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HG106 is a potent SLC7A11 inhibitor. HG106 markedly decreased cystine uptake and intracellular glutathione biosynthesis. HG106 can be used for the research of KRAS-mutant lung adenocarcinoma .
HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation .
HG2 is a fast-acting antimicrobial peptide. HG2 shows anti-biofilm and anti-inflammatory activities. HG2 is active against Gram-positive pathogens, especially against MRSA strains (MIC: 16-32?μg/mL). HG2 can bind to bacterial lipids and reduces ATP concentration in S. aureus MRSA USA300 cells .
HG4 is a fast-acting antimicrobial peptide. HG4 shows anti-biofilm and anti-inflammatory activities. HG4 is active against Gram-positive pathogens, especially against MRSA strains (MIC: 32-64?μg/mL). HG4 can bind to bacterial lipids and reduces ATP concentration in S. aureus MRSA USA300 cells .
HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC50 values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC50 values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research .
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
HG-14-10-04 is a potent ALK and mutant EGFR inhibitor with IC50s of 20 nM, 15.6 nM, 22.6 nM and 124.5 nM for ALK, EGFR LR/TM, EGFR 19del/TM/CS and EGFR LR/TM/CS, respectively. HG-14-10-04 can be used to research anticancer .
HG-7-85-01-NH2 is the ligand of SNIPER(ABL)-033. SNIPER(ABL)-033, conjugating HG-7-85-01 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 value of 0.3 μM .
HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIK) inhibitor with IC50s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3 respectively.
HG6-64-1 is a potent and selective B-Raf inhibitor extracted from patent WO 2011090738 A2, example 9 (XI-1); has a IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells.
H-Gly-Pro-Gly-NH2 is a tripeptide that inhibits HIV-1 replication. H-Gly-Pro-Gly-NH2 inhibits the activity of HIV-1 IIIB and HIV-2 ROD with EC50 values of 35 µM and 30 µM, respectively. H-Gly Pro Gly NH2 inhibits HIV-1 replication in vitro by interfering with capsid formation. H-Gly Pro Gly NH2 has antiviral activity and can be used for virus research .
H-Gly-Sar-Sar-OH is an orally active tripeptide. H-Gly-Sar-Sar-OH is transported through PepT1 within Caco-2 cells. H-Gly Sar Sar OH has potential applications in material transportation .
H-(Gly)3-Lys(N3)-OH (hydrochloride) is a click chemistry reagent. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity .
TFMB-(R)-2-HG, a cell membrane-permeable version of (R)-2-HG, is a carcinogenic factor in Acute myeloid leukemia (AML).
TFMB-(R)-2-HG impairs SCF ER-Hoxb8 cells differentiation in response to estrogen withdrawal .
TFMB-(S)-2-HG is a potent inhibitor of the 5'-methylcytosine hydroxylase TET2. TFMB-(S)-2-HG also inhibits the EglN prolyl hydroxylases. TFMB-(S)-2-HG has the potential for the research of acute myeloid leukemia (AML) .
GST-HG131 is a specific inbihitor of hepatitis B virus (HBV) surface antigen, belongs to dihydrobenzopyridooxazepine (DBP) series. GST-HG131 exhibits excellent and specific HBV antigens inhibition with EC50 of 28.2 nM (HBsAg) and 16.0 nM (HBeAg), respectively, but also it is safety for animal .
PH-HG-005-5 (compound 16c) is a derivative of SN-38 (HY-13704) and can be used as Drug-Linker Conjugates for ADC. PH-HG-005-5 can conjugate to targeting peptides for ADCs synthesis .
o-Pah is a BODIPY derivative with an -NH2 and -OH substituted meso-Ph group. o-Pah exhibits metal-induced J-aggregation in the presence of Cu 2+ and a specific fluorescence enhancement for Hg2+ (Ex/Em=483/(495-600) nM) .
SNIPER(ABL)-044, conjugating HG-7-85-01 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM .
SNIPER(ABL)-047, conjugating HG-7-85-01 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 2 μM .
SNIPER(ABL)-033, conjugating HG-7-85-01 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM .
Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity .
Nrf2 activator-9 (compound D-36) is an Nrf2 activator that inhibits oxidized low-density lipoprotein (oxLDL) and high glucose (HG)-induced apoptosis in HUVEC cells. Nrf2 activator-9 inhibits oxLDL and HG-induced vascular endothelial cell (VEC) injury and can effectively prevent and treat atherosclerosis .
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
(2R)-Octyl-α-hydroxyglutarate (sodium) is the sodium salt form of (2R)-Octyl-α-hydroxyglutarate. (2R)-Octyl-α-hydroxyglutarate has anti-inflammatory effects .
mIDH1-IN-1 (compound 43) is a potent and selective mIDH1 (mutant isocitrate dehydrogenases 1) inhibitor, with an IC50 of 961.5 nM. mIDH1-IN-1 potently inhibits intracellular 2-HG (2-hydroxyglutarate) production in HT1080 cells, with an EC50 of 208.6 ± 8.0 nM. mIDH1-IN-1 shows a significant anti-proliferation activity on IDH1 mutant-U-87 cells, with an IC50 of 41.8 nM. mIDH1-IN-1 is an antitumor agent, and can be used for IDH1 mutated solid tumors research .
Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K .
(S,R)-GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-GSK321 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-GSK321can be used for research of acute myeloid leukemia (AML) and other cancers .
IDH2 R140Q-IN-2 (compound 36) is an an orally active IDH2 R140Q inhibitor (IC50: 29 nM). IDH2 R140Q-IN-2 reduces D2HG production in TF-1 cell lines expressing mutant IDH2 R140Q (IC50: 10 nM). IDH2 R140Q-IN-2 suppresses D2HG levels in tumor tissue. IDH2 R140Q-IN-2 can be used for research of acute myeloid leukemia (AML) .
Cariporide is a Na+/H+ Exchanger 1 (NHE-1) inhibitor. Cariporide inhibits the expression of monocyte endothelial cell adhesion and intercellular adhesion molecule-1 (ICAM-1) mediated by high glucose (HG) by inhibiting the activation of NHE-1 .
(1R)-IDH889 is the isomer of IDH889 (HY-112289), and can be used as an experimental control. IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .
OAT1/3-IN-1 (compound 7) is a dual inhibitor of OAT1 and OAT3. OAT1/3-IN-1 can reverse the toxicity of Cys-Hg on HEK-OAT1 cells (10 μM) and has a potential protective effect on the kidneys. OAT1/3-IN-1 can be used to study mercury-induced kidney damage .
OAT1/3-IN-2 (compound 8) is a dual inhibitor of OAT1 and OAT3. OAT1/3-IN-2 can reverse the toxicity of Cys-Hg on HEK-OAT1 cells (10 μM) and has a potential protective effect on the kidneys. OAT1/3-IN-2 can be used to study mercury-induced kidney damage .
EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo. EHT 1864 dependently suppresses the release of migrasomes from podocytes induced by LPS, PAN, or HG .
o-Pah is a BODIPY derivative with an -NH2 and -OH substituted meso-Ph group. o-Pah exhibits metal-induced J-aggregation in the presence of Cu 2+ and a specific fluorescence enhancement for Hg2+ (Ex/Em=483/(495-600) nM) .
HG2 is a fast-acting antimicrobial peptide. HG2 shows anti-biofilm and anti-inflammatory activities. HG2 is active against Gram-positive pathogens, especially against MRSA strains (MIC: 16-32?μg/mL). HG2 can bind to bacterial lipids and reduces ATP concentration in S. aureus MRSA USA300 cells .
HG4 is a fast-acting antimicrobial peptide. HG4 shows anti-biofilm and anti-inflammatory activities. HG4 is active against Gram-positive pathogens, especially against MRSA strains (MIC: 32-64?μg/mL). HG4 can bind to bacterial lipids and reduces ATP concentration in S. aureus MRSA USA300 cells .
