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Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor [1].
Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
Trilaciclib (G1T28) hydrochloride is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib hydrochloride attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy [1].
Trilaciclib (G1T28) is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. . Trilaciclib can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy [1].
Aflatoxin G1 is one type of aflatoxins occuring in nature. It is produced by molds, such as Aspergillus flavus and Aspergillus parasiticus. Aflatoxins are hepatogenic, teratogenic, imunosuppressive, and carcinogenic fungal metabolites found in feeds, nuts, wine-grapes, spices, and other grain crops [1] .
Aflatoxin G1- 13C17 is the 13C labeled Aflatoxin G1 (HY-N6697) [1]. Aflatoxin G1 is one type of aflatoxins occuring in nature. It is produced by molds, such as Aspergillus flavus and Aspergillus parasiticus. Aflatoxins are hepatogenic, teratogenic, imunosuppressive, and carcinogenic fungal metabolites found in feeds, nuts, wine-grapes, spices, and other grain crops .
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 [1].
T2AA is a monoubiquitinated proliferating cell nuclear antigen (PCNA) inhibitor that prevents DNA repair, increases double-strand break (DSB) formation and promotes necroptosis and cell cycle arrest in G1 phase [1].
Kazusamycin B is an antibiotic that could be isolated from the fermentation broth of Streptomyces sp. No. 81-484. Kazusamycin B inhibits cell growth and arrests cell cycle at G1 phase. Kazusamycin B can be used in research of cancer [1] .
Ganoderic acid DM, a natural triterpenoid isolated from Ganoderma lucidum, induces DNA damage, G1 cell cycle arrest and apoptosis in human breast cancer cells. Ganoderic acid DM as a specific inhibitor of osteoclastogenesis [1] .
Dipyrithione is a potent antimicrobial agent. Dipyrithione shows antifungal activity and antiproliferative activity. Dipyrithione induces apoptosis and cycle arrest at G1 phase. Dipyrithione shows anti-inflammatory activity in vivo. Dipyrithione shows anti-tumor activity. Dipyrithione has the potential for the research of dermatophytosis [1] .
DNA topoisomerase II inhibitor 1 (compound 8ed) is a potent DNA topoisomerase II inhibitor. DNA topoisomerase II inhibitor 1 shows anti-proliferative activity. DNA topoisomerase II inhibitor 1 induces apoptosis and cell cycle arrest at sub G1 phase [1].
GSPT1degrader-1 (compound 9q) is a potent degrader of G1 to S phase transition 1 (GSPT1) via ubiquitin-proteasome system. GSPT1degrader-1 also induces cell G0/G1 phase arrest and apoptosis[1].
Cu(II)-Elesclomol is a Cu 2+ complex of Elesclomol (HY-12040). Cu(II)-Elesclomol induces cuproptosis. Cu(II)-Elesclomol also inducesapoptosis, causes a G1 cell cycle block and induces DNA double strand breaks in K562 cells. Cu(II)-Elesclomol also weakly inhibits DNA topoisomerase I. Cu(II)-Elesclomol has anticancer activity [1].
Imbotolimod, immunoglobulin G1-kappa, is a humanized monoclonal antibody with anti-ERBB2 and antineoplastic activity. Imbotolimod is a derivative of telratolimod [1].
Sovipostobart is an immunoglobulin G1-kappa, anti-CTLA-4 human monoclonal antibody with cleavable prodomain. Sovipostobart is an immunostimulant and antineoplastic [1].
Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15[1] .
Physachenolide C is a potent and selective BET inhibitor that induces apoptosis and arrests the cell cycle in the G0-G1 phase, with antitumor activity [1].
FLT3-IN-18 is a potent and selective FLT3 inhibitor with an IC50 value of 0.003 μM. FLT3-IN-18 induces apoptosis and cell cycle arrest at G1 phase. FLT3-IN-18 inhibits FLT3 and STAT5 phosphorylation. FLT3-IN-18 has the potential for the research of acute myeloid leukemia (AML) [1].
VEGFR-2-IN-23 (compound 11b) is a potent and selective VEGFR-2 inhibitor with an IC50 value of 0.34 nM. VEGFR-2-IN-23 shows antitumor activity. VEGFR-2-IN-23 induces apoptosis and cell cycle arrest at G1 phase [1].
ZDLD20, a β-carboline, is orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 6.51 μM. ZDLD20 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD20 exhibits potent anticancer activity [1].
JUN-1111 is an irreversible and selective Cdc25 phosphatase inhibitor with IC50 values of 0.38, 1.8, 0.66, 28, 37 µM for Cdc25A, Cdc25B, Cdc25C, VHR, PTP1B, respectively. JUN-1111 induces cell cycle arrest at G1 and G2/M phases. JUN-1111 decreases the expression of phosphoCdk1[1] .
ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model [1].
Hygrolidin is a 16-membered macrolide antibiotic produced by Streptomyces hygroscopicus D-1166. Hygrolidin has anti-fungus activity against Valsa ceratosperma. Hygrolidin induces p21 expression and abrogates cell cycle progression at G1 and S phases. Hygrolidin has antitumor activity [1] .
Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication [1] .
Typhatifolin B (Compd 2), an anti-cancer agent, could remarkably induce cell apoptosis and G0/G1 cycle arrest, as well as block cell migration and invasion [1].
Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity [1].
TJ08, a 1,2,5-trisubstituted benzimidazole derivative, efficiently induces G1/S phase arrest and promotes apoptosis in various cancer cells. TJ08 is an anticancer agent [1].
Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities [1] .
CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cell cycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer [1].
Tosatoxumab (AR-301; KBSA301) is a human immunoglobulin G1 monoclonal antibody that specifically neutralizes alpha-toxin (alpha-hemolysin; Hla) of S. aureus. Tosatoxumab binds to an N-terminal epitope of alpha-toxin, thereby preventing functional toxin pore oligomerisation. Tosatoxumab has the potential for passive immunotherapy in the S. aureus pneumonia as an adjunctive therapy to standard antibiotic agent [1] .
Enibarcimab is a humanised murine monoclonal immunoglobulin G1(IgG1) antibody, could be used for acute heart failure, COVID-19 infections and septic shock research [1].
Antiproliferative agent-43 (Compound e4 ) has notable cytotoxic effects against cancer cell lines and causes apoptosis by stopping the cell cycle at G1 phase [1].
Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity [1].
CCT018159, a 3,4-diaryl pyrazoleresorcinol, is a ATP-competitive HSP90 ATPase activity inhibitor with IC50s of 3.2 and 6.6 µM for human Hsp90β and yeast Hsp90, respectively. CCT018159 caused cell cytostasis associated with a G1 arrest and induces apoptosis. CCT018159 inhibits key endothelial and tumor cell functions implicated in invasion and angiogenesis [1].
Thymidine- 13C is the 13C labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1]
Thymidine-d2 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1
CDK7-IN-27 (Compound 37) is a selective inhibitor for cyclin-dependent kinase 7 (CDK7), with Ki of 3 nM. CDK7-IN-27 arrests the cell cycle at G0/G1 phase [1].
Cdc25A (80-93) (human) is a polypeptide that controls the cell proliferation and tumorigenesis by a change in expression of proteins involved in cyclin D1 regulation and G1/S transition. Cdc25A (80-93) (human) can be used in cancer research [1].
Remternetug is a human immunoglobulin G1-kappa, anti-APP (amyloid beta A4 precursor protein) Aβ42 N3pGlu peptide monoclonal antibody. Remternetug recognizes a pyroglutamated form of Aβ that aggregates into amyloid plaques [1].
ICL-CCIC-0019 is an inhibitor of choline kinase α (CHKα). ICL-CCIC-0019 induces G1 block, endoplasmic reticulum stress apoptosis in cancer cell lines [1].
Meisoindigo (Dian III), a derivative of Indirubin (HY-N0117), halts the cell cycle at the G0/G1 phase and induces apoptosis in primary acute myeloid leukemia (AML) cells. Meisoindigo exhibits high antitumor activity [1] .
Thymidine-d4 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1][2][3].
Thymidine-d3 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1][2][3].
NS-3-008 hydrochloride is an orally active transcriptional inhibitor of G0/G1 switch 2 (G0s2) with an IC50 of 2.25 μM. NS-3-008 hydrochloride can be used for chronic kidney disease [1].
Illudin S, a cytotoxic Illudin, is a natural sesquiterpene with strong anti-tumour and antiviral activities. Illudin S has genotoxic activities. Illudin S blocks the G1-S phase interface of the cell cycle in human leukemia cells [1] .
YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma [1].
Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis[1].
Thymidine-2′- 13C is the 13C labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1]<
Antitumor agent-111 (compound 46) is an c-Met kinase inhibitor (IC50=46 nM) with antitumor and antiproliferative activity. Antitumor agent-111 arrests cell cycle at G0/G1 phase, and induces apoptosis[1].
Antitumor agent-103 (compound 24l) is an apoptosis inducer with antiproliferative and anti-clony formation activities. Antitumor agent-103 arrests cell cycle at G0/G1 phase, enhances NO production, and exhibits anti-tumor activity [1].
Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model [1] .
Protosappanin B is a phenolic compound extracted from Caesalpinia sappan. Anti-cancer activity [1]. Protosappanin B induces apoptosis and causes G1 cell cycle arrest in human bladder cancer cells .
HNHA is a potent histone deacetylase (HDAC) inhibitor. HNHA arrests the cell cycle at the G1/S phase via p21 induction. HNHA inhibits tumor growth and tumor neovascularization. HNHA may be a potent anti-cancer agent against breast cancer [1].
Thymidine- 13C-2 is the 13C labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1]
Thymidine- 13C-1 is the 13C labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1]
Antitumor agent-92, an Icaritin (HY-N0678) derivative, causes arrest at the G0/G1 phase in the cell cycle and induces cell apoptosis. Antitumor agent-92 has the potential for hepatocellular carcinoma (HCC) research [1].
p-Tolylmaleimide (compound 9) is a naphthalimide derivative that has cytotoxic effects on cancer cells. p-Tolylmaleimide can arrest the cell cycle of human acute myeloid leukemia cells K562 in the sub-G0/G1 phase and induce apoptosis [1].
Tozorakimab (MEDI-3506) is a human immunoglobulin G1 monoclonal antibody targeting interleukin-33. Tozorakimab reduces inflammation and epithelial dysfunction. Tozorakimab can be used to research chronic obstructive pulmonary disease [1].
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect [1].
DC-CPin711 is a potent and selective inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 0.0626 μM. DC-CPin711 arrests cell cycle at G1 phase and induces apoptosis[1].
ZC0109 is a dual inhibitor of IDO1 and thioredoxin reductase 1(TrxR1) with IC50s of 50 nM and 3.0 μM, respectively. ZC0109 induces ROS accumulation and cell cycle arrest at G1/S phase, thus leads to cancer cells apoptosis[1].
Thymidine- 15N2 is the 15N labeled Thymidine[1]. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[2][3][4].
