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PROTACs

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Cat. No. Product Name Field of Application Chemical Structure
DC80383 CBP/p300/BRD4 ligand-1
CBP/p300/BRD4 ligand-1 is a small-molecule inhibitor targeting CBP, p300, and BRD4. CBP/p300/BRD4 ligand-1 competitively binds to the functional domains of target proteins without disrupting key interactions. CBP/p300/BRD4 ligand-1 can be used for the construction of dual-target PROTAC degraders in studies related to prostate cancer and other cancers.
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DC80382 CBP/p300 ligand-Linker Conjugate 3
CBP/p300 ligand-Linker Conjugate 3 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for CBP/p300 and a PROTAC linker, which recruits E3 ligases. CBP/p300 ligand-Linker Conjugate 3 can be used for synthesis of PROTAC CBP/P300 Degrader-2.
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DC80379 Cbl-b-IN-29
Cbl-b-IN-29 is an orally active CBL-B inhibitor. Cbl-b-IN-29 binds to the CBL-B active pocket. Cbl-b-IN-29 induces Jurkat cell release IL-2 with an EC50 of 159 nM, effectively inhibiting the function of immune E3 ubiquitin ligase. Cbl-b-IN-29 demonstrates robust anti-tumor efficacy in vivo with good tolerability and no observed adverse reactions. Cbl-b-IN-29 can be used for cancer immunotherapy, colorectal cancer and immune-oncology combination research.
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DC80371 Carboxyatractyloside
Carboxyatractyloside (CATR) is a tight-binding inhibitor of adenine nucleotide translocase, and represents the major toxic component of Xanthium sibiricum. Carboxyatractyloside competes with ADP for binding to the translocase, blocks the translocation of ADP/ATP across the inner mitochondrial membrane, and thereby inhibits ADP-stimulated respiration. In the presence of Cyclosporin A, Carboxyatractyloside still induces permeability transition in liver mitochondria of aged rats, exhibiting significant hepatotoxicity and nephrotoxicity. Carboxyatractyloside is widely used in studies related to hepatotoxicity, nephrotoxicity and Alzheimer's disease.
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DC80370 Carbiphene
Carbiphene is a GABAA receptor allosteric modulator. Carbiphene inhibits [35S] TBPS binding and enhances [3H] muscimol binding on rat forebrain membranes, acting on specific GABAA receptor subsets. Carbiphene can be used in research related to schizophrenia.
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DC80366 CaMKII-IN-3
CaMKII-IN-3 (Example 321) is a CaMKII inhibitor with an IC50 of less than 10 nM. CaMKII-IN-3 can be used for the study of heart diseases.
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DC80365 CAD204520 dihydrochloride
CAD204520 dihydrochloride, a SERCA inhibitor (IC50 = 0.34 μM), targets mutated over wild type NOTCH1 proteins in T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL). CAD204520 dihydrochloride can be used for T-ALL and MCL research.
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DC80364 CAB7-3
CAB7-3 is an orally active HBV capsid assembly modulator (CAM). CAB7-3 exhibits an exceptional antiviral efficacy reducing HBV DNA with an EC50 = 70 nM, CC50 = 32.3 μM in HepDES19 cells. CAB7-3 exhibits significant anti-HBV activity in HBV-integrated HepDES19 (EC50 = 70 nM), HepAD38 (EC50 = 1 nM) and HBV-infected HLCZ01 cells (EC50 = 2 nM), respectively. CAB7-3 effectively reduces Hepatic HBV core protein levels and suppresses viral replication in vivo. CAB7-3 demonstrates a favorable drug-like and safety profile. CAB7-3 can be used for Hepatitis B Virus (HBV) research.
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DC80361 C14-Tri-LAN-Gly
C14-Tri-LAN-Gly is a highly selective and potent NOD1 agonist. C14-Tri-LAN-Gly activates NOD1. C14-Tri-LAN-Gly inhibits the expression of cleaved-caspase3. C14-Tri-LAN-Gly upregulates A20 expression. C14-Tri-LAN-Gly protects mice from lethal hepatitis by inhibiting hepatocyte Apoptosis. C14-Tri-LAN-Gly inhibits osteoblastogenesis and promots osteoclastogenesis.
