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Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment . Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Agrimol B, a polyphenol, is an orally active and potent SIRT1 activator. Agrimol B shows anti-adipogenic and anticancer activity. Agrimol B shows antibacterial activity against plant pathogens. Agrimol B dramatically inhibits 3T3-L1 adipocyte differentiation by reducing PPARγ, C/EBPα, FAS, UCP-1, and apoE expression. The action of Agrimol B on the cancer cells is likely derived from its effect on c-MYC, SKP2 and p27 .
GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors .
TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation. SZL P1-41, like Skp2 deficiency, augments p27-mediated apoptosis/senescence, while it impairs Akt-driven glycolysis. Anti-tumor activities .
NSC139021 (ERGi-USU) is a RIOK2 inhibitor with anticancer activity. RIOK2 can highly selectively inhibit the growth of ERG-positive cancer cells with IC50s of 30-400 nM against cell lines. RIOK2 also causes cell cycle arrest and apoptosis in glioblastoma via induction of Skp2 and Skp2-p27/p21-Cyclin E/CDK2-pRb signaling .
KW-2478 is an HSP90 inhibitor (IC50 = 3.8 nM). KW-2478 inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 downregulates STAT3 expression. KW-2478 may be used in research on cancers such as CML and liver cancer .
SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells .
p27 Analogue CP2 is a macrocyclic peptide inhibitor targeting the Cks1-Skp2-Skp1 complex (Kd = 32 nM). p27 Analogue CP2 blocks SCFSkp2/Cks1-mediated ubiquitylation and degradation of p27, restoring p27 levels and inhibiting cell proliferation. p27 Analogue CP2 is promising for research of cancers dependent on Skp2 overexpression such as breast cancer .
TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne witha variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .
NSC689857 is a potent EGFR and SCF SKP2 inhibitor with an IC50 value of 36 μM for Skp2-Cks1. NSC689857 can inhibit p27 ubiquitylation (IC50=30 μM). NSC689857 has varied activity across cancer types, with more activity against leukemia cell lines than others .
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .
CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27Kip1, as confirmed by dose-response analysis.
Ubiquitination-IN-1 (compound 24) is a ubiquitination and Cksl-Skp2 protein-protein interaction (IC50=0.17 μM) inhibitor. Ubiquitination-IN-1 increases levels of p27. Ubiquitination-IN-1 has the potential for treatment disease by blocking the degradation of tumor suppressors .
PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α .
SJ572403 (SJ403) is a p27Kip1 inhibitor. SJ572403 has high specificity for specific regions within the D2 subdomain of p27-KID with a Kd value of 2.2 mM. SJ572403 can be used for the research of diseases associated with intrinsically disordered proteins (IDPs) .
WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2 .
Brilliant Blue G-250 is a dye commonly used for the visualization of proteins separated by SDS-PAGE, offering a simple staining procedure and high quantitation. In the Bradford protein assay, protein concentrations are determined by the absorbance at 595 nm due to the binding of Brilliant Blue G-250 to proteins. Brilliant Blue G-250 is a safe highly selective P2×7R antagonist with promising consequent inactivation of NLRP3 inflammasome .
Pim-1/2 kinase inhibitor 1 is an orally active pim-1/2 kinase inhibitor. Pim-1/2 kinase inhibitor 1 blocks the ability of Pim kinases to phosphorylate peptides, and inhibits the pim protein kinase directed phosphorylation of 4E-BP1 and p27Kip1. Pim-1/2 kinase inhibitor 1 can be used in study of cancer, especially prostate cancer .
Pro-GA is a γ-glutamyl cyclotransferase (GGCT) inhibitor. Pro-GA inhibits the enzymatic activity of GGCT, disrupts glutathione homeostasis, induces the production of mitochondrial ROS, and upregulates the expression of p21, p27 and p16 in cells. Pro-GA inhibits the growth of cancer cells, induces cell cycle arrest and cellular senescence. Pro-GA exerts anti-tumor effects in breast cancer xenograft mouse models. Pro-GA can be used in research related to bladder cancer and breast cancer .