Risovalisib (CYH33) is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. Risovalisib inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Risovalisib has potent activity against solid tumors [1] .
Crebanine, an alkaloid from Stephania venosa, induces G1 arrest and apoptosis in human cancer cells. Crebanine exhibits anti-inflammatory activity via suppressing MAPKs and Akt signaling. Crebanine also possesses antiarrhythmic effect [1] .
Ganoderic acid Mf is an antitumor triterpenoid. Ganoderic acid Mf causes cell cycle arrest in the G1 phase. Ganoderic acid Mf shows high selectivity between normal and cancer cells and induces cell apoptosis via mitochondria mediated pathway [1].
Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitory activity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population [1] .
MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo [1].
Antitumor agent-45 (Compound 21) could induce and stimulate A549 cells apoptosis in G0/G1 and G2/M phase. Antitumor agent-45 (Compound 21) inhibits c-Met expression to regulate the growth of tumor cells [1].
Ethylene glycol dimethacrylate is a methacrylate monomer, exhibits cytotoxic and genotoxic effects on human gingival fibroblasts (HGFs). Ethylene glycol dimethacrylate increases intracellular reactive oxygen species (ROS) production, causes DNA damage, increases apoptosis and causes cell cycle arrest in G1/G0 phase [1].
1D228 is a c-Met/TRK inhibitor with antitumor activity. 1D228 inhibits cyclin D1 to induce G0/G1 arrest and inhibit cancer cell proliferation and migration. 1D228 can be used in the study of gastric, liver and vascular tumors [1].
Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis[1] .
Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation [1] .
Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis[1] .
Anticancer agent 66 (Compound 13e) is an anti-cancer agent. Anticancer agent 66 induces apoptosis and increases sub-G1 cell population in MCF-7 cells. Anticancer agent 66 is a ciprofloxacin analog [1].
Anticancer agent 67 (Compound 13g) is an anti-cancer agent. Anticancer agent 67 induces apoptosis and increases sub-G1 cell population in MCF-7 cells. Anticancer agent 67 is a ciprofloxacin analog [1].
Sterigmatocystine is a precursor of aflatoxins and a mycotoxin produced by common mold strains from Aspergillus versicolor[1] . Sterigmatocystine, a inhibitor of G1 Phase and DNA synthesis, is used to inhibit p21 activity. Sterigmatocystine has teratogenic, and carcinogenic effects in animals .
Kobusine derivative-2, a kobusine derivative, has antiproliferative activity against cancer cells. Kobusine derivative-2 can induce the arrest of MDA-MB-231 cells in the sub-G1 phase. Anticancer activity [1].
Antileishmanial agent-23 (compound G1/9) is a potent and selective trypanothione reductase (TR) inhibitor, with an IC50 of 2.24 ± 0.52 μM. Antileishmanial agent-23 inhibits the growth of Leishmania, Trypanosoma cruzi, and Trypanosoma brucei[1].
CYH33 methanesulfonate is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 methanesulfonate inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 methanesulfonate has potent activity against solid tumors [1] .
LCAHA (LCA hydroxyamide) is a deubiquitinase USP2a inhibitor with IC50s of 9.7 μM and 3.7μM in Ub-AMC Assay and Di-Ub Assay, respectively. LCAHA destabilizes Cyclin D1 and induces G0/G1 arrest by inhibiting deubiquitinase USP2a [1].
Thymidine- 13C10, 15N2 is the 13C and 15N labeled Thymidine[1]. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[2][3][4].
YS-363 is a potent, selective, and orally active EGFR inhibitor, with IC50s of 0.96 nM and 0.67 nM for wild-type and L858R mutant forms of EGFR, respectively. YS-363 can induce G0/G1 cell cycle arrest and apoptosis[1].
HR488B is an efficient HDAC1 inhibitor. HR488B specifically suppressed the growth of CRC cells by inducing cell cycle G0/G1 arrest and apoptosis. HR488B causes mitochondrial dysfunction, reactive oxygen species (ROS) generation, and DNA damage accumulation [1].
Bet-in-23 (Compound 23) is a BD2-selective BET inhibitor with an IC50 of 2.9 nM. BET-IN-23 has anticancer activity and can significantly inhibit the proliferation of acute myeloid leukemia (AML) cell lines by inducing G0/G1 arrest and apoptosis in vitro [1].
Anticancer agent 204 (Compound 6), a cinnamide fluorinated derivative, possesses anticancer activity. Anticancer agent 204 can arrest the cell cycle of HepG2 cells in the G1 phase and induce apoptosis by reducing the level of mitochondrial membrane polarization (MMP) [1].
GEM144 is a potent and orally active DNA polymerase α(POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts [1].
cis,trans-Germacrone is a isomer of Germacrone (HY-N0440). Germacrone exhibits a wide range of antitumor, antioxidant and anti-inflammatory effects. Germacrone inhibits lung cancer cell proliferation and alters the Akt/MDM2/p53. Germacrone also arrests cell cycle at G1/S phase [1].
Thymidine-d14 (DThyd-d14; NSC 21548-d14) is deuterium labeled Thymidine (HY-N1150). Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
Suberosin, isolated from Plumbago zeylanica, exhibits anti-inflammatory and anticoagulant activity. Suberosin suppresses PHA-induced PBMC proliferation and arrested cell cycle progression from the G1 transition to the S phase through the modulation of the transcription factors NF-AT and NF-κB[1] .
PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFR Del19 in HCC827 cells with the DC50 of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase [1].
Galiximab (IDEC 114) is a primatized immunoglobulin G1 (IgG1) lambda monoclonal antibody directed against the CD80 antigen. Galiximab has variable regions are primatized (cynomologous monkeys), and the constant regions are human. Galiximab can be used in research of B-cell lymphoma [1].
DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor activity [1].
PAK4-IN-2 is a highly potent PAK4 inhibitor with IC50 value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cell apoptosis. PAK4-IN-2 can be used for researching cancer [1].
P300 bromodomain-IN-1 (Compoun 1u) is a potent p300 (EP300) bromodomain inhibitor with an IC50 of 49 nM. P300 bromodomain-IN-1 suppresses the expression of c-Myc and induces G1/G0 phase arrest and apoptosis in OPM-2 cells [1].
Compound 26F not only optimized the effective inhibitory enzyme (ic50= 28.2 nm), but also showed relatively less cytotoxicity (ic50= 3.32 μ M) And induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in g0/g1 phase.
N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma [1]- .
(-)-Hinesol (Hinesol) is a potent anticancer agent. (-)-Hinesol induces apoptosis and cell cycle arrest at G0/G1 phase. (-)-Hinesol downregulates MEK/ERK pathway and NF-κB pathway and mediates theexpression of cyclin D1, Bax and Bcl-2. (-)-Hinesol has the potential for the research of non–small cell lung cancer [1].
Thymidine- 13C10 (DThyd- 13C10; NSC 21548- 13C10) is 13C-labeled Thymidine (HY-N1150). Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
Picrasidine Q, an alkaloid component extracted from Angelica keiskei species, has the capacity of anti-cell transformation and anti-cancer. Picrasidine Q induces cell apoptosis and G1 phase arrest in human esophageal cancer cell lines, and directly inhibits FGFR2 kinase activity [1].
PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFR Del19 in HCC827 cells with the DC50 of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase [1].
Cucurbitacin C is a triterpenoid calabinoid that can be isolated from Cucurbitaceae plants. Cucurbitacin C has anti-cancer activity in vivo and in vitro. Cucurbitacin C can induce cell cycle arrest in G1 or G2/M phase and apoptosis by inhibiting Akt signaling [1].
Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment [1] .
EGFR-IN-55 (Compound 8a) is a potent EGFR inhibitor with IC50 values of 70 nM and 3.9 nM against EGFR WT and EGFR L858R/T790M, respectively. EGFR-IN-55 arrests NCI-H1975 cells in G0/G1 phase and shows anticancer activity [1].
[1,1′:4′,1′′-Terphenyl]-3,4′′,5-triol (compound 13g) is a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells. [1,1′:4′,1′′-Terphenyl]-3,4′′,5-triol shows a potent apoptotic effect [1].
BK50164 is a potent CD73 inhibitor with an IC50 value of 13.089 µM. BK50164 binds to CD99 with a KD value of 1.5 µM. BK50164 shows antiproliferative activity. BK50164 induced Apoptosis and cell cycle arrest at Sub-G1 phase [1].
Solanezumab is a humanized monoclonal IgG1 antibody directed against the mid-domain of the amyloid-β (Aβ) peptide. Solanezumab has the potential for the research of Alzheimer’s disease [1].
Ramucirumab is a human VEGFR-2 antagonist for the treatment of solid tumors. Ramucirumab is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D. Ramucirumab is also an angiogenesis inhibitor [1] .
Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis [1] .
Aflatoxin B2 is a major naturally produced aflatoxin. Aflatoxin B2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [1].
Aflatoxin G2 is a major naturally produced aflatoxin. Aflatoxin G2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [1].
Aflatoxin M2 is a major metabolite of Aflatoxin B1. Aflatoxin M2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [1].
EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1[1].
Antitumor agent-55 (compound 5q) is a potent antitumor agent. Antitumor agent-55 effectively inhibits PC3, with an IC50 of 0.91 μM. Antitumor agent-55 effectively inhibits the colony formation, suppresses the cell migration in PC3. Antitumor agent-55 induces G1/S phase arrest and apoptosis in PC3 [1].
AKT-IN-12 (compound 3e) is a potent Akt kinase inhibitor with an IC50 value of 0.55 μM. AKT-IN-12 induces G0/G1 cell cycle arrest and apoptosis. AKT-IN-12 also inhibits p-AKT, p-ERK, and activates p-JNK, JNK. AKT-IN-12 can be used for researching leukemia [1].
Anticancer agent 70 (Compound 21), an anticancer agent, exhibits remarkable cytotoxic activity against numerous human cancer cell lines. Anticancer agent 70 results in the G0/G1-cell cycle arrest with a concomitant increase in p53 and p21 protein levels. Anticancer agent 70 leads to ATP depletion and disruption of the mitochondrial membrane potential [1].
HSP90-IN-23 (Comp 12-1) is an inhibitor of heat shock protein 90(HSP90) with an IC50 of 9 nM. HSP90-IN-23 induces apoptosis of tumor cells and arrests the tumor cell cycle in G0/G1 phase. HSP90-IN-23 can be used for cancer research [1].
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth [1].
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models [1] .
Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase [1] .
Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexe. Lobaplatin arrests cell cycle at G1 and G2/M phase. Lobaplatin induces apoptosis by increasing expressions of caspase and Bax, decreasing expression of Bcl-2. Lobaplatin can be used for research of cancer [1] .
INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research [1].
Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner [1] .
Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis [1] .
