genes in KARPAS422 cells.
TCIP1 kills diffuse large B cell lymphoma cell lines, including chemotherapy-resistant, TP53-mutant lines, at EC50 of 1-10 nM in 72 h and exhibits cell-specific and tissue-specific effects, capturing the combinatorial specificity inherent to transcription. |
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| DC72902 |
ARD-2051 |
ARD-2051 is a potent and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 can be used for the research of prostate cancer. |
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| DC65680 |
Lipid 2-10
Featured
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Lipid 2-10, an ionizable lipid with a pKa of 6.16, is utilized in the formulation of lipid nanoparticles (LNPs) featuring a bilayer structure. |
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| DC60510 |
Iso-A11B5C1
Featured
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Iso-A11B5C1 is an ionizable lipid. The iso-A11B5C1 LNP demonstrates a high level of muscle-specific mRNA delivery efficiency. exhibiting transfection efficiency comparable to the commercially available lipid SM-102, while considerably reducing inadvertent mRNA expression in main organs such as the liver and spleen.Additionally, study results show that intramuscular administration of mRNA formulated with iso-A11B5C1 LNP caused potent cellular immune responses, even with limited expression observed in lymph nodes. |
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| DC60530 |
BTK-IN-24(NX-5948)
Featured
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NX-5948,be also known as BTK-IN-24,is an oral BTK degrader.
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| DC65810 |
KT-333
Featured
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KT-333 is a first-in-class molecular glue that induces selective degradation of STAT3 via the ubiquitin-proteasome system by simultaneously engaging STAT3 and the VHL E3 ligase. This novel mechanism enables potent STAT3 depletion with minimal off-target effects, demonstrating strong anti-tumor activity in hematologic malignancies. |
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| DC74301 |
NX-1607
Featured
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NX-1607 (Compound 23) is an inhibitor of Cbl-b, an E3 enzyme in the ubiquitin-proteasome pathway, with an IC50 value of less than 1 nM. NX-1607 can be used in cancer research. |
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