GGTI-2417 is a potent and selective inhibitor of GGTase I. GGTI-2417 inhibits the Cdk2-mediated phosphorylation of p27Kip1 at Thr187 and accumulates p27Kip1 in the nucleus. GGTI-2417 also induces breast cancer cell apoptosis .
Coelonin is a dihydrophenanthrene with anti-inflammation activity. Coelonin inhibits LPS-induced PTEN phosphorylation. Coelonin inhibits NF-κB activation and p27Kip1 degradation by regulating the PI3K/AKT pathway negatively. Coelonin can inhibit IκBα phosphorylation and degradation and increases the expression of IκBα protein .
Tyroserleutide hydrochloride is a tripeptide isolated from the degradation products of porcine spleen with antitumor activity. Tyroserleutide hydrochloride can upregulate the expression of the tumor suppressor gene PTEN and inhibit the activity of AKT and PDK1. Tyroserleutide hydrochloride inhibits tumor cell proliferation and MDM2 phosphorylation by inhibiting the PI3K/AKT pathway, and also upregulates P21, P27, P53, and induces mitochondrial damage and cell apoptosis .
IFI27 Human Pre-designed siRNA Set A contains three designed siRNAs for IFI27 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UR-1505 is a nuclear factor of activated T cells (NF-AT) inhibitor. UR-1505 can suppress CD3/CD28 induced T cell proliferation, increase p27KIP levels, and induce G1/S cell cycle arrest. UR-1505 can also inhibit the production of IL-5 and IFN-γ in activated T cells. UR-1505 has immunomodulatory properties and can be used in the study of atopic dermatitis .
KW-2478 hydrochloride is an HSP90 inhibitor (IC50 = 3.8 nM). KW-2478 hydrochloride inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 hydrochloride weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 hydrochloride downregulates STAT3 expression. KW-2478 hydrochloride may be used in research on cancers such as CML and liver cancer .
RL71 is a curcuminoid anticancer agent that exhibits potent cytotoxicity against a variety of ER-negative breast cancer cells. RL71 (1 μM) induces cell cycle arrest in the G2/M phase and induces apoptosis in SKBr3 cells. RL7 also decreases HER2/neu phosphorylation and increases p27. RL71 also significantly reduced the phosphorylation of Akt and transiently increased the stress kinases JNK1/2 and p38 MAPK. Furthermore, RL71 exhibited anti-angiogenic potential in vitro, inhibiting the migration of HUVEC cells and the ability of these cells to form tubular networks .
Caudatin (Standard) is the analytical standard of Caudatin (HY-N1983). This product is intended for research and analytical applications. Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne witha variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .
Cdkn1b Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdkn1b gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
MEK-IN-9 (Compound 4-82) is a MEK inhibitor. MEK-IN-9 induces p15 and p27 protein. MEK-IN-9 can be used in the research of renal adenocarcinoma and colorectal cancer .
CEP1612 is a dipeptidyl proteasome inhibitor with the IC50 of 60 nM. CEP1612 induces p21(WAF1)and p27(KIP1) expression and cell apoptosis. CEP1612 shows anticancer activity in vivo .
Argyrin A, a cyclical peptide, is a potent antitumoral agent. Argyrin A exerts its effects through a potent inhibition of the proteasome. Argyrin A leads to increased endogenous p27kip1 levels by preventing protein turnover .
VDR agonist 1 (compound 28) is a nonsteroidal Vitamin D receptor (VDR) agonist, with an IC50 of 690 nM in MCF-7 cells. VDR agonist 1 arrests the cell cycle through the up-regulation of p21 and p27, promotes apoptosis by increasing the expression of BAX and decrease the expression of Bcl-2 .
WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2 .
P18IN005 hydrochloride is a novel inhibitor of p18, exhibiting potent activity in negatively regulating haematopoietic stem cell (HSC) self-renewal. P18IN005 hydrochloride has been shown to be more effective than p27 in inhibiting HSC self-renewal in mouse models. P18IN005 hydrochloride promotes the expansion of functional HSCs in short-term cultures. P18IN005 hydrochloride serves as a valuable tool for dissecting the signaling pathways involved in stem cell self-renewal.
