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(S)-Crizotinib is a potent and selective MTH1 (mutT homologue) inhibitor with an IC50 of 330 nM. (S)-Crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induces an increase in DNA single strand breaks, activates DNA repair in human colon carcinoma cells, and effectively suppresses tumour growth in animal models .
ML179 (SR-1309) is a inverse LRH1 (Liver receptor homologue-1) agonist with IC50 of 320 nM. ML179 shows anti-proliferation activity in MDA-MB-231 cells. ML179 has the potential for the research of ER-negative breast cancer .
24-norursodeoxycholic acid (Norucholic acid) is a side chain-shortened C23homologue of UDCA and has shown potent anti-cholestatic, anti-inflammatory and anti-fibrotic properties.
Iso-RJW100 (compound 24-endo) is a dual-liver receptor homologue-1 (LRH-1) and steroidogenic factor-1 (SF-1) agonist with pEC50 of 6.4 and 7.2, respectively .
Ceanothic acid (Emmolic acid) is a ring-A homologue of betulinic acid. Ceanothic acid inhibits OVCAR-3, HeLa, and FS-5 cells with the cell survival of 68%, 65%, and 81%, respectively .
H-HoArg-OH-d4 is a deuterium labeled H-HoArg-OH (HY-W008385). H-HoArg-OH, a homologue arginine, is a strong inhibitor of human bone and liver alkaline phosphatase.
3-Pyridylacetic acid (hydrochloride) (Standard) is the analytical standard of 3-Pyridylacetic acid (hydrochloride). This product is intended for research and analytical applications. 3-Pyridineacetic acid hydrochloride is a higher homologue of nicotinic acid, a breakdown product of nicotine (and other tobacco alkaloids) .
3-Isomangostin, extracted from Garciniamangostana.L. shell, is a potent MutT homologue 1 (MTH1) inhibitor with an IC50 value of 52 nM. 3-Isomangostin would be an attractive chemical tool for the development of anticancer agents .
3-Pyridylacetic acid-d4 (hydrochloride) is the deuterium labeled 3-Pyridylacetic acid hydrochloride[1]. 3-Pyridineacetic acid hydrochloride is a higher homologue of nicotinic acid, a breakdown product of nicotine (and other tobacco alkaloids)[2][3].
ALLO-1, an autophagy receptor, is essential for autophagosome formation around paternal organelles and directly binds to the worm LC3 homologue LGG-1 through its LC3-interacting region (LIR) motif .
Danburstotug (IMC-001) is an IgG1-lambda anti-CD274 (PDL1, B7 homologue 1, B7H1) human monoclonal antibody. Danburstotug also is immunostimulant and antineoplastic .
EZH2-IN-21 is a potent inhibitor of the histone lysine methyltransferase enhancer of zeste homologue 2 (EZH2) with anticancer activity. EZH2-IN-21 is competitive with the cofactor SAM and noncompetitive with peptide or nucleosome substrates .
Azetidine-2-carboxylic acid is a non proteinogenic amino acid homologue of proline. Found in common beets. Azetidine-2-carboxylic acid can be misincorporated into proteins in place of proline in many species, including humans. Toxic and teratogenic agent .
EZH2-IN-18 (compound 9e) is a potent inhibitor of enhancer of zeste homologue 2 (EZH2WT) , with the IC50 of 1.01 nM. EZH2-IN-18 shows inhibition in proliferation and induction in apoptosis in tumor cells .
LB244 is a homologue of BB-Cl-amidine, which is an orally effective STING inhibitor (EC50=0.8 μM) and can be used to inhibit STING-dependent inflammatory diseases. The pharmacokinetic properties of LB244 indicate limited oral activity in mice .
SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues .
QStatin is a potent and selective inhibitor of SmcR (V. harveyi LuxR homologue) with an EC50 of 208.9 nM, binding tightly to SmcR and changes the flexibility of the protein, thereby altering its transcription regulatory activity. QStatin shows pan-QS (Vibrio quorum sensing) inhibitor activity in diverse Vibrio species and attenuates their virulence in an aquatic host. QStatin may be a sustainable antivibriosis agent useful in aquacultures .
AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains (mean IC50=32 nM), Ugandan field isolates (mean ex vivo IC50=64 nM), and murine P. berghei and P. falciparum infections .
SOS1 agonist-1 (compound 79) is an agonist for the Son of sevenless homologue SOS1. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP to GTP on RAS and regulates RAS activation. SOS1 agonists increase nucleotide exchange on RAS, enhance cellular RAS-GTP levels, and trigger biphasic signaling changes in ERK1/2 phosphorylation. Play an anti-cancer role [1] .
DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N 6 methyladenosine (m 6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4−11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research .
KU-177 is a potent inhibitor of Hsp90 ATPase homologue 1 (Aha1), ablates Aha1-driven enhancement of Hsp90-dependent tau aggregation. KU-177 also disrupts Aha1/Hsp90 interactions (IC50=4.08 μM) without inhibition of Hsp90’s ATPase activity. KU-177 can be used for tauopathies research .
ts-SA is a carbonic anhydrase (CA) inhibitor with activity against seven human CA homologues. ts-SA can bind to the Zn(II) ion in the enzyme active site in a deprotonated form. The organic skeleton of ts-SA extends in the enzyme cavity and participates in multiple interactions with amino acid residues and water molecules. Due to its structural differences, the inhibitory performance of ts-SA is significantly better than that of another pyridine derivative. ts-SA exhibits low nanomolar inhibitory activity and is a multi-target CA inhibitor .