Sudubrilimab (HS636) is an Ig G1-kappa monoclonal antibody against PDL1. Sudubrilimab is fused at the C terminus of the heavy chain to a TGF-β1 receptor Ⅱ ectodomain (TGFBR2-ECD), and which can sequester the PD-1/PD-L1 pathway and TGF-β bioactivity in the immunosuppressive tumor microenvironment [1].
BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1(IC50=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage [1].
LWY713 is a FLT3 degrader (DC50=0.64 nM) that selectively induces FLT3 degradation in a cereblon- and proteasome-dependent manner. LWY713 inhibits cell proliferation and induces G0/G1 arrest and apoptosis in MV4-11 cells. LWY713 exhibits potent in vivo antitumor activity in an MV4-11 xenograft model [1].
FGFR1 inhibitor-6 is a potent FGFR1 inhibitor with an IC50 value of 16.31 nM. FGFR1 inhibitor-6 shows cytotoxic activities. FGFR1 inhibitor-6 induces apoptosis and cell cycle arrest at pre-G1 and G2/M phase [1].
Antiproliferative agent-26 (compound 4g) is an antiproliferative agent with much broad range of activity targeting Leukemia, CNS, Melanoma, Renal and Breast (at the concentration of 10 μM). Antiproliferative agent-26 inhibits colony forming and arrests cell cycle at G1 phase/S phase at 5 μM and 25 μM, respectively [1].
Sterigmatocystine (Standard) is the analytical standard of Sterigmatocystine. This product is intended for research and analytical applications. Sterigmatocystine is a precursor of aflatoxins and a mycotoxin produced by common mold strains from Aspergillus versicolor[1] . Sterigmatocystine, a inhibitor of G1 Phase and DNA synthesis, is used to inhibit p21 activity. Sterigmatocystine has teratogenic, and carcinogenic effects in animals .
Isoeugenol-d3 is deuterated labeled Sterigmatocystine (HY-N6725). Sterigmatocystine is a precursor of aflatoxins and a mycotoxin produced by common mold strains from Aspergillus versicolor[1] . Sterigmatocystine, a inhibitor of G1 Phase and DNA synthesis, is used to inhibit p21 activity. Sterigmatocystine has teratogenic, and carcinogenic effects in animals .
Apoptotic agent-4 (Compound 9) is a apoptosis inducer. Apoptotic agent-4 inhibits VEGFR-2 with an IC50 of 0.5717 μM. Apoptotic agent-4 inhibits cancer cell proliferation and arrests the cell at both the G2/M and Pre-G1 phases [1].
Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is an orally active mycotoxin produced by Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [1] .
PAK4-IN-3(compound 27e) is aPAK4inhibitor, with theIC50of 10 nM.PAK4-IN-3shows antiproliferative activity against A549 cells with anIC50value of 0.61μM, and inducesapoptosisof A549 cells in a concentration-dependent manner and blocked the cell cycle at phase G0/G1[1].
Menin-MLL inhibitor-25 (compound A6) is a potent Menin-MLL interaction inhibitor with an IC50 value of 0.38 µM. Menin-MLL inhibitor-25 shows anti-proliferative activity. Menin-MLL inhibitor-25 induces apoptosis and cell cycle arrest at G0/G1 phase. Menin-MLL inhibitor-25 reverses the differentiation arrest [1].
J208 is a dual inhibitor for histone deacetylase (HDAC) and DNA methyltransferase (DNMT). J208 inhibits proliferation of cancer cells, as well as the migration/invasion of triple-negative breast cancer (TNBC) cells. J208 induces apoptosis, arrests the cell cycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs) [1].
Ramucirumab (anti-VEGFR) is a human VEGFR-2 antagonist for the treatment of solid tumors. Ramucirumab (anti-VEGFR) is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D. Ramucirumab (anti-VEGFR) is also an angiogenesis inhibitor [1] .
6-CEPN is a RAS inhibitor. 6-CEPN can inhibit RAS activation by binding to Icmt binding sites. 6-CEPN has anticancer activity. 6-CEPN can block cancer cells in the G1 phase. 6-CEPN can induce autophagy and necrosis of Cancer cells (Icmt: isovalerylcysteine carboxymethyltransferase) [1].
Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma [1] .
HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies [1] .
VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase [1].
NTQ1062 is a potent and orally active Akt inhibitor with IC50s of 0.4 nM, 6.3 nM and 0.1 nM for Akt1, Akt2 and Akt3, respectively. NTQ1062 induces cell apoptosis and arrests the cell cycle at G0/G1 phase. NTQ1062 exhibits antiproliferation activity against various cancer cells. NTQ1062 exhibits potent antitumor efficacy in LNCap xenograft mouse model [1].
hCAIX-IN-16 (Compound 12d) is hCA IX inhibitor, with Ki values of 190.0 and 187.9 nM for hCA IX and hCA XII, respectively. hCAIX-IN-16 can arrest the cell cycle of breast cancer MDA-MB-468 in G0-G1 and S phase and induce apoptosis. hCAIX-IN-16 shows good broad-spectrum anticancer activity and can be used for cancer research [1].
Estrogen receptor modulator 10 (compound G-5b) is an Estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 can induce apoptosis. Estrogen receptor modulator 10 can block cells at the G1/G0 phase. Estrogen receptor modulator 10 can be used in cancer studies [1].
Mevastatin (Standard) is the analytical standard of Mevastatin. This product is intended for research and analytical applications. Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment [1] .
EGFR-IN-45 is a potent epidermal growth factor receptor (EGFR) pan inhibitor, with IC50s of 0.4 µM and 1.6 µM for EGFR and CDK2, respectively. EGFR-IN-45 also inhibit Topo I and Topo II. EGFR-IN-45 arrests cancer cells in the pre-G1 phase and induces apoptosis[1].
SIAIS164018 is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857) [1].
Secalonic acid D is a toxic compound against tumor cells. Secalonic acid D can be isolated from the metabolites of Aspergillus aculeatus. Secalonic acid D activates GSK3-β, and degrades β-catenin. Thus, Secalonic acid D down-regulates c-Myc expression, arrests cell cycle at G1 phase, induces cell apoptosis[1] .
BRD4-IN-4 (Compound 1) is a BRD4 inhibitor (IC50=6.83 μM). BRD4-IN-4 selectively inhibits MV4-11 cell line proliferation and arrests cell at G1 phase. BRD4-IN-4 can be used for research of MLL leukemia [1].
SIAIS164018 hydrochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857) [1].
Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations [1] .
BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with an IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity [1].
14-3-3η Protein inhibitor 1 (Compound C11) is a 14-3-3η protein inhibitor with a KD of 35 µM. 14-3-3η Protein inhibitor 1 shows inhibitory activities against several typical human liver cancer cell lines. 14-3-3η Protein inhibitor 1 induces cell apoptosis and G1-S cell cycle arrest with good metabolic stability [1].
PI3K/mTOR Inhibitor-8 (Compound 18b) is a PI3K and mTOR dual inhibitor with IC50 values of 0.46 nM and 12 nM against PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-8 induces HCT-116 cells apoptosis and arrests cell cycle at the G1/S phase [1].
ALK/EGFR-IN-2 is a potent dual inhibitor of ALK and EGFR. ALK/EGFR-IN-2 induces apoptosis and G0/G1 cell cycle arrest in cancer cells. ALK/EGFR-IN-2 significantly inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC50s of 0.0034, 0.0065, and 0.0018 μM, respectively [1].
EGFR WT/T790M-IN-2 (Compound 7c) is a EGFR T790M/WT inhibitor with IC50 values of 0.08 and 0.13 μM, respectively. EGFR WT/T790M-IN-2 induces apoptosis by blocking the G0-G1 phase (apoptosis). EGFR WT/T790M-IN-2 has antitumor activity [1].
Duocarmycin A, which is one of well-known antitumor antibiotics, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels [1].
Sarilumab (Anti-Human IL6Rα, Human Antibody) is a human immunoglobulin G1 monoclonal antibody. Sarilumab, a interleukin-6 (IL-6) receptor antagonist, binds to the IL-6 receptor with high affinity and inhibits cis and trans signaling by IL-6, resulting in reduced inflammation. Sarilumab can be used for the research of Rheumatoid arthritis [1] .
Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin [1].
FB49 is a highly selective inhibitor of Bcl-2-associated athanogene 3 (BAG3), with the Ki of 45 μM. FB49 inhibits the cell growth in human tumoral cells, but has no toxicity in human peripheral mononuclear cells. FB49 block cell cycle in G1 phase and to induce apoptosis as well as autophagy in medulloblastoma HD-MB03 treated cells [1].
KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively [1]. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells . KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation .
K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2 with IC50 values of 680 and 406 nM, respectively. K783-0308 inhibits the growth of MOLM-13 (IC50=10.5 µM) and MV-4-11 (IC50=10.4 µM) cells. K783-0308 promotes acute myeloid leukemia (AML) cell apoptosis and cell cycle arrests in the G0/G1 phase [1].
USP7-IN-9 is a highly potent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 value of 40.8 nM. USP7-IN-9 can induce apoptosis and arrest cell progression at G0/G1 and S phases in RS4; 11 cells. USP7-IN-9 reduces the protein levels of oncoproteins MDM2 and DNMT1 and increases the protein levels of tumor suppressors p53 and p21 [1].
BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAF V600E/CRAF. BRAF V600E/CRAF-IN-1 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-1 has the potential for the research of cancer diseases [1].
HDAC1/6-IN-1 (compound D7) is a potent multitarget inhibitor of GLP, HDAC6 and HDAC1, with IC50 values of 1.3, 13, and 89 nM, respectively. HDAC1/6-IN-1 can inhibit the methylation and deacetylation of H3K9 on protein level. HDAC1/6-IN-1 induces cancer cell apoptosis, G0/G1 cell cycle arrest, and blocks migration and invasion [1].
Aflatoxin G2- 13C17 is the 13C labeled Aflatoxin G2 (HY-N6698) [1]. Aflatoxin G2 is a major naturally produced aflatoxin. Aflatoxin G2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 .
Aflatoxin M1 (Standard) is the analytical standard of Aflatoxin M1. This product is intended for research and analytical applications. Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [1].
Anticancer agent 205 (compound 9) is a potent anticancer agent. Anticancer agent 205 binds to G4-mtDNA target and inhibits the replication, transcription, and translation of mtDNA (mitochondrial genome). Anticancer agent 205 causes mitochondrial dysfunction, increases ROS production, induces DNA damage and cellular senescence. Anticancer agent 205 induces apoptosis and cell cycle arrests at G0/G1 phase. Anticancer agent 205 has the potential for the research of colorectal cancer [1].
Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation [1].
VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase [1].
SGC0946 is a selective DOT1LH3K79 methyltransferase) inhibitor, with an IC50 of 0.3 nM. SGC0946 results in G1 arrest, inhibits potential of cell self-renewal and metastatic, also induces cell differentiation. SGC0946 can be used in studies of leukemia and solid tumors and also serve as a probe to further investigate the cellular mechanism of DOT1L in both normal and diseased cells [1] .