Aurora kinase-IN-1 (Compound 9) is a potent inhibitor of aurora kinase. Aurora kinase-IN-1 upregulates the expression of G1 cell cycle inhibitory proteins including p21 and p27, and G1 progressive cyclin D1, and downregulates G1-to-S progressive cyclins, resulting in cell cycle arrest at the G1/S boundary. Aurora kinase-IN-1 also induces apoptosis. Aurora kinase-IN-1 is a lead compound for chemotherapeutic agents .
9-cis-UAB30 is a rexinoid agonist. 9-cis-UAB30 significantly decreases the proliferation, viability, and motility of both patient-derived xenografts (PDXs). 9-cis-UAB30 induced cell-cycle arrest as demonstrated by the significant increase in the percentage of cells in G1 and a decrease in the percentage of cells in S phase by downregulating SKP2 and/or 20S proteasome activity, which leads to increased p27kip1 protein stability. 9-cis-UAB30 downregulates the abundance of stem cell marker mRNAs (Oct4, Nanog, Sox2, nestin) and upregulates the abundance of differentiation marker mRNAs (β3-tubulin, NSE, HOXC9, GAP43). 9-cis-UAB30 has no adverse effects on the central nervous system and cardiovascular system at the tested dose. 9-cis-UAB30 can be used for the study of neuroblastoma, cutaneous T-cell lymphomas, and breast cancer .
CP2-CPP is a conjugate of p27 Analogue CP2 (HY-P11020) and Antennapedia Peptide (HY-P0307). CP2-CPP crosses cell membranes and localizes to live cell cytosol. CP2-CPP blocks SCF Skp2/Cks1-p27 interaction to inhibit p27 ubiquitination and degradation, restoring p27 levels and inhibiting cell proliferation. CP2-CPP can be used for the research of cancer, such as breast cancer .
RL71-d6 is a deuterium labeled RL71 (HY-121605). RL71 is a curcuminoid anticancer agent that exhibits potent cytotoxicity against a variety of ER-negative breast cancer cells. RL71 (1 μM) induces cell cycle arrest in the G2/M phase and induces apoptosis in SKBr3 cells. RL7 also decreases HER2/neu phosphorylation and increases p27. RL71 also significantly reduced the phosphorylation of Akt and transiently increased the stress kinases JNK1/2 and p38 MAPK. Furthermore, RL71 exhibited anti-angiogenic potential in vitro, inhibiting the migration of HUVEC cells and the ability of these cells to form tubular networks .
ALK/PI3K/AKT-IN-1 (Compound 45) inhibits the proliferation of cancer cell A549, H1975 and PC9 with an IC50 of 0.44, 0.83 and 1.51 μM. ALK/PI3K/AKT-IN-1 increases the expression of p21 and p27, inhibits the activity of CDK2 and p-Rb, arrests the cell cycle at G1 phase. ALK/PI3K/AKT-IN-1 inhibits the ALK/PI3K/AKT signaling pathway, promotes the depolarization of mitochondrial membrane potential, and inducing apoptosis in A549 cell. ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheroids .
Apoptosis inducer 50 (Compound 5e) is an apoptosis inducer as well as an autophagy inducer agent. Apoptosis inducer 50 exhibits potent and selective anti-cancer activity against triple-negative breast cancer cells and metastatic colon cancer cells. Apoptosis inducer 50 upregulates the expression of pro-apoptotic proteins (Bax, Bim, cleaved Caspase-9) and downregulates the expression of the anti-apoptotic protein (BCL-XL). Apoptosis inducer 50 upregulates key autophagy markers such as Beclin-1 and ATG5, and enhances the conversion of LC3-I to LC3-II., Apoptosis inducer 50 arrests cancer cells in the G1/S phase by upregulating the expression of p21 and p27 while downregulating Cyclin D1. Apoptosis inducer 50 increases the level of ROS .