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DC80346 BRL 34778
BRL 34778 is a potent, selective and orally active dopamine D2 receptor antagonist with a Ki of 2.14 nM. BRL 34778 exhibits antipsychotic activity with low activity for extrapyramidal effects and sedation. BRL 34778 can be used for the research of neurological disease, such as schizophrenia.
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DC80345 Brigimadlin enantiomer
Brigimadlin (BI 907828) enantiomer is the Brigimadlin enantiomer. Brigimadlin is an MDM2 inhibitor with anti-cancer activity.
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DC80340 BRD3 ligand-1
BRD3 ligand-1 is a target protein ligand that can be used for the synthesis of PROTACs, such as PROTAC BRD3 degrader-1.
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DC80326 BMS-442606
BMS-442606, the S-enantiomer of 6-hydroxybuspirone (6OHB), is an orally active 5-HT1A partial agonist. BMS-442606 can be used for generalized anxiety disorder (GAD) research.
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DC80325 BMS-181885
BMS-181885 is a selective 5-HT1 receptor agonist and a ligand for 5-HT1B/1D receptors. BMS-181885 exhibits anti-migraine activity. BMS-181885 can be used in the research of neurological diseases such as migraine.
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DC80324 BMS-159
BMS-159 is an orally active, direct phosphate prodrug of BMS-135. BMS-135 is a potent ATP-competitive inhibitor of CK2. BMS-159 can be used in the research of neurological disorders and tumors.
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DC80311 BILA 1906 BS
BILA 1906 BS is a HIV protease inhibitor. BILA 1906 BS prevents HIV-1 replication via inhibition of viral protease-mediated cleavage of Gag and Gag-Pol polyprotein precursors during virion maturation. BILA 1906 BS blocks maturation of p24 proteins in wild-type HIV-1, impairing polyprotein processing and viral maturation. BILA 1906 BS can be used for the research of human immunodeficiency virus type 1 (HIV-1) infection.
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DC80310 BI-135585 hydrate
BI-135585 hydrate is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC50 of 13 nM. BI-135585 hydrate exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 hydrate can be used for type 2 diabetes research.
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DC80309 BF-175
BF-175 is a selective SIRT1 agonist. BF175 increases SIRT1-mediated activation of PGC1-α, induces Apoptosis, induces Autophagy and inhibits SREBP activity. BF-175 protects against high glucose-mediated mitochondrial injury. BF-175 attenuates diabetic kidney disease progression. BF175 inhibits endometrial carcinoma.
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DC80307 Betamethasone succinate
Betamethasone succinate (NSSL-BMS) is a nano-formulation that can cross the blood-brain barrier. Betamethasone succinate is prepared by encapsulating the Betamethasone semi-succinate in PEG-liposomes. Betamethasone succinate utilizes the enhanced permeation and retention effects of liposomes to target and deliver the potent glucocorticoid to the inflammatory sites. Betamethasone succinate inhibits the secretion of pro-inflammatory cytokines (such as TNF-α and IL-6) while maintaining the level of anti-inflammatory cytokine TGF-β. Betamethasone succinate can be used in the research of arthritis and cerebral malaria.
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DC80300 BE2012
BE2012, SR8278 derivative, is a potent and selective REV-ERBα/β Antagonist with EC50 values of 0.285 and 0.346 μM. BE2012 binds to the ligand-binding domain (LBD) of REV-ERB, preventing the receptor from recruiting co-inhibitory factors and thereby releasing the transcriptional repression on downstream target genes. BE2012 can upregulate the expression of myogenic transcription factors Myf5 and Myod, promoting muscle regeneration and repair in acute muscle injury micemodels.