Mosunetuzumab (BTCT-4465A) is a full-length, fully humanized immunoglobulin G1 (IgG1) T-cell-dependent bispecific (TDB) antibody targeting CD20 (B cells) and CD3 (T cells). Mosunetuzumab redirects T cells to engage and eliminate malignant B cells and can be used for the research of relapsed or refractory (R/R) B-cell non-Hodgkin lymphomas (B-NHLs) [1] .
Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models [1].
BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC50 of ∼5 µM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 induces apoptosis and displays antitumour activities in orthotopic mammary tumours in mice [1] .
JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities [1].
3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases [1] .
EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis[1].
Aflatoxin M2- 13C17 is the 13C labeled Aflatoxin M2 (HY-N6700) [1]. Aflatoxin M2 is a major metabolite of Aflatoxin B1. Aflatoxin M2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 .
Aflatoxin M1- 13C17 is the 13C labeled Aflatoxin M1 (HY-N6699) [1]. Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 .
Aflatoxin B2- 13C17 is 13C- and 15N-labeled Aflatoxin B2 (HY-N6696). Aflatoxin B2 is a major naturally produced aflatoxin. Aflatoxin B2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [1] .
Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cell cycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity [1] .Tunicamycin increases exosome release in cervical cancer cells .
HDAC-IN-37 is a potent HDAC inhibitor with IC50s of 0.0551 μM, 1.24 μM, 0.948 μM and 34.2 μM for HDAC1, HDAC3, HDAC8 and HDAC6, respectively. HDAC-IN-37 induces histone acetylation in a slow-off manner. HDAC-IN-37 prevents cell transition from G1 phase to S phase and induces early cell apoptosis[1].
CDK4/6-IN-15 is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression [1].
CTL-06 is an inhibitor of Fatty Acid Synthase (FASN) (IC50: 3 μM) and can induce apoptosis. CTL-12 blocks the cell cycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research [1].
Cysmethynil is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research [1] .
BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAF V600E/CRAF with IC50s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases [1].
PI3K-IN-48 is a PI3K inhibitor with IC50 value of 1.55 ± 0.18 μM for A549 cells. PI3K-IN-48 can induce G0/G1 phase arrest, cell apoptosis, and down-regulate expression of p-PI3K and p-Akt. PI3K-IN-48 can be used for human lung cancers diseases research [1].
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice was 75.4% [1].
anti-TNBC agent-1 is a potent anti-triple-negative breast cancer (TNBC) agent. anti-TNBC agent-1 exhibits potent activity against different breast cancer cells with IC50 values ranging from 0.20 μM to 0.27 μM. anti-TNBC agent-1 induces apoptosis of SUM-159 cells through mitochondria pathway and causes G1 phase arrest of SUM-159 cells [1].
FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model [1].
CTL-12 is an inhibitor of fatty acid synthase (FASN) (IC50: 2.5 μM) and can induce apoptosis. CTL-12 blocks the cell cycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research [1].
NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase [1].
HDAC-IN-50 is a potent and orally active FGFR and HDAC dual inhibitor with IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-50 induces Apoptosis and cell cycle arrest at G0/G1 phase. HDAC-IN-50 decreases the expression of pFGFR1, pERK, pSTAT3. HDAC-IN-50 shows anti-tumor activity [1].
BML-278 is a SIRT1 activator (EC150: 1 μM). BML-278 increases H3K9 methylation and inhibits H3K9 acetylation in both the paternal and maternal pronucleus. BML-278 improves early embryonic development. BML-278 arrests the cell cycle at the G1/S phase, and reduces senescence in primary human mesenchymal cells. BML-278 reduces tubulin acetylation in U937 cells. BML-278 also increases mitochondrial density in murine C2C12 myoblasts [1] .
1-Octanol-d5 is deuterated labeled Carvacrol (HY-N0711). Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations [1] .
20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity [1] . 20(R)-Ginsenoside Rh2 inhibits the replication and proliferation of mouse and human gammaherpesvirus 68 (MHV-68) with an IC50 of 2.77 μM for murine MHV-68 .
FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML) [1].
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) [1].
EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis[1].
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC50: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC50: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) [1].
SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research [1].
EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines [1].
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML [1].
HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population [1].
Batiraxcept (AVB-S6-500) is a highly potent and specific AXL inhibitor, a recombinant fusion protein dimer containing the extracellular domain of human AXLM and human immunoglobulin G1 heavy chain (Fc). Batiraxcept binds to GAS6 and inhibits the interaction of GAS6 with AXL, thereby substantially reducing AXL signaled invasion and migration of highly metastatic cells in vitro and inhibiting metastatic disease in nonclinical models of aggressive human cancers. Batiraxcept is available for studies in advanced or metastatic clear cell renal cell carcinoma (ccRCC) and platinum sensitive recurrent ovarian cancer [1] .
HDAC-IN-56 ((S)-17b) is an orally active class I histone deacetylase (HDAC) inhibitor with IC50 values of 56.0 ± 6.0, 90.0 ± 5.9, 422.2 ± 105.1, >10000 nM for HDAC1, HDAC2, HDAC3, and HDAC4-11, respectively. HDAC-IN-56 has potent inhibitory activity while strongly increasing intracellular levels of acetylhistone H3 and P21 and effectively inducing G1 cell cycle arrest and apoptosis.HDAC-IN-56 has antitumor activity [1].
S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies [1] . S116836 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanoma cells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer [1]. HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PIM-1/HDAC-IN-1 (compound 4d) is a PIM-1 inhibitor, with an IC50 of 343.87 nM. PIM-1/HDAC-IN-1 has strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. PIM-1/HDAC-IN-1 exhibits apoptosis inducing potential in MCF-7 cell lines. PIM-1/HDAC-IN-1 shows pre-G1 apoptosis and cell cycle arrest at G2/M phase [1].
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively [1].
PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) [1].
[Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 (Compound 3) is a copper complex, which inhibits cell viability of HCT116, HCT116DoxR, A2780 and fibroblasts, with IC50s of 0.13, 0.15, 0.66 and 6.24 μM, respectively. [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 induces apoptosis and autophagy, and arrests cell cycle at G0/G1 phase in HCT116DoxR. [Cu2Cl2(4'-(4-Methoxy-1-naphthyl)-terpy)2](PF6)2 exhibits antimetastatic efficacy [1].
EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity [1].
AP1G1 Human Pre-designed siRNA Set A contains three designed siRNAs for AP1G1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
EIF4G1 Human Pre-designed siRNA Set A contains three designed siRNAs for EIF4G1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
CSNK1G1 Human Pre-designed siRNA Set A contains three designed siRNAs for CSNK1G1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
UBE2G1 Human Pre-designed siRNA Set A contains three designed siRNAs for UBE2G1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
PLA2G1B Human Pre-designed siRNA Set A contains three designed siRNAs for PLA2G1B gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
ATP6V1G1 Human Pre-designed siRNA Set A contains three designed siRNAs for ATP6V1G1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Tadocizumab (C4G1; YM-337) is a humanized monoclonal antibody tageting integrin αIIbβ3. Tadocizumab has antiplatelet and antithrombotic effects, and can be used for cardiovascular disease research [1] .
Pexelizumab (h5G1. 1-SC) is a humanized scFv monoclonal antibody directed against the C5 complement component. Pexelizumab inhibits apoptosis and leukocyte infiltration. Pexelizumab can be used for the research of cerebral IR injury and myocardial infarction [1] .
CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively [1].
Antitumor agent-150 (V10), an anti-breast cancer agent, is a PROTAC-based MDM2 protein degrader (Red: Ganoderic acid A; Black: 4O-PEG linker; Blue: VHL ligand) [1].
MSC2504877 (M2912) is a potent and orally active tankyrase inhibitor with IC50s of 0.0007, 0.0008, 0.54 µM for TNKS, TNKS2, PARP1, respectively. MSC2504877 increases the expression of AXIN2 and TNKS protein levels and decreases β-catenin levels. MSC2504877 shows anti-tumor activity [1].
MDMX/MDM2-IN-2 is a potent p53-MDM2/MDMX dual inhibitors with Kis of 0.23 μM and 2.45 μM for MDM2 and MDMX, respectively. MDMX/MDM2-IN-2 inhibits the binding of p53 and MDM2 proteins. MDMX/MDM2-IN-2 restores the function of p53 and enables cell cycle arrest and apoptosis. MDMX/MDM2-IN-2 inhibits cell migration and invasion. MDMX/MDM2-IN-2 has antitumor activity [1].
BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ [1] .
ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer [1].
GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer [1] .
BTK-IN-7 is a potent and selective inhibitor of BTK (IC50=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels (ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity [1].
GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity [1].
VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC50=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition [1].
Celangulin XIX is a insecticidal that can be isolated from Celastrus angulatu. Celangulin XIX has strong insecticidal activity against Mythimna separate with an ED50 of 73.3 μg/g .
PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity [1] .
5-Aminoimidazole ribonucleotide (AIR) is an intermediate in the biosynthesis of purines, as AIR is further modified by additional enzymes to eventually produce inosine monophosphate (IMP), which can then be converted into the purine bases adenine (A) and guanine (G) .
Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research [1] .
CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC50s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM) [1].
Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G) .
JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research [1].
SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G .
Suc-Ala-Ala-Pro-Phe-SBzl can be used as the substrate of rat intestinal mast cell protease (RMCP I), rat skeletal muscle mast cell protease (RMCP II) and Chymotrypsin (HY-108910). Suc-Ala-Ala-Pro-Phe-SBzl can be hydrolyzed by glycine (R208G) .
SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 quarterhydrate shows no inhibitory activity against cathepsin G .
ODN 6016 is a CpG-A oligonucleotides. ODN 6016 can induce IFN-α production, can be used for researching immune disorders including immunodeficiency caused by HIV-1. ODN 6016 sequence: T-sp-C-G-A-C-G-T-C-G-T-G-G-sp-G-sp-G-sp-G .
ODN 6016 sodium is a CpG-A oligonucleotides. ODN 6016 sodium can induce IFN-α production, and can be used for researching immune disorders including immunodeficiency caused by HIV-1. ODN 6016 sequence: T-sp-C-G-A-C-G-T-C-G-T-G-G-sp-G-sp-G-sp-G .
Q94 hydrochloride, a selective PAR1 antagonist (IC50=916 nM), can selectively block PAR1/Gαq interaction and signalling. Q94 hydrochloride blocks PAR1-mediated increases in both CCL2 mRNA and protein levels in a dose-dependent manner. Q94 hydrochloride also completely blocks thrombin-induced ERK1/2 and MLC phosphorylation [1].
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1(PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects [1] .
CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cell cycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer [1].
Cdc25A (80-93) (human) is a polypeptide that controls the cell proliferation and tumorigenesis by a change in expression of proteins involved in cyclin D1 regulation and G1/S transition. Cdc25A (80-93) (human) can be used in cancer research [1].