PI3Kα-IN-28 (Compound 23) is an efficient dual targeted PI3K/BRD4 inhibitor. PI3Kα-IN-28 can inhibit the proliferation of various cells, such as KYSE180 and KYSE450 cells. PI3Kα-IN-28 can concentration dependently inhibit migration and colony formation, induce G0/G1 phase arrest, significantly inhibit DNA synthesis, and significantly increase the proportion of senescent cells. PI3Kα-IN-28 can inhibit the expression of p-AKT and c-Myc and activate the AMPK-p27 pathway. PI3Kα-IN-28 can be used for research on cancers such as esophageal cancer .
PSMD9 Human Pre-designed siRNA Set A contains three designed siRNAs for PSMD9 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Dctn6 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Dctn6 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
DCTN6 Human Pre-designed siRNA Set A contains three designed siRNAs for DCTN6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cdkn1b Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdkn1b gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
TMED7 Human Pre-designed siRNA Set A contains three designed siRNAs for TMED7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Methoxyfenoterol is a β2-adrenergic receptor agonist. Methoxyfenoterol stimulates intracellular cAMP accumulation, inhibits tumor cell proliferation, induces G1 cell cycle arrest, upregulates cyclin-dependent kinase inhibitor p27, downregulates cyclin D1 and cyclin A, and inhibits Akt phosphorylation. Methoxyfenoterol crosses the blood-brain barrier and inhibits growth of astrocytoma xenografts. Methoxyfenoterol can be used for the research of astrocytoma, glioblastoma .
Pralatrexate (Standard) is the analytical standard of Pralatrexate. This product is intended for research and analytical applications. Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment . Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Argyrin F a cyclic peptide with antitumoral activities. Argyrin F inhibits cell proliferation, migration, invasion and colony formation by partial induction of apoptosis and epithelial-mesenchymal transition (EMT). Argyrin F stabilizes p27kip, up-regulated p21 waf1/cip1 and depletes COX2. Argyrin F can be used for the study of pancreatic ductal adenocarcinoma (PDAC) .
SZL P1-41 (Standard) is the analytical standard of SZL P1-41 (HY-100237). This product is intended for research and analytical applications. SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation. SZL P1-41, like Skp2 deficiency, augments p27-mediated apoptosis/senescence, while it impairs Akt-driven glycolysis. Anti-tumor activities .
Americanin A is a Neolignan. Americanin A can be isolated from the seeds of Phytolacca americana. Americanin A activates ATM and ATR, initiating the subsequent signal transduction cascades that include Chk1, Chk2, and tumor suppressor p53. Americanin A targets selectively Skp2 for degradation and thereby stabilizesp27. Americanin A suppresses the activity of Cyclin B1 and its partner cdc2 to prevent entry into Mitosis. Americanin A induces Apoptosis by producing excessive ROS. Americanin A has anti-cancer activity against colorectal cancer .
EGFR-IN-187 (Compound 4d) is a selective EGFR inhibitor with an IC50 of 25.41 μM. EGFR-IN-187 can cause cancer cells S amd G2/M phase arrest and induce apoptosis and autophagy. EGFR-IN-187 upregulates CCNE1, Bax, LC3B-II and P27 expression and downregulates CCNA1 and Bcl-2 levels. EGFR-IN-187 can be used for the research of cancer, such as lung cancer .
MHY219 is a histone deacetylase (HDAC) inhibitor with an IC50 of 0.276 μM. MHY219 inhibits total HDAC enzyme activity, increases histone H3 and H4 hyperacetylation. MHY219 induces cance cells phase arrest, apoptosis and inhibits proliferationin. MHY219 increases cleavage of PARP, Bax, cytochrome c levels, androgen receptor expression and decreases Bcl-2 expression. MHY219 can be used for the research of prostate cancer .
CSN5-IN-3 (Compound 30) is a CSN5 inhibitor with an IC50 of 0.58 μM. CSN5-IN-3 inhibits the enzymatic activity of CSN5, leading to increased accumulation of NEDD8-Cul1 and promoting the degradation of PD-L1. CSN5-IN-3 downregulates Bcl-2, and upregulates P53 and Cleaved caspase-3. CSN5-IN-3 exhibits anticancer activity against triple-negative breast cancer .