HGly-Pro-Hyp-OH (Tripeptide 29) is an orally active bioactive peptide against UVB-induced skin aging and has been reported used as a cosmetic ingredient [1]
H-Gly-Pro-Gly-NH2 is a tripeptide that inhibits HIV-1 replication. H-Gly-Pro-Gly-NH2 inhibits the activity of HIV-1 IIIB and HIV-2 ROD with EC50 values of 35 µM and 30 µM, respectively. H-Gly Pro Gly NH2 inhibits HIV-1 replication in vitro by interfering with capsid formation. H-Gly Pro Gly NH2 has antiviral activity and can be used for virus research .
G6PI 325-339 (human) is an efficient inducer of arthritis in B10.Q mice. G6PI 325-339 (human) primes Th1 and Th17 cells cross-reacted with the murine G6PI protein. G6PI 325-339 (human) induces arthritis model operating through a T and B cell-dependent pathway but without antibody effector mechanisms .
H-Gly-Sar-Sar-OH is an orally active tripeptide. H-Gly-Sar-Sar-OH is transported through PepT1 within Caco-2 cells. H-Gly Sar Sar OH has potential applications in material transportation .
G6PI 325-339 (human) hydrochloride is an efficient inducer of arthritis in B10.Q mice. G6PI 325-339 (human) hydrochloride primes Th1 and Th17 cells cross-reacted with the murine G6PI protein. G6PI 325-339 (human) hydrochloride induces arthritis model operating through a T and B cell-dependent pathway but without antibody effector mechanisms .
OAT1/3-IN-1 (compound 7) is a dual inhibitor of OAT1 and OAT3. OAT1/3-IN-1 can reverse the toxicity of Cys-Hg on HEK-OAT1 cells (10 μM) and has a potential protective effect on the kidneys. OAT1/3-IN-1 can be used to study mercury-induced kidney damage .
OAT1/3-IN-2 (compound 8) is a dual inhibitor of OAT1 and OAT3. OAT1/3-IN-2 can reverse the toxicity of Cys-Hg on HEK-OAT1 cells (10 μM) and has a potential protective effect on the kidneys. OAT1/3-IN-2 can be used to study mercury-induced kidney damage .
EBP1 protein participates in the signal transduction pathway regulated by ERBB3 and is related to growth regulation. As an androgen receptor (AR) corepressor, it is regulated by the ERBB3 ligand neregulin-1/heregulin (HRG). EBP1 Protein, Human (His) is the recombinant human-derived EBP1 protein, expressed by E. coli , with N-His labeled tag. The total length of EBP1 Protein, Human (His) is 393 a.a., with molecular weight of ~32 kDa.
The Lgr5/GPR49 protein is a receptor for R-spondins that enhances the canonical Wnt signaling pathway and marks stem cells in the intestinal epithelium and hair follicles. Lgr5/GPR49 binds R-spondins (RSPO1-4), binds to phosphorylated LRP6 and Frizzled receptors, initiates Wnt signaling and amplifies target gene expression. Lgr5/GPR49 Protein, Human (HEK293, hFc) is the recombinant human-derived Lgr5/GPR49 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of Lgr5/GPR49 Protein, Human (HEK293, hFc) is 522 a.a., with molecular weight of 110-120 kDa.
Lgr5/GPR49 Protein, the receptor for R-spondins, potentiates the canonical Wnt signaling pathway and marks stem cells in the intestinal epithelium and hair follicle. Binding R-spondins (RSPO1-4), Lgr5/GPR49 associates with phosphorylated LRP6 and frizzled receptors, initiating Wnt signaling and amplifying target gene expression. Unlike classical G-protein coupled receptors, Lgr5/GPR49 does not activate heterotrimeric G-proteins, showcasing its unique regulatory role in Wnt signaling. It's crucial for adult intestinal stem cell development and maintenance, identified in a complex with RNF43 and RSPO1, and interacts with RSPO2-4, demonstrating diverse participation in cellular signaling pathways. Lgr5/GPR49 Protein, Human (CHO, hFc) is the recombinant human-derived Lgr5/GPR49 protein, expressed by CHO, with C-hFc labeled tag. The total length of Lgr5/GPR49 Protein, Human (CHO, hFc) is 539 a.a., with molecular weight of 88-110 kDa.