TAT-p16 (p16INK4a peptide) is a peptide mimic of p16INK4a that can induce an early G phase cell cycle arrest in the absence of active cyclin E:Cdk2 complex [1].
Suc-Ala-Ala-Pro-Phe-SBzl can be used as the substrate of rat intestinal mast cell protease (RMCP I), rat skeletal muscle mast cell protease (RMCP II) and Chymotrypsin (HY-108910). Suc-Ala-Ala-Pro-Phe-SBzl can be hydrolyzed by glycine (R208G) .
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1(PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects [1] .
Nesvacumab is a fully human immunoglobulin G1 (IgG1) monoclonal antibody that specifically binds and inactivates the Tie2 receptor ligand Angiopoietin-2 (Ang2) with high affinity, but shows no binding to Ang1[1].
Rocatinlimab (AMG 451) (KHK4083) is a fully human, non-fucosylated, immunoglobulin G1 (IgG1) anti-OX40 monoclonal antibody. Rocatinlimab can be used for the research of atopic dermatitis (AD) [1].
Calpurbatug is an immunoglobulin G1 antibody. Calpurbatug has activity with anti-bacterial DNA-binding protein DNABII family and anti-human monoclonal TRL1068 γ1-chain [1].
Sovipostobart is an immunoglobulin G1-kappa, anti-CTLA-4 human monoclonal antibody with cleavable prodomain. Sovipostobart is an immunostimulant and antineoplastic [1].
Renvistobart is an immunoglobulin G1-κ, anti-[Homo sapiens TIGIT (T cell immunoreceptor with Ig domain and ITIM, VSIG9, VSTM3)] Homo sapiens monoclonal antibody [1].
Ifinatamab is monoclonal immunoglobulin G1-kappa with anti-human B7 homolog 3 protein (Human B7-H3). Ifinatamab is a glycoforme α immunomodulateur [1].
Lesabelimab (LDP) is an immunoglobulin G1-kappa anti-CD274 monoclonal antibody. CD274 is an immune checkpoint ligand, represses antitumour immunity through the interaction with PDCD1 receptor [1] .
Tosatoxumab (AR-301; KBSA301) is a human immunoglobulin G1 monoclonal antibody that specifically neutralizes alpha-toxin (alpha-hemolysin; Hla) of S. aureus. Tosatoxumab binds to an N-terminal epitope of alpha-toxin, thereby preventing functional toxin pore oligomerisation. Tosatoxumab has the potential for passive immunotherapy in the S. aureus pneumonia as an adjunctive therapy to standard antibiotic agent [1] .
Enibarcimab is a humanised murine monoclonal immunoglobulin G1(IgG1) antibody, could be used for acute heart failure, COVID-19 infections and septic shock research [1].
Remternetug is a human immunoglobulin G1-kappa, anti-APP (amyloid beta A4 precursor protein) Aβ42 N3pGlu peptide monoclonal antibody. Remternetug recognizes a pyroglutamated form of Aβ that aggregates into amyloid plaques [1].
Tozorakimab (MEDI-3506) is a human immunoglobulin G1 monoclonal antibody targeting interleukin-33. Tozorakimab reduces inflammation and epithelial dysfunction. Tozorakimab can be used to research chronic obstructive pulmonary disease [1].
Puxitatug is an immunoglobulin G1-κ, anti-[Homo sapiens VTCN1 (Vset domain containing T cell activation inhibitor 1, B7 family member H4, B7H4, B7-H4)] Homo sapiens monoclonal antibody [1].
Galiximab (IDEC 114) is a primatized immunoglobulin G1 (IgG1) lambda monoclonal antibody directed against the CD80 antigen. Galiximab has variable regions are primatized (cynomologous monkeys), and the constant regions are human. Galiximab can be used in research of B-cell lymphoma [1].
Vopratelimab (JTX-2011) is a humanized immunoglobulin G1-kappa agonist monoclonal antibody that pecifically binds to the Inducible CO-Stimulator of T cells (ICOS). Vopratelimab retains species cross-reactivity with affinities of 0.93 nM to hICOS, 0.46 nM to cynomolgus ICOS, 3.7 nM to rat ICOS, and 0.64 nM to mICOS. Vopratelimab has antitumor immune response [1].
Solanezumab is a humanized monoclonal IgG1 antibody directed against the mid-domain of the amyloid-β (Aβ) peptide. Solanezumab has the potential for the research of Alzheimer’s disease [1].
Ramucirumab is a human VEGFR-2 antagonist for the treatment of solid tumors. Ramucirumab is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D. Ramucirumab is also an angiogenesis inhibitor [1] .
Sudubrilimab (HS636) is an Ig G1-kappa monoclonal antibody against PDL1. Sudubrilimab is fused at the C terminus of the heavy chain to a TGF-β1 receptor Ⅱ ectodomain (TGFBR2-ECD), and which can sequester the PD-1/PD-L1 pathway and TGF-β bioactivity in the immunosuppressive tumor microenvironment [1].
Ramucirumab (anti-VEGFR) is a human VEGFR-2 antagonist for the treatment of solid tumors. Ramucirumab (anti-VEGFR) is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D. Ramucirumab (anti-VEGFR) is also an angiogenesis inhibitor [1] .
Sarilumab (Anti-Human IL6Rα, Human Antibody) is a human immunoglobulin G1 monoclonal antibody. Sarilumab, a interleukin-6 (IL-6) receptor antagonist, binds to the IL-6 receptor with high affinity and inhibits cis and trans signaling by IL-6, resulting in reduced inflammation. Sarilumab can be used for the research of Rheumatoid arthritis [1] .
Mosunetuzumab (BTCT-4465A) is a full-length, fully humanized immunoglobulin G1 (IgG1) T-cell-dependent bispecific (TDB) antibody targeting CD20 (B cells) and CD3 (T cells). Mosunetuzumab redirects T cells to engage and eliminate malignant B cells and can be used for the research of relapsed or refractory (R/R) B-cell non-Hodgkin lymphomas (B-NHLs) [1] .
Batiraxcept (AVB-S6-500) is a highly potent and specific AXL inhibitor, a recombinant fusion protein dimer containing the extracellular domain of human AXLM and human immunoglobulin G1 heavy chain (Fc). Batiraxcept binds to GAS6 and inhibits the interaction of GAS6 with AXL, thereby substantially reducing AXL signaled invasion and migration of highly metastatic cells in vitro and inhibiting metastatic disease in nonclinical models of aggressive human cancers. Batiraxcept is available for studies in advanced or metastatic clear cell renal cell carcinoma (ccRCC) and platinum sensitive recurrent ovarian cancer [1] .
Tadocizumab (C4G1; YM-337) is a humanized monoclonal antibody tageting integrin αIIbβ3. Tadocizumab has antiplatelet and antithrombotic effects, and can be used for cardiovascular disease research [1] .
Pexelizumab (h5G1. 1-SC) is a humanized scFv monoclonal antibody directed against the C5 complement component. Pexelizumab inhibits apoptosis and leukocyte infiltration. Pexelizumab can be used for the research of cerebral IR injury and myocardial infarction [1] .
Aflatoxin G1 is one type of aflatoxins occuring in nature. It is produced by molds, such as Aspergillus flavus and Aspergillus parasiticus. Aflatoxins are hepatogenic, teratogenic, imunosuppressive, and carcinogenic fungal metabolites found in feeds, nuts, wine-grapes, spices, and other grain crops [1] .
Ganoderic acid DM, a natural triterpenoid isolated from Ganoderma lucidum, induces DNA damage, G1 cell cycle arrest and apoptosis in human breast cancer cells. Ganoderic acid DM as a specific inhibitor of osteoclastogenesis [1] .
Physachenolide C is a potent and selective BET inhibitor that induces apoptosis and arrests the cell cycle in the G0-G1 phase, with antitumor activity [1].
Hygrolidin is a 16-membered macrolide antibiotic produced by Streptomyces hygroscopicus D-1166. Hygrolidin has anti-fungus activity against Valsa ceratosperma. Hygrolidin induces p21 expression and abrogates cell cycle progression at G1 and S phases. Hygrolidin has antitumor activity [1] .
Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication [1] .
Typhatifolin B (Compd 2), an anti-cancer agent, could remarkably induce cell apoptosis and G0/G1 cycle arrest, as well as block cell migration and invasion [1].
Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities [1] .
Meisoindigo (Dian III), a derivative of Indirubin (HY-N0117), halts the cell cycle at the G0/G1 phase and induces apoptosis in primary acute myeloid leukemia (AML) cells. Meisoindigo exhibits high antitumor activity [1] .
Illudin S, a cytotoxic Illudin, is a natural sesquiterpene with strong anti-tumour and antiviral activities. Illudin S has genotoxic activities. Illudin S blocks the G1-S phase interface of the cell cycle in human leukemia cells [1] .
Apiole is an anti-tumor agent that induces apoptosis and inhibits human colon cancer cells by inducing G0/G1 cell cycle arrest. Apiole also significantly inhibited colon tumor development in an in vivo mouse xenograft model [1] .
Protosappanin B is a phenolic compound extracted from Caesalpinia sappan. Anti-cancer activity [1]. Protosappanin B induces apoptosis and causes G1 cell cycle arrest in human bladder cancer cells .
Crebanine, an alkaloid from Stephania venosa, induces G1 arrest and apoptosis in human cancer cells. Crebanine exhibits anti-inflammatory activity via suppressing MAPKs and Akt signaling. Crebanine also possesses antiarrhythmic effect [1] .
Ganoderic acid Mf is an antitumor triterpenoid. Ganoderic acid Mf causes cell cycle arrest in the G1 phase. Ganoderic acid Mf shows high selectivity between normal and cancer cells and induces cell apoptosis via mitochondria mediated pathway [1].
Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitory activity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population [1] .
Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation [1] .
Sterigmatocystine is a precursor of aflatoxins and a mycotoxin produced by common mold strains from Aspergillus versicolor[1] . Sterigmatocystine, a inhibitor of G1 Phase and DNA synthesis, is used to inhibit p21 activity. Sterigmatocystine has teratogenic, and carcinogenic effects in animals .
Suberosin, isolated from Plumbago zeylanica, exhibits anti-inflammatory and anticoagulant activity. Suberosin suppresses PHA-induced PBMC proliferation and arrested cell cycle progression from the G1 transition to the S phase through the modulation of the transcription factors NF-AT and NF-κB[1] .
N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma [1]- .
(-)-Hinesol (Hinesol) is a potent anticancer agent. (-)-Hinesol induces apoptosis and cell cycle arrest at G0/G1 phase. (-)-Hinesol downregulates MEK/ERK pathway and NF-κB pathway and mediates theexpression of cyclin D1, Bax and Bcl-2. (-)-Hinesol has the potential for the research of non–small cell lung cancer [1].
Picrasidine Q, an alkaloid component extracted from Angelica keiskei species, has the capacity of anti-cell transformation and anti-cancer. Picrasidine Q induces cell apoptosis and G1 phase arrest in human esophageal cancer cell lines, and directly inhibits FGFR2 kinase activity [1].