N-Palmitoyl-D-glucosamine is an orally active TLR4 antagonist. N-Palmitoyl-D-glucosamine stably binds MD-2 with, preventing LPS-induced NF-κB signaling, decreases pro-inflammatory cytokines (IL-1β, TNF-α, and IL-6), increases anti-inflammatory IL-10 and IL-1rα, and normalizes miR-20a-5p, miR-106a-5p, and miR-27a-3p levels. N-Palmitoyl-D-glucosamine decreases allodynia and prevents myelino-axonal degeneration of peripheral nerves. N-Palmitoyl-D-glucosamine can be used for the researches of keratitis and peripheral neuropathy .
Brilliant Blue G-250 is a dye commonly used for the visualization of proteins separated by SDS-PAGE, offering a simple staining procedure and high quantitation. In the Bradford protein assay, protein concentrations are determined by the absorbance at 595 nm due to the binding of Brilliant Blue G-250 to proteins. Brilliant Blue G-250 is a safe highly selective P2×7R antagonist with promising consequent inactivation of NLRP3 inflammasome .
Brilliant Blue G-250 is a dye commonly used for the visualization of proteins separated by SDS-PAGE, offering a simple staining procedure and high quantitation. In the Bradford protein assay, protein concentrations are determined by the absorbance at 595 nm due to the binding of Brilliant Blue G-250 to proteins. Brilliant Blue G-250 is a safe highly selective P2×7R antagonist with promising consequent inactivation of NLRP3 inflammasome .
p27 Analogue CP2 is a macrocyclic peptide inhibitor targeting the Cks1-Skp2-Skp1 complex (Kd = 32 nM). p27 Analogue CP2 blocks SCFSkp2/Cks1-mediated ubiquitylation and degradation of p27, restoring p27 levels and inhibiting cell proliferation. p27 Analogue CP2 is promising for research of cancers dependent on Skp2 overexpression such as breast cancer .
Tyroserleutide hydrochloride is a tripeptide isolated from the degradation products of porcine spleen with antitumor activity. Tyroserleutide hydrochloride can upregulate the expression of the tumor suppressor gene PTEN and inhibit the activity of AKT and PDK1. Tyroserleutide hydrochloride inhibits tumor cell proliferation and MDM2 phosphorylation by inhibiting the PI3K/AKT pathway, and also upregulates P21, P27, P53, and induces mitochondrial damage and cell apoptosis .
CP2-CPP is a conjugate of p27 Analogue CP2 (HY-P11020) and Antennapedia Peptide (HY-P0307). CP2-CPP crosses cell membranes and localizes to live cell cytosol. CP2-CPP blocks SCF Skp2/Cks1-p27 interaction to inhibit p27 ubiquitination and degradation, restoring p27 levels and inhibiting cell proliferation. CP2-CPP can be used for the research of cancer, such as breast cancer .
Agrimol B, a polyphenol, is an orally active and potent SIRT1 activator. Agrimol B shows anti-adipogenic and anticancer activity. Agrimol B shows antibacterial activity against plant pathogens. Agrimol B dramatically inhibits 3T3-L1 adipocyte differentiation by reducing PPARγ, C/EBPα, FAS, UCP-1, and apoE expression. The action of Agrimol B on the cancer cells is likely derived from its effect on c-MYC, SKP2 and p27 .
Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne witha variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer .
Coelonin is a dihydrophenanthrene with anti-inflammation activity. Coelonin inhibits LPS-induced PTEN phosphorylation. Coelonin inhibits NF-κB activation and p27Kip1 degradation by regulating the PI3K/AKT pathway negatively. Coelonin can inhibit IκBα phosphorylation and degradation and increases the expression of IκBα protein .
Caudatin (Standard) is the analytical standard of Caudatin (HY-N1983). This product is intended for research and analytical applications. Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne witha variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .
Argyrin A, a cyclical peptide, is a potent antitumoral agent. Argyrin A exerts its effects through a potent inhibition of the proteasome. Argyrin A leads to increased endogenous p27kip1 levels by preventing protein turnover .
