Cancer Targeted Therapy

CRBN ligand-822 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-822 can be linked to a target protein ligand via a linker to form a PROTAC.

Fmoc-NH-CH2-PEG3-C2-NH2 (hydrochloride) is a PROTAC linker that can be used in the synthesis of PROTACs.

Ataluren-¹³C₆ (PTC124-¹³C₆) is ¹³C labeled Ataluren. Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.

Tacedinaline (Standard) is the analytical standard of Tacedinaline. This product is intended for research and analytical applications. Tacedinaline (N-acetyldinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively.

Tert-butyl 3-(((methylsulfonyl)oxy)methyl)azetidine-1-carboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.

TM-233 is an inhibitor of the JAK/STAT and NF-κB signaling pathways, exhibiting significant antitumor activity. TM-233 reduces the expression of the anti-apoptotic protein Mcl-1 by inhibiting the phosphorylation of JAK2 and STAT3, and regulates its transcription by directly binding to the Mcl-1 gene promoter. Additionally, TM-233 prevents the translocation of NF-κB from the cytoplasm to the nucleus by inhibiting its DNA-binding activity, thereby reducing nuclear NF-κB expression. TM-233 shows potential in overcoming Bortezomib (HY-10227) resistance and can be applied in research related to multiple myeloma.

CRBN ligand-461 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-461 can be linked to a target protein ligand via a linker to form a PROTAC.

AKT-I-1 is a selective inhibitor of Akt1, with an IC₅₀ of 4.6 µM.

Carboxyamidotriazole (Standard) is the analytical standard of Carboxyamidotriazole. This product is intended for research and analytical applications. Carboxyamidotriazole (L-651582) is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole shows anti-tumor, anti-inflammatory and antiangiogenic effects.

Samuraciclib hydrochloride (Standard) is the analytical standard of Samuraciclib hydrochloride (HY-103712A). This product is intended for research and analytical applications. Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC₅₀ of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects.

CRBN ligand-710 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-710 can be linked to a target protein ligand via a linker to form a PROTAC.

4-Methoxycinnamic acid ethyl ester (Ethyl p-methoxycinnamate) is an orally active natural compound found. 4-Methoxycinnamic acid ethyl ester exerts anti-inflammatory effects by inhibiting cyclooxygenase (COX-1 (IC₅₀ = 1.12 μM) and COX-2 (IC₅₀ = 0.83 μM)), NF-κB (IC₅₀ = 88.7 μM) and cytokine production (TNF-α (IC₅₀ = 96.84 μg/mL) and IL-1β (IC₅₀ = 166.4 μg/mL)). 4-Methoxycinnamic acid ethyl ester inhibits tumor cell proliferation, migration and cancer metabolism and induces apoptosis.4-Methoxycinnamic acid ethyl ester inhibits VEGF expression, thereby inhibiting angiogenesis. 4-Methoxycinnamic acid ethyl ester has a significant inhibitory effect on dengue virus and Mycobacterium tuberculosis. 4-Methoxycinnamic acid ethyl ester has analgesic effects in rats.

TWS119 (Standard) is the analytical standard of TWS119. This product is intended for research and analytical applications. TWS119 is a specific inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway.

SB-505124 (Standard) is the analytical standard of SB-505124. This product is intended for research and analytical applications. SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

NH2-spiro[3.3]heptane-methyl formate is a PROTAC linker that can be used in the synthesis of PROTACs.

CRBN ligand-840 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-840 can be linked to a target protein ligand via a linker to form a PROTAC.

tert-Butyl 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoyl)piperazine-1-carboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.

CB 3703 is an inhibitor of thymidylate synthase (TS) and dihydrofolate reductase (DHFR). CB 3703 has an IC₅₀ of 0.25 μM against rat TS, a K_i of 0.47 μM against mouse TS, an IC₅₀ of 6.8 nM against rat DHFR, and a K_i of 0.6 pM against mouse DHFR. CB 3703 is transported via the reduced folate pathway, has a short plasma half-life, and can prolong the survival of tumor-bearing mice. CB 3703 can be used in the research of L1210 ascites tumors.

SB-699551 (Standard) is the analytical standard of SB-699551 (HY-103100). This product is intended for research and analytical applications. SB-699551 is a potent and selective 5-HT5A antagonist with a K_i value of 5.1 μM. SB-699551 increases the phosphorylation levels of CREB and ATF1, and decreases the phosphorylation levels of AKT, PRAS40, P70S6K, FOXO1, and S6RP. SB-699551 improves drug-induced cognitive deficits. SB-699551 improves social withdrawal and forgetfulness. SB-699551 inhibits breast cancer.

cis-3-(Aminomethyl)cyclobutanol hydrochloride is a PROTAC linker that can be used in the synthesis of PROTACs.