Cucurbitacin C is a triterpenoid calabinoid that can be isolated from Cucurbitaceae plants. Cucurbitacin C has anti-cancer activity in vivo and in vitro. Cucurbitacin C can induce cell cycle arrest in G1 or G2/M phase and apoptosis by inhibiting Akt signaling [1].
Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment [1] .
Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis [1] .
Aflatoxin B2 is a major naturally produced aflatoxin. Aflatoxin B2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [1].
Aflatoxin G2 is a major naturally produced aflatoxin. Aflatoxin G2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [1].
Aflatoxin M2 is a major metabolite of Aflatoxin B1. Aflatoxin M2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [1].
Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth [1].
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models [1] .
Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase [1] .
Sterigmatocystine (Standard) is the analytical standard of Sterigmatocystine. This product is intended for research and analytical applications. Sterigmatocystine is a precursor of aflatoxins and a mycotoxin produced by common mold strains from Aspergillus versicolor[1] . Sterigmatocystine, a inhibitor of G1 Phase and DNA synthesis, is used to inhibit p21 activity. Sterigmatocystine has teratogenic, and carcinogenic effects in animals .
Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is an orally active mycotoxin produced by Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [1] .
Mevastatin (Standard) is the analytical standard of Mevastatin. This product is intended for research and analytical applications. Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment [1] .
Secalonic acid D is a toxic compound against tumor cells. Secalonic acid D can be isolated from the metabolites of Aspergillus aculeatus. Secalonic acid D activates GSK3-β, and degrades β-catenin. Thus, Secalonic acid D down-regulates c-Myc expression, arrests cell cycle at G1 phase, induces cell apoptosis[1] .
Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations [1] .
Aflatoxin M1 (Standard) is the analytical standard of Aflatoxin M1. This product is intended for research and analytical applications. Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [1].
3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases [1] .
Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cell cycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity [1] .Tunicamycin increases exosome release in cervical cancer cells .
20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity [1] . 20(R)-Ginsenoside Rh2 inhibits the replication and proliferation of mouse and human gammaherpesvirus 68 (MHV-68) with an IC50 of 2.77 μM for murine MHV-68 .
Celangulin XIX is a insecticidal that can be isolated from Celastrus angulatu. Celangulin XIX has strong insecticidal activity against Mythimna separate with an ED50 of 73.3 μg/g .
5-Aminoimidazole ribonucleotide (AIR) is an intermediate in the biosynthesis of purines, as AIR is further modified by additional enzymes to eventually produce inosine monophosphate (IMP), which can then be converted into the purine bases adenine (A) and guanine (G) .
Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research [1] .
Cyclin E controls the G1/S transition of the cell cycle. Cyclin E Protein, Human (SF9, His-GST) is the recombinant human-derived Cyclin E protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of Cyclin E Protein, Human (SF9, His-GST) is 410 a.a., with molecular weight of ~70 kDa.
Cyclin E, a vital regulator in cell cycle control, governs the G1/S transition by forming a potent serine/threonine kinase complex with CDK2. This complex, featuring UHRF2, CDK2, and CCNE1, involves Cyclin E's direct interaction with UHRF2, leading to CCNE1 ubiquitination independently of phosphorylation. Cyclin E's intricate dance with CDK2, CABLES1, and CCNA1 highlights its crucial role in tightly regulated cell cycle progression. Cyclin E Protein, Mouse (SF9, His-GST) is the recombinant mouse-derived Cyclin E protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of Cyclin E Protein, Mouse (SF9, His-GST) is 408 a.a., with molecular weight of ~75 kDa.
The FGF-9 protein undergoes autoproteolysis and cholesterol attachment in the endoplasmic reticulum. It acts as a morphogen during development, inducing ventral cell fate, participating in limb bud patterning, and aiding in axon guidance. FGF-9 binds to the PTCH1 receptor and activates target gene transcription when in association with SMO, while PTCH1 represses SMO signaling in the absence of FGF-9. CDK1-CCNE1 Heterodimer Protein, Human (sf9, His-GST) is a recombinant protein dimer complex containing human-derived CDK1-CCNE1 Heterodimer protein, expressed by Sf9 insect cells , with N-10*His, N-GST labeled tag. CDK1-CCNE1 Heterodimer Protein, Human (sf9, His-GST), has molecular weight of ~109.7 (60.4+49.3) kDa.
CDK3 protein is a serine/threonine protein kinase that plays a key role in regulating the eukaryotic cell cycle, especially affecting the G0-G1 and G1-S transitions. It interacts with CCNC/cyclin-C during interphase and phosphorylates substrates such as histone H1, ATF1, RB1, and CABLES1. CDK3-CCNE1 Heterodimer Protein, Human (Sf9) is a recombinant protein dimer complex containing human-derived CDK3-CCNE1 Heterodimer protein, expressed by Sf9 insect cells , with tag free.
CDK3 protein is a serine/threonine protein kinase that plays a key role in regulating the eukaryotic cell cycle, especially affecting the G0-G1 and G1-S transitions. It interacts with CCNC/cyclin-C during interphase and phosphorylates substrates such as histone H1, ATF1, RB1, and CABLES1. CDK3-CCNE1 Heterodimer Protein, Human (Sf9, GST, FLAG, His) is a recombinant protein dimer complex containing human-derived CDK3-CCNE1 Heterodimer protein, expressed by Sf9 insect cells , with N-6*His, N-Flag, N-GST labeled tag.
The CDK6ic complex is an important serine/threonine protein kinase that regulates cell cycle progression and differentiation, promoting the G1/S transition by phosphorylating substrates such as pRB/RB1 and NPM1. It interacts with D-type G1 cyclins during interphase to form active pRB/RB1 kinase, which controls cell cycle entry. CDK6-CCND2 Heterodimer Protein, Human (Sf9) is a recombinant protein dimer complex containing human-derived CDK6-CCND2 Heterodimer protein, expressed by Sf9 insect cells , with tag free.
The CDK6ic complex is an important serine/threonine protein kinase that regulates cell cycle progression and differentiation, promoting the G1/S transition by phosphorylating substrates such as pRB/RB1 and NPM1. It interacts with D-type G1 cyclins during interphase to form active pRB/RB1 kinase, which controls cell cycle entry. CDK6-CCND3 Heterodimer Protein, Human (Sf9) is a recombinant protein dimer complex containing human-derived CDK6-CCND3 Heterodimer protein, expressed by Sf9 insect cells , with tag free.
The CDK6ic complex is an important serine/threonine protein kinase that regulates cell cycle progression and differentiation, promoting the G1/S transition by phosphorylating substrates such as pRB/RB1 and NPM1. It interacts with D-type G1 cyclins during interphase to form active pRB/RB1 kinase, which controls cell cycle entry. CDK6-CCND2 Heterodimer Protein, Human (Sf9, GST, FLAG, His) is a recombinant protein dimer complex containing human-derived CDK6-CCND2 Heterodimer protein, expressed by Sf9 insect cells , with N-Flag, N-8*His, N-GST labeled tag.
The CDK6ic complex is an important serine/threonine protein kinase that regulates cell cycle progression and differentiation, promoting the G1/S transition by phosphorylating substrates such as pRB/RB1 and NPM1. It interacts with D-type G1 cyclins during interphase to form active pRB/RB1 kinase, which controls cell cycle entry. CDK6-CCND3 Heterodimer Protein, Human (Sf9, GST, His) is a recombinant protein dimer complex containing human-derived CDK6-CCND3 Heterodimer protein, expressed by Sf9 insect cells , with N-10*His, N-GST labeled tag.
The CCND1 protein is a regulatory component of the cyclin D1-CDK4 complex that coordinates phosphorylation and RB family inhibition to regulate the G(1)/S transition. This promotes the dissociation of E2F from the RB/E2F complex and promotes the transcription of E2F target genes critical for G(1) phase progression. CCND1 Protein, Human (His) is the recombinant human-derived CCND1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of CCND1 Protein, Human (His) is 295 a.a., with molecular weight of ~37.7 kDa.
SNTG1 acts as an adapter protein that binds and potentially organizes various proteins, serving as a link between the receptor and the actin cytoskeleton or dystrophin glycoprotein complex. It may modulate the subcellular distribution of diacylglycerol kinase-zeta and contribute to the rapid inactivation of diacylglycerol upon receptor activation. SNTG1 Protein, Human (Myc, His) is the recombinant human-derived SNTG1 protein, expressed by E. coli , with N-His, C-Myc labeled tag. The total length of SNTG1 Protein, Human (Myc, His) is 517 a.a., with molecular weight of ~63.0 kDa.
The CDK6ic complex is an important serine/threonine protein kinase that regulates cell cycle progression and differentiation, promoting the G1/S transition by phosphorylating substrates such as pRB/RB1 and NPM1. It interacts with D-type G1 cyclins during interphase to form active pRB/RB1 kinase, which controls cell cycle entry. CDK6-CCND1 Heterodimer Protein, Human (Sf9) is a recombinant protein dimer complex containing human-derived CDK6-CCND1 Heterodimer protein, expressed by Sf9 insect cells , with tag free.
Serpin G1 protein binds complement and inhibits serine-type endopeptidases. It is located in the extracellular space and is involved in aging. Serpin G1 Protein, Rat (HEK293, His) is the recombinant rat-derived Serpin G1 protein, expressed by HEK293 , with C-His labeled tag. The total length of Serpin G1 Protein, Rat (HEK293, His) is 482 a.a., with molecular weight of ~ 70-95 kDa.
Serpin G1, also known as C1-inhibitor, controls C1 complex activation by forming a proteolytically inactive complex with C1r or C1s proteases. Its interactions regulate physiological pathways like complement activation, blood coagulation, fibrinolysis, and kinin generation. As a potent inhibitor of FXIIa, chymotrypsin, and kallikrein, Serpin G1 binds to E. coli stcE, protecting against complement-mediated lysis, and engages with MASP1, showcasing its intricate involvement in various cellular processes. Serpin G1 Protein, Human (500a.a, HEK293, His) is the recombinant human-derived Serpin G1 protein, expressed by HEK293, with C-10*His labeled tag. The total length of Serpin G1 Protein, Human (500a.a, HEK293, His) is 478 a.a., with molecular weight of ~110 kDa.
Serpin G1 Protein, also called C1-inhibitor, regulates complement activation, blood coagulation, fibrinolysis, and kinin generation. It forms inactive complexes with C1r or C1s proteases, controlling C1 complex activation. Serpin G1 efficiently inhibits FXIIa and possibly chymotrypsin and kallikrein, and interacts with MASP1. Its inhibitory effects maintain pathway balance, preventing excessive activation and ensuring proper physiological function. Serpin G1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Serpin G1 protein, expressed by HEK293, with C-6*His labeled tag. The total length of Serpin G1 Protein, Mouse (HEK293, His) is 485 a.a., with molecular weight of 92-95 kDa.