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DC80299 BCX-5
BCX-5 (PD 141955) is an orally active inhibitor of purine nucleoside phosphorylase (PNP) with a Ki of 0.08 μM. BCX-5 can inhibit cell proliferation and mixed lymphocyte reaction. BCX-5 can increase plasma inosine and guanosine levels. BCX-5 can be used for the research of immunology.
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DC80290 Aβ/tau aggregation-IN-4
Aβ/tau aggregation-IN-4 (Compound D21) is an Aβ/tau aggregation inhibitor. Aβ/tau aggregation-IN-4 promotes the degradation of Aβ40/42 (Aβ40, IC50 = 2.151 μM; Aβ42, IC50 = 3.622 μM). Aβ/tau aggregation-IN-4 shows selective AChE inhibition (IC50: 5.56 μM). Aβ/tau aggregation-IN-4 inhibits MAO-A and MAO-B with IC50s of 0.59 μM and 0.09 μM, respectively. Aβ/tau aggregation-IN-4 suppresses intracellular ROS levels. Aβ/tau aggregation-IN-4 can be used in the research of Alzheimer's disease.
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DC80289 Aβ aggregation-IN-4
Aβ aggregation-IN-4 can alleviate the neurotoxicity of amyloid-β protein (Aβ) and significantly reduce the level of oligomeric complexes of Aβ (Aβ-OCs). Aβ aggregation-IN-4 does not decrease the level of amyloid-β protein (Aβ). Aβ aggregation-IN-4 attenuates Aβ oligomerization and prevents oligomer-induced death of primary cortical neurons. Aβ aggregation-IN-4 can be used for the study of Alzheimer’s disease (AD).
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DC80288 Azimexon
Azimexon (BM 12.531) is an orally active immunomodulator with radioprotective and antitumor activities. Azimexon prolongs survival in multiple mouse models, enhances immunity and hematopoiesis, and alleviates radiation injury and tumor metastasis. Azimexon causes reversible hemolytic anemia in rats and dogs, and exerts therapeutic activity against adjuvant-induced arthritis in rats. Azimexon can be used for the research of lung carcinoma, leukemia, multiple myeloma, lung tumor, arthritis, breast cancer and AIDS‑related complex.
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DC80277 Autotaxin-IN-8
Autotaxin-IN-8 (Compound 14E) is an orally active Autotaxin inhibitor with an IC50 of 14.2 nM against hAutotaxin. Autotaxin-IN-8 inhibits Autotaxin activity, MAPK activation, LPAR1 and p-ERK1/2. Autotaxin-IN-8 reduces the phosphorylation levels of JNK and p38. Autotaxin-IN-8 decreases collagen deposition in a mouse model of pulmonary fibrosis. Autotaxin-IN-8 can be used in research related to pulmonary fibrosis.\n
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DC80267 AT-051/43421517
AT-051/43421517 is a cytoprotective agent and apoptosis inhibitor that binds to human phosphoglycerate kinase 1 (hPgk1). AT-051/43421517 protects cells from rotenone-induced cell death without inducing cell proliferation. AT-051/43421517 can be used for the research of parkinson’s disease.
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DC80261 Asciminib-NH2
Asciminib-NH2 is a BCR-ABL ligand and can be used for the synthesis of PROTACs, such as P19As.
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DC80257 Aromatase-IN-1
Aromatase-IN-1 is a competitive aromatase (P450arom) inhibitor with a human IC50 of 40 nM and a Ki of 1.05 nM. Aromatase-IN-1 binds via coordination of imidazole nitrogen to the heme iron of aromatase. Aromatase-IN-1 can be used for the research of breast cancer.
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DC80250 AR antagonist 17
AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC50 = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC).
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DC80244 AP-22161
AP22161 is a potent and selective Src SH2 domain inhibitor with an IC50 of 0.24 µM. AP22161 exhibits >120-fold selectivity over Yes SH2 (IC50 = 29.38 µM) and ZAP SH2 (IC50 = 421.86 µM). AP22161 inhibits Src-dependent cellular activity and diminishes osteoclast resorptive activity. AP22161 can be used for osteoporosis research.
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