68

Daporinad

68 Publications Verification

Cat. No.: HY-50876

CAS No.: 658084-64-1

Synonyms: FK866; APO866

Target:

NAMPT Autophagy Apoptosis mTOR p38 MAPK ERK

Research Areas:

Cancer

Daporinad (FK866) is a non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a K_i value of 0.3 nM. Daporinad depletes NAD+ and ATP levels, inhibits mTORC1 and MAPK/ERK pathways, and activates TFEB to induce autophagy. Daporinad causes the depletion of the endoplasmic reticulum Ca²⁺ pool, ultimately weakening the mitogen-induced Ca²⁺ signal and the activation and function of T cells. Daporinad induces cell cycle arrest and apoptosis, and inhibits cell proliferation. Daporinad can be used for the study of myeloma, liver cancer, and immunosuppression .

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8

SKI II

8 Cited Publications

Cat. No.: HY-13822

CAS No.: 312636-16-1

Purity: 99.25%

Target:

SphK Dihydroceramide Desaturase 1 (DES1) Apoptosis Reactive Oxygen Species (ROS) mTOR PERK Keap1-Nrf2

Research Areas:

Infection Neurological Disease Cancer

SKI-II is an orally active dual-target inhibitor of SphK1/2 and DES1, with K_i values of 16 µM and 0.3 µM against SphK1 and DES1, respectively. SKI-II activates the PERK-Nrf2 antioxidant pathway by stabilizing Nrf2, and synergizes with Temozolomide (HY-17364) to induce oxidative/endoplasmic reticulum stress and cancer cell death under hypoxic conditions. In vivo, SKI-II inhibits SphK activity, promotes ceramide accumulation and apoptosis, and synergizes with Cisplatin (HY-17394) to reverse drug resistance via the ras/MAPK pathway. SKI-II reduces measles virus replication by inhibiting mTORC1 activity. SKI-II binds to VCP to induce M1 polarization, enhances host tolerance to Staphylococcus aureus infection, and exerts radioprotective effects through Nrf2 activation and accelerated DNA repair. SKI-II can be used in research related to glioblastoma, acute myeloid leukemia, gastric cancer, measles virus infection, Staphylococcus aureus infection, and acute radiation syndrome .

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4

Nuvisertib

4 Cited Publications

Cat. No.: HY-101126

CAS No.: 1361951-15-6

Purity: 99.96%

Synonyms: TP-3654

Target:

Pim JAK mTOR c-Myc TGF-β Receptor BCRP

Research Areas:

Cancer

Nuvisertib (TP-3654) is an orally active second-generation pan-PIM kinase inhibitor with K_i values of 5 nM, 239 nM, and 42 nM against PIM-1, PIM-2, and PIM-3, respectively. Nuvisertib inhibits JAK-independent inflammatory and survival signaling pathways, reduces the production of proinflammatory cytokines, restores apoptotic sensitivity, inhibits mTORC1, MYC, and TGF-β signaling pathways, and decreases the expression of fibrosis markers. Nuvisertib selectively impairs the transport function of ABCG2, resensitizes multidrug-resistant cancer cells to cytotoxic drugs, and overcomes JAK2 inhibitor resistance. Nuvisertib can be used in research related to myelofibrosis, renal cell carcinoma, multidrug-resistant cancer, advanced solid tumors, urothelial carcinoma, and prostate adenocarcinoma .

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3

O6-Benzylguanine

3 Cited Publications

Cat. No.: HY-W002585

CAS No.: 19916-73-5

Target:

DNA Methyltransferase Apoptosis MDM-2/p53 p38 MAPK mTOR CDK PERK Caspase

Research Areas:

Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer

O6-Benzylguanine is an orally active, blood-brain barrier-penetrant inhibitor of O ⁶-methylguanine-DNA methyltransferase (MGMT/AGT). O6-Benzylguanine modulates p53 and its downstream p21 and cyclins to induce cell cycle arrest and apoptosis, and on the other hand activates mTORC1/MAPK and other signaling pathways to induce cellular senescence by inhibiting intracellular MGMT. O6-Benzylguanine is used in research related to various tumors, cellular senescence, and vascular smooth muscle dysfunction .

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3

Endoxifen (Z-isomer)

3 Cited Publications

Cat. No.: HY-18719

CAS No.: 112093-28-4

Target:

PKC Estrogen Receptor/ERR PI3K Akt mTOR Apoptosis Reactive Oxygen Species (ROS)

Research Areas:

Neurological Disease Cancer

Endoxifen Z-isomer is an orally active selective PKCβ1 inhibitor with an IC₅₀ of 360 nM against human PKCβ1. Endoxifen Z-isomer also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. Endoxifen Z-isomer can be used in research related to ER ⁺ breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .

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3

CCT007093

3 Cited Publications

Cat. No.: HY-15880

CAS No.: 176957-55-4

Purity: 98.34%

Target:

Phosphatase Apoptosis Autophagy

Research Areas:

Cancer

CCT007093 is an effective protein phosphatase 1D (PPM1D Wip1) inhibitor. Wip1 inhibition can activate the mTORC1 pathway and enhance hepatocyte proliferation after hepatectomy .

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3

Endoxifen (Z-isomer hydrochloride)

3 Cited Publications

Cat. No.: HY-18719A

CAS No.: 1032008-74-4

Target:

PKC Estrogen Receptor/ERR PI3K Akt mTOR Apoptosis Reactive Oxygen Species (ROS)

Endoxifen Z-isomer hydrochloride is an orally active selective PKCβ1 inhibitor with an IC₅₀ of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer hydrochloride binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer hydrochloride inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER ⁺ breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .

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