UBE2G1 Protein, a crucial ubiquitin-proteasome system player, acts as an E2 ubiquitin-conjugating enzyme, facilitating ubiquitin attachment to diverse protein substrates. In vitro, UBE2G1 demonstrates catalytic competence in 'Lys-48' and 'Lys-63'-linked polyubiquitination reactions. This multifaceted enzyme is implicated in potential roles, including the degradation of muscle-specific proteins, emphasizing its involvement in cellular processes related to protein turnover. Additionally, UBE2G1 mediates the polyubiquitination of CYP3A4, a cytochrome P450 enzyme, underscoring its significance in regulating specific cellular pathways. UBE2G1 Protein, Human is the recombinant human-derived UBE2G1 protein, expressed by E. coli, with tag free. The total length of UBE2G1 Protein, Human is 170 a.a., with molecular weight of ~19.5 kDa.
AIF1 protein influences macrophage activation, modulating immune response and cellular activities. Its involvement implies broader influence on immune regulation and inflammation. Studying AIF1's mechanisms in macrophage activation can provide insights into its role in immune homeostasis and signaling pathways governing macrophage functions. AIF1 Protein, Bovine (N-His, C-Myc) is the recombinant bovine-derived AIF1 protein, expressed by E. coli, with C-Myc, N-10*His labeled tag. The total length of AIF1 Protein, Bovine (N-His, C-Myc) is 146 a.a., with molecular weight of 27.6 kDa.
GPR56, a cell adhesion receptor, mediates cell-matrix adhesion in developing neurons and hematopoietic stem cells. It acts as a receptor for collagen III (COL3A1), influencing cortical development and hematopoietic stem cell maintenance. Additionally, GPR56 plays a pivotal role in cancer progression by inhibiting angiogenesis via PRKCA-mediated signaling and is essential for testis development. GPR56 Protein, Human (HEK293, His) is the recombinant human-derived GPR56 protein, expressed by HEK293, with C-His labeled tag. The total length of GPR56 Protein, Human (HEK293, His) is 317 a.a., with molecular weight of 45-70 kDa.
CDK1; cyclin-dependent kinase 1; CDC2, cell division cycle 2, G1 to S and G2 to M; CDC28A; p34 protein kinase; cell cycle controller CDC2; cell division protein kinase 1; cell division control protein 2 homolog; cell division cycle 2, G1 to S and G2 to M; CDC2; P34CDC2; MGC111195; DKFZp686L20222
CDK1; cyclin-dependent kinase 1; CDC2, cell division cycle 2, G1 to S and G2 to M; CDC28A; p34 protein kinase; cell cycle controller CDC2; cell division protein kinase 1; cell division control protein 2 homolog; cell division cycle 2, G1 to S and G2 to M; CDC2; P34CDC2; MGC111195; DKFZp686L20222
CDK1; cyclin-dependent kinase 1; CDC2, cell division cycle 2, G1 to S and G2 to M; CDC28A; p34 protein kinase; cell cycle controller CDC2; cell division protein kinase 1; cell division control protein 2 homolog; cell division cycle 2, G1 to S and G2 to M; CDC2; P34CDC2; MGC111195; DKFZp686L20222
CDK1; cyclin-dependent kinase 1; CDC2, cell division cycle 2, G1 to S and G2 to M; CDC28A; p34 protein kinase; cell cycle controller CDC2; cell division protein kinase 1; cell division control protein 2 homolog; cell division cycle 2, G1 to S and G2 to M; CDC2; P34CDC2; MGC111195; DKFZp686L20222
RVFV is an RNA virus in the Phlebovirus genus of the Bunyaviridae family. The virus is enveloped, spherical, and has a diameter of approximately 80-120 nm. G1 is a glycoprotein that enter the viral envelope to form a ribonucleoprotein complex (RNP) with the N protein. RVFV is a high-risk pathogen that can induce fatal encephalitis and hemorrhagic fever in humans and ruminants. glycoprotein/G1 Protein, RVFV (sf9, His) is the recombinant Virus-derived glycoprotein/G1 protein, expressed by Sf9 insect cells , with C-His labeled tag. The total length of glycoprotein/G1 Protein, RVFV (sf9, His) is 426 a.a., with molecular weight of ~47.8 kDa.
EIF4G1 is a key component of the eIF4F complex and plays a critical regulatory role in translation initiation. EIF4G1 plays different roles in complexes with EIF1 or EIF4E. EIF4G1 Protein, Human (P.pastoris, His) is the recombinant human-derived EIF4G1 protein, expressed by P. pastoris , with N-His labeled tag. The total length of EIF4G1 Protein, Human (P.pastoris, His) is 350 a.a., with molecular weight of ~41.6 kDa.
The PLA2G1B protein is a secreted calcium-dependent phospholipase A2 that targets dietary phospholipids in the intestine. Phosphatidylethanolamine and phosphatidylglycerol are preferred, which hydrolyze the ester bond of the fatty acyl group at the sn-2 position. PLA2G1B Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived PLA2G1B protein, expressed by HEK293 , with C-hFc labeled tag. The total length of PLA2G1B Protein, Mouse (HEK293, Fc) is 124 a.a., with molecular weight of 48-50 kDa.
The PLA2G1B protein is a secreted calcium-dependent phospholipase A2 that targets dietary phospholipids in the intestine. It hydrolyzes the fatty acyl group at the sn-2 position, preferentially hydrolyzing phosphatidylethanolamine and phosphatidylglycerol. PLA2G1B Protein, Human (HEK293, His) is the recombinant human-derived PLA2G1B protein, expressed by HEK293 , with C-6*His labeled tag. The total length of PLA2G1B Protein, Human (HEK293, His) is 126 a.a., with molecular weight of 17-20 kDa.
The PLA2G1B protein is a secreted calcium-dependent phospholipase A2 that targets dietary phospholipids in the intestine. Phosphatidylethanolamine and phosphatidylglycerol are preferred, which hydrolyze the ester bond of the fatty acyl group at the sn-2 position. PLA2G1B Protein, Mouse (HEK293, His) is the recombinant mouse-derived PLA2G1B protein, expressed by HEK293 , with C-6*His labeled tag. The total length of PLA2G1B Protein, Mouse (HEK293, His) is 131 a.a., with molecular weight of ~15.0 kDa.
NTNG1, a master conductor in neural circuit development, intricately guides patterning across laminar, cellular, subcellular, and synaptic dimensions. Its influential role extends to fostering neurite outgrowth for axons and dendrites. In the symphony of neurodevelopment, NTNG1 interacts with NGL1, adding specificity to its involvement in shaping the intricate landscape of neuronal connectivity. NTNG1 Protein, Human (HEK293, His) is the recombinant human-derived NTNG1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of NTNG1 Protein, Human (HEK293, His) is 381 a.a., with molecular weight of ~51.0 kDa.
Apolipoprotein H/APOH proteins have multiple functions and can bind to negatively charged substances such as heparin and phospholipids. Its diverse interactions highlight the adaptability that is critical for preventing activation of the intrinsic coagulation cascade by binding to phospholipids on the surface of damaged cells. Apolipoprotein H/APOH Protein, Rat (HEK293, His) is the recombinant rat-derived Apolipoprotein H/APOH protein, expressed by HEK293 , with C-His labeled tag. The total length of Apolipoprotein H/APOH Protein, Rat (HEK293, His) is 345 a.a., with molecular weight of 45-70 kDa.
NTNG1, a master conductor in neural circuit development, intricately guides patterning across laminar, cellular, subcellular, and synaptic dimensions. Its influential role extends to fostering neurite outgrowth for axons and dendrites. In the symphony of neurodevelopment, NTNG1 interacts with NGL1, adding specificity to its involvement in shaping the intricate landscape of neuronal connectivity. NTNG1 Protein, Human (Biotinylated, HEK293, Avi-His) is the recombinant human-derived NTNG1 protein, expressed by HEK293 , with C-Avi, C-6*His labeled tag. The total length of NTNG1 Protein, Human (Biotinylated, HEK293, Avi-His) is 381 a.a., with molecular weight of 55-65 kDa.
The CD1D protein, a key antigen-presenting molecule, binds self and non-self glycolipids, presenting them to T-cell receptors on natural killer T-cells. Partnering with B2M, it centrally orchestrates immune responses, and its interactions with MHC II emphasize its significance in the intricate network of immune system regulation. CD1D Protein, Human (HEK293, His) is the recombinant human-derived CD1D protein, expressed by HEK293, with C-His labeled tag. The total length of CD1D Protein, Human (HEK293, His) is 301 a.a., with molecular weight of 45-50 kDa.
CD1D protein, in partnership with B2M, functions as an antigen-presenting protein, binding self and non-self glycolipids. It presents these molecules to T-cell receptors on natural killer T-cells, playing a pivotal role in immune responses. CD1D also interacts with MHC II and CD74, contributing to the coordination of the adaptive immune system. CD1D Protein, Mouse (HEK293, His) is the recombinant mouse-derived CD1D protein, expressed by HEK293 , with C-His labeled tag. The total length of CD1D Protein, Mouse (HEK293, His) is 305 a.a., with molecular weight of 45-50 kDa.
Apolipoprotein H Protein, Human (HEK293, His) expresses in HEK293 with a His tag at the N-terminus. Apolipoprotein H (ApoH) is the main target of anti-phospholipid antibodies (aPLs) found in many patients with systemic lupus erythematosus and antiphospholipid syndrome (APS).
Apolipoprotein H Protein, Mouse (HEK293, His) expresses in HEK293 with a His tag at the N-terminus. Apolipoprotein H (ApoH) is the main target of anti-phospholipid antibodies (aPLs) found in many patients with systemic lupus erythematosus and antiphospholipid syndrome (APS).
CD1D protein, in partnership with B2M, functions as an antigen-presenting protein, binding self and non-self glycolipids. It presents these molecules to T-cell receptors on natural killer T-cells, playing a pivotal role in immune responses. CD1D also interacts with MHC II and CD74, contributing to the coordination of the adaptive immune system. CD1D Protein, Mouse (HEK293, His-Fc) is the recombinant mouse-derived CD1D protein, expressed by HEK293 , with C-hFc, C-His labeled tag. The total length of CD1D Protein, Mouse (HEK293, His-Fc) is 305 a.a., with molecular weight of ~60.4 kDa.
The CSNK1G1 protein is a member of the casein kinase family that preferentially phosphorylates acidic proteins, including casein, exhibiting broad substrate specificity. Functionally, it actively participates in the Wnt signaling pathway and regulates cellular responses. CSNK1G1 Protein, Human (sf9, His-GST) is the recombinant human-derived CSNK1G1 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
Apolipoprotein H/APOH protein binds to heparin, phospholipids, and dextran sulfate, preventing activation of the blood coagulation cascade by interacting with phospholipids on damaged cell surfaces. Apolipoprotein H/APOH Protein, Mouse (HEK293, C-His) is the recombinant mouse-derived Apolipoprotein H/APOH protein, expressed by HEK293, with C-His labeled tag. The total length of Apolipoprotein H/APOH Protein, Mouse (HEK293, C-His) is 326 a.a., with molecular weight of 55-75 kDa.
