Cancer Targeted Therapy

AG957 (Standard) is the analytical standard of AG957. This product is intended for research and analytical applications. AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity. AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210bcr/abl autokinase activity.

5-Iodo-indirubin-3'-monoxime (Standard) is the analytical standard of 5-Iodo-indirubin-3'-monoxime (HY-111930). This product is intended for research and analytical applications. 5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the K_inase, with IC₅₀s of 9, 20 and 25 nM, respectively.

Aliskiren (hemifumarate) (Standard) is the analytical standard of Aliskiren (hemifumarate). This product is intended for research and analytical applications. Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hemifumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.

Mitoxantrone (Standard) is the analytical standard of Mitoxantrone. This product is intended for research and analytical applications. Mitoxantrone is a potent topoisomerase II inhibitor. Mitoxantrone also inhibits protein kinase C (PKC) activity with an IC₅₀ of 8.5 μM. Mitoxantrone induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone shows antitumor activity. Mitoxantrone also has anti-orthopoxvirus activity with EC₅₀s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.

TDP-665759 is an inhibitor for HDm2:p53 complex, and thus activates p53, inhibits STAT3 signaling pathway (EC₅₀ of 5.90 μM) and the cell viability of p53 expressing A549R (IC₅₀ of 7.02 μM). TDP-665759 induces apoptosis in HepG2. TDP-665759 exhibits antitumor efficacy in mouse models.

Tolterodine tartrate-d₁₄ (Kabi-2234-d₁₄) is deuterium labeled Tolterodine tartrate. Tolterodine ((R)-(+)-Tolterodine) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine can be used for the research of urinary tract infections and overactive bladder.

Lys-SMCC-DM1 (Standard) is the analytical standard of Lys-SMCC-DM1 (HY-101982). This product is intended for research and analytical applications. Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) is a agent-linker conjugates for ADC that can inhibit tubulin polymerization. Lys-SMCC-DM1 is the active metabolite of T-DM1. T-DM1 is a HER2-targeting ADC with a tubulin polymerization inhibitor DM1. Lys-SMCC-DM1 can be used in the research of breast cancer.

CRBN ligand-853 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-853 can be linked to a target protein ligand via a linker to form a PROTAC.

RGFP966 (Standard) is the analytical standard of RGFP966 (HY-13909). This product is intended for research and analytical applications. RGFP966 is a highly selective HDAC3 inhibitor with an IC₅₀ of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).

8-Bromo-cAMP (Standard) is the analytical standard of 8-Bromo-cAMP (HY-12306A). This product is intended for research and analytical applications. 8-Bromo-cAMP (8-Br-Camp), a cyclic AMP analog, is an activator of cyclic AMP-dependent protein K_inase (PKA). 8-Bromo-cAMP has anti-proliferative and apoptotic effects against cancer cells.

AKT-IN-26 (Compound 453) is an AKT inhibitor that binds to the Pleckstrin homology (PH) domain of AKT. AKT-IN-26 can be used in research related to AKT pathway-associated cell proliferation and cancer.

Arbutin-d₄ is deuterium labeled Arbutin. Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with K_iapp values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties.

TX1-85-1 (Standard) is the analytical standard of TX1-85-1 (HY-100848). This product is intended for research and analytical applications. TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.

CRBN ligand-443 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-443 can be linked to a target protein ligand via a linker to form a PROTAC.

Doramapimod (Standard) is the analytical standard of Doramapimod. This product is intended for research and analytical applications. Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM.

CRBN ligand-758 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-758 can be linked to a target protein ligand via a linker to form a PROTAC.

ZEN-3219 (Standard) is the analytical standard of ZEN-3219 (HY-111977). This product is intended for research and analytical applications. ZEN-3219 is a BET inhibitor with IC₅₀s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4.

PCSK9-IN-32 (compund 8) is a PCSK9[1:33]-GFP translation inhibitor.

CTS-1027 (Standard) is the analytical standard of CTS-1027 (HY-10398). This product is intended for research and analytical applications. CTS-1027 is a potent small molecule inhibitor of MMPs, with IC₅₀s of 0.3 nM, 0.5 nM for MMP2, MMP13, respectively, and has > 1,000 fold selectivity over MMP1.

CRBN ligand-773 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-773 can be linked to a target protein ligand via a linker to form a PROTAC.