Argyrin F a cyclic peptide with antitumoral activities. Argyrin F inhibits cell proliferation, migration, invasion and colony formation by partial induction of apoptosis and epithelial-mesenchymal transition (EMT). Argyrin F stabilizes p27kip, up-regulated p21 waf1/cip1 and depletes COX2. Argyrin F can be used for the study of pancreatic ductal adenocarcinoma (PDAC) .
Americanin A is a Neolignan. Americanin A can be isolated from the seeds of Phytolacca americana. Americanin A activates ATM and ATR, initiating the subsequent signal transduction cascades that include Chk1, Chk2, and tumor suppressor p53. Americanin A targets selectively Skp2 for degradation and thereby stabilizesp27. Americanin A suppresses the activity of Cyclin B1 and its partner cdc2 to prevent entry into Mitosis. Americanin A induces Apoptosis by producing excessive ROS. Americanin A has anti-cancer activity against colorectal cancer .
N-Palmitoyl-D-glucosamine is an orally active TLR4 antagonist. N-Palmitoyl-D-glucosamine stably binds MD-2 with, preventing LPS-induced NF-κB signaling, decreases pro-inflammatory cytokines (IL-1β, TNF-α, and IL-6), increases anti-inflammatory IL-10 and IL-1rα, and normalizes miR-20a-5p, miR-106a-5p, and miR-27a-3p levels. N-Palmitoyl-D-glucosamine decreases allodynia and prevents myelino-axonal degeneration of peripheral nerves. N-Palmitoyl-D-glucosamine can be used for the researches of keratitis and peripheral neuropathy .
The CDKN1B protein is a key cell cycle regulator that inhibits CDK2 when bound to cyclin A, thereby inhibiting G1 phase progression. It exhibits significant inhibitory effects on cyclin E- and cyclin A-CDK2 complexes. CDKN1B Protein, Human (His) is the recombinant human-derived CDKN1B protein, expressed by E. coli , with N-6*His labeled tag.
C11orf59; LAMTOR1; Late endosomal/lysosomal adaptor and MAPK and MTOR activator 1; Lipid raft adaptor protein p18; LTOR1_HUMAN; p18; P27Kip1-releasing factor from RhoA; P27RF-Rho; PDRO; PP7157; Protein associated with DRMs and endosomes; Ragulator complex protein LAMTOR1; ragulator complex protein PDRO; Ragulator1; RhoA activator C11orf59
The LAMTOR1 protein is an important component of the Ragulator complex and plays dual roles in amino acid sensing and mTORC1 activation. It acts as a guanine nucleotide exchange factor (GEF) for Rag GTPases and mediates their recruitment to the lysosomal membrane. LAMTOR1 Protein, Human (His) is the recombinant human-derived LAMTOR1 protein, expressed by E. coli , with N-His labeled tag.
RL71-d6 is a deuterium labeled RL71 (HY-121605). RL71 is a curcuminoid anticancer agent that exhibits potent cytotoxicity against a variety of ER-negative breast cancer cells. RL71 (1 μM) induces cell cycle arrest in the G2/M phase and induces apoptosis in SKBr3 cells. RL7 also decreases HER2/neu phosphorylation and increases p27. RL71 also significantly reduced the phosphorylation of Akt and transiently increased the stress kinases JNK1/2 and p38 MAPK. Furthermore, RL71 exhibited anti-angiogenic potential in vitro, inhibiting the migration of HUVEC cells and the ability of these cells to form tubular networks .
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment . Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
IFI27 Human Pre-designed siRNA Set A contains three designed siRNAs for IFI27 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cdkn1b Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdkn1b gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
PSMD9 Human Pre-designed siRNA Set A contains three designed siRNAs for PSMD9 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Dctn6 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Dctn6 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
DCTN6 Human Pre-designed siRNA Set A contains three designed siRNAs for DCTN6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cdkn1b Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdkn1b gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
TMED7 Human Pre-designed siRNA Set A contains three designed siRNAs for TMED7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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