Lymphocyte antigen 6G/LY6G protein is uniquely expressed in bone marrow, indicating its involvement in the hematopoietic microenvironment. This suggests a role in regulating immune cell development or function within the bone marrow niche. Lymphocyte antigen 6G/LY6G Protein, Mouse (P.pastoris) is the recombinant mouse-derived Lymphocyte antigen 6G/LY6G protein, expressed by P. pastoris , with N-6*His labeled tag. The total length of Lymphocyte antigen 6G/LY6G Protein, Mouse (P.pastoris) is 93 a.a., with molecular weight (glycosylation form) of ~34 kDa.
NGL-1/LRRC4C protein promotes neurite outgrowth in thalamic neurons, shaping neural circuit architecture. It interacts with NTNG1 and WHRN to modulate neurite outgrowth and synaptic connections. Investigating its mechanisms and downstream effects could provide insights into its role in neural development and circuit formation. NGL-1/LRRC4C Protein, Mouse (HEK293, His) is the recombinant mouse-derived NGL-1/LRRC4C protein, expressed by HEK293 , with C-His labeled tag. The total length of NGL-1/LRRC4C Protein, Mouse (HEK293, His) is 527 a.a., with molecular weight of ~55.5 KDa.
NGL-1/LRRC4C protein may promote neurite outgrowth of thalamic neurons, suggesting a role in neurodevelopment. The specific molecular mechanisms and their interactions with NTNG1 and WHRN require further study. NGL-1/LRRC4C Protein, Human (527a.a, HEK293, His) is the recombinant human-derived NGL-1/LRRC4C protein, expressed by HEK293 , with C-His labeled tag. The total length of NGL-1/LRRC4C Protein, Human (527a.a, HEK293, His) is 483 a.a., with molecular weight of ~55.51 KDa.
Apolipoprotein H/APOH proteins have multiple functions and can bind to negatively charged substances such as heparin and phospholipids. Its diverse interactions highlight the adaptability that is critical for preventing activation of the intrinsic coagulation cascade by binding to phospholipids on the surface of damaged cells. Apolipoprotein H/APOH Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived Apolipoprotein H/APOH protein, expressed by HEK293 , with C-His labeled tag. The total length of Apolipoprotein H/APOH Protein, Cynomolgus (HEK293, His) is 326 a.a., with molecular weight of 50-65 kDa.
The CD1D protein, a key antigen-presenting molecule, binds self and non-self glycolipids, presenting them to T-cell receptors on natural killer T-cells. Partnering with B2M, it centrally orchestrates immune responses, and its interactions with MHC II emphasize its significance in the intricate network of immune system regulation. CD1D-B2M Heterodimer Protein, Human (HEK293, His) is a recombinant protein dimer complex containing human-derived CD1D-B2M Heterodimer protein, expressed by HEK293, with C-His labeled tag. CD1D-B2M Heterodimer Protein, Human (HEK293, His), has molecular weight of ~48 & 12 kDa, respectively.
Hemagglutinin (HA) protein is crucial for virus attachment to host cells, binding to sialic acid receptors and initiating virion internalization through clathrin-dependent or -independent pathways. As a Class I viral fusion protein, HA determines host range and virulence, mediating virus penetration into the cell cytoplasm. Its fusion role between the endocytosed virus and endosomal membranes is vital for infection. Acidic endosomal conditions prompt an irreversible HA2 conformational change, releasing the fusion peptide. Cooperative trimer action forms a fusion pore, highlighting HA's intricate role in viral entry. Hemagglutinin/HA Protein, H4N4 (Q0A4G1, HEK293, His) is the recombinant Virus-derived Hemagglutinin/HA protein, expressed by HEK293, with C-His labeled tag. The total length of Hemagglutinin/HA Protein, H4N4 (Q0A4G1, HEK293, His) is 528 a.a., with molecular weight of ~65 kDa.
PSG1 Protein is extremely vital to development and health of a fetus. PSG1 Protein is important in inducing, enhancing or inhibiting an immune response. PSG1 Protein, Human (HEK293, His) is the recombinant human-derived PSG1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of PSG1 Protein, Human (HEK293, His) is 385 a.a., with molecular weight of ~68 kDa.
PSG1 Protein is extremely vital to development and health of a fetus. PSG1 Protein is important in inducing, enhancing or inhibiting an immune response. PSG1 Protein, Human (HEK293, Fc) is the recombinant human-derived PSG1 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of PSG1 Protein, Human (HEK293, Fc) is 419 a.a., with molecular weight of ~70.2 kDa.
Hemagglutinin (HA) protein is crucial for virus attachment to host cells, binding to sialic acid receptors and initiating virion internalization through clathrin-dependent or -independent pathways. As a Class I viral fusion protein, HA determines host range and virulence, mediating virus penetration into the cell cytoplasm. Its fusion role between the endocytosed virus and endosomal membranes is vital for infection. Acidic endosomal conditions prompt an irreversible HA2 conformational change, releasing the fusion peptide. Cooperative trimer action forms a fusion pore, highlighting HA's intricate role in viral entry. HA1/Hemagglutinin Protein, H4N4 (Q0A4G1, HEK293, His) is the recombinant Virus-derived HA1/Hemagglutinin protein, expressed by HEK293, with C-His labeled tag. The total length of HA1/Hemagglutinin Protein, H4N4 (Q0A4G1, HEK293, His) is 343 a.a., with molecular weight of ~50 KDa.
TREM-2 Protein is an immune receptor expressed on immune and non-immune cells. It is an anti-inflammatory molecule and considered a marker for microglia activation. CD1E-B2M Heterodimer Protein, Cynomolgus (HEK293, His) is a recombinant protein dimer complex containing cynomolgus-derived CD1E-B2M Heterodimer protein, expressed by HEK293 , with N-His labeled tag. CD1E-B2M Heterodimer Protein, Cynomolgus (HEK293, His), has molecular weight of ~37.8 & 13.6 kDa, respectively.
ZNHIT1 is a key chromatin remodeling protein that regulates gene expression by promoting the incorporation of histone variants H2AZ1/H2A.Z. In muscle differentiation, ZNHIT1 is recruited to the MYOG promoter, mediating H2AZ1 binding and inducing muscle-specific gene expression. ZNHIT1 Protein, Human (His) is the recombinant human-derived ZNHIT1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of ZNHIT1 Protein, Human (His) is 154 a.a., with molecular weight of ~21.0 kDa.
Together with its regulatory partners CCNH and MNAT1, CDK7 functions as an important serine/threonine kinase in cell cycle regulation and RNA polymerase II-mediated transcription. As the catalytic subunit of the CDK-activated kinase (CAK) complex, CDK7 plays a key role in activating CDK1/cyclin-B and CDK2/cyclin during cell cycle transitions. CDK7-CCNH-MNAT1 Protein, Human (Sf9) is the recombinant human-derived CDK7-CCNH-MNAT1 protein, expressed by Sf9 insect cells , with tag free.
Thymidine-d4 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1][2][3].
Aflatoxin G1- 13C17 is the 13C labeled Aflatoxin G1 (HY-N6697) [1]. Aflatoxin G1 is one type of aflatoxins occuring in nature. It is produced by molds, such as Aspergillus flavus and Aspergillus parasiticus. Aflatoxins are hepatogenic, teratogenic, imunosuppressive, and carcinogenic fungal metabolites found in feeds, nuts, wine-grapes, spices, and other grain crops .
Thymidine- 13C is the 13C labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1]
Thymidine-d2 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1
Thymidine-d3 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1][2][3].
Thymidine-2′- 13C is the 13C labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1]<
Thymidine- 13C-2 is the 13C labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1]
Thymidine- 13C-1 is the 13C labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1]
Thymidine- 15N2 is the 15N labeled Thymidine[1]. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[2][3][4].
Thymidine- 13C10, 15N2 is the 13C and 15N labeled Thymidine[1]. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[2][3][4].
Thymidine-d14 (DThyd-d14; NSC 21548-d14) is deuterium labeled Thymidine (HY-N1150). Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
Thymidine- 13C10 (DThyd- 13C10; NSC 21548- 13C10) is 13C-labeled Thymidine (HY-N1150). Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
Isoeugenol-d3 is deuterated labeled Sterigmatocystine (HY-N6725). Sterigmatocystine is a precursor of aflatoxins and a mycotoxin produced by common mold strains from Aspergillus versicolor[1] . Sterigmatocystine, a inhibitor of G1 Phase and DNA synthesis, is used to inhibit p21 activity. Sterigmatocystine has teratogenic, and carcinogenic effects in animals .
Aflatoxin G2- 13C17 is the 13C labeled Aflatoxin G2 (HY-N6698) [1]. Aflatoxin G2 is a major naturally produced aflatoxin. Aflatoxin G2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 .
Aflatoxin M2- 13C17 is the 13C labeled Aflatoxin M2 (HY-N6700) [1]. Aflatoxin M2 is a major metabolite of Aflatoxin B1. Aflatoxin M2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 .
Aflatoxin M1- 13C17 is the 13C labeled Aflatoxin M1 (HY-N6699) [1]. Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 .
Aflatoxin B2- 13C17 is 13C- and 15N-labeled Aflatoxin B2 (HY-N6696). Aflatoxin B2 is a major naturally produced aflatoxin. Aflatoxin B2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2 [1] .
1-Octanol-d5 is deuterated labeled Carvacrol (HY-N0711). Carvacrol is an orally active monoterpenic phenol that can be extract from an abundant number of aromatic plants, including thyme and oregano, possessing antioxidant, antibacterial, antifungal, anticancer, anti-inflammatory, hepatoprotective, spasmolytic, and vasorelaxant properties. Carvacrol also causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis. Carvacrol is used in low concentrations as a food flavoring ingredient and preservative, as well as a fragrance ingredient in cosmetic formulations [1] .
TAT-p16 (p16INK4a peptide) is a peptide mimic of p16INK4a that can induce an early G phase cell cycle arrest in the absence of active cyclin E:Cdk2 complex [1].
Cyclin E1 Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 47 kDa, targeting to Cyclin E1. It can be used for WB,IHC-F,IHC-P,ICC/IF,ELISA assays with tag free, in the background of Human, Mouse, Rat.
Phospho-Cyclin E1 (Thr395) Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 47 kDa, targeting to Phospho-Cyclin E1 (Thr395). It can be used for WB assays with tag free, in the background of Human.
eIF4G1 Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 175 kDa, targeting to eIF4G1. It can be used for WB,IHC-P,ICC/IF assays with tag free, in the background of Human, Mouse, Rat.
c-Fos Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 41 kDa, targeting to c-Fos. It can be used for ICC/IF,WB,IHC-F,IHC-P,ELISA assays with tag free, in the background of Human, Mouse, Rat.