DapL-IN-1 is an inhibitor of L,L-diaminoheptanoic acid aminotransferase (DapL) with the characteristics of inhibiting DapL activity in bacteria and plants. DapL-IN-1 can be used to design and discover new biocides such as antibiotics, herbicides or algaecides with the potential to be non-toxic to animals. DapL-IN-1 shows differential sensitivity in inhibiting different DapL homologues, which can provide important information for further drug development. DapL-IN-1 may affect its biological activity by affecting the interaction with residues adjacent to the active site, which may lead to different binding modes .
CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12 .
SMARCA2-IN-8 (Compound 13) is an orally active inhibitor for SWI/SNF chromatin remodeling complexe SMARCA2 (also known as Brahma homologue, BRM) and SMARCA4 (also known as Brahma-related gene 1, BRG1) with IC50 of 5 and 6 nM. SMARCA2-IN-8 inhibits the proliferation of SMARCA2 mutated cancer cell SKMEL5 with AAC50 of 5 nM. SMARCA2-IN-8 downregulates the SMARCA2-dependent KRT80 gene expression with AAC50 of 10 nM. SMARCA2-IN-8 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice .
CHET3 is a sex-selective activator with potent analgesic activity. CHET3 was discovered to be a highly selective omnidirectional modulator of TASK-3-containing K2P channels, including TASK-3 homologues and TASK-3/TASK-1 heterologues. CHET3 exhibited significant analgesic effects in multiple acute and chronic pain models in mice, which could be abolished by pharmacological means or genetic knockout of TASK-3. CHET3 is able to functionally modulate the membrane excitability of specific small sensory neurons, which supports its analgesic effects on thermal hypersensitivity and mechanical hyperalgesia in chronic pain .
K103 is an inhibitor discovered from the screen that is an analog of the serotonin antagonist benzazocine. K103 exhibited inhibition of SHIP homologues, labelling it a pan-SHIP1/2 inhibitor, but the molecule had no effect on another 5' inositol phosphatase, OCRL. In line with the "two PIPs hypothesis", the molecule exhibited significant anti-tumour effects against a variety of cell lines, particularly breast cancer cells. Additional studies with K103 revealed that inhibition of SHIP1/2 in multiple myeloma cells resulted in G2/M cell cycle arrest followed by extensive apoptosis via activation of the caspase cascade. K103 fits the commonly used small molecule agent property profile, but while this work was being conducted, it was discovered that K103 caused psychoactive effects in mice, which limited the utility of the molecule in vivo. Therefore, certain synthetic studies were conducted on this tryptamine to identify the features that needed to be present in the molecule to maintain pan-SHIP1/2 inhibition in order to design an inhibitor with favourable pharmacodynamic properties and an improved side effect profile.
Tnrnflrfamide is a neuropeptide that modulates the receptor muscles of the lobster abdominal stretch receptors and their exoskeletal muscle homologues. Tnrnflrfamide enhances motor performance, including the amplitude of excitatory postsynaptic potentials and the development of nerve-evoked tension .
Danburstotug (IMC-001) is an IgG1-lambda anti-CD274 (PDL1, B7 homologue 1, B7H1) human monoclonal antibody. Danburstotug also is immunostimulant and antineoplastic .
Ceanothic acid (Emmolic acid) is a ring-A homologue of betulinic acid. Ceanothic acid inhibits OVCAR-3, HeLa, and FS-5 cells with the cell survival of 68%, 65%, and 81%, respectively .
3-Isomangostin, extracted from Garciniamangostana.L. shell, is a potent MutT homologue 1 (MTH1) inhibitor with an IC50 value of 52 nM. 3-Isomangostin would be an attractive chemical tool for the development of anticancer agents .
Azetidine-2-carboxylic acid is a non proteinogenic amino acid homologue of proline. Found in common beets. Azetidine-2-carboxylic acid can be misincorporated into proteins in place of proline in many species, including humans. Toxic and teratogenic agent .
3-Pyridylacetic acid (hydrochloride) (Standard) is the analytical standard of 3-Pyridylacetic acid (hydrochloride). This product is intended for research and analytical applications. 3-Pyridineacetic acid hydrochloride is a higher homologue of nicotinic acid, a breakdown product of nicotine (and other tobacco alkaloids) .
OX40 (TNFRSF4), is a receptor for OX40 Ligand. OX40 is preferentially expressed by T cells. OX40 can be activated by OX40 Ligand, thereby functioning as a T cell co-stimulatory molecule. The OX40-OX40 Ligand interaction promotes effector T-cell survival and effectively induces memory T-cell generation, as well as enhances the helper function of Tfh for B cells, and also promotes the differentiation and maturation of DCs. OX40/TNFRSF4 Protein, Mouse (His-Avi) is a recombinant mouse OX40 (V20-P211) with C-terminal Avi and His tag, which is produced in HEK293.
OX40 (TNFRSF4), is a receptor for OX40 Ligand. OX40 is preferentially expressed by T cells. OX40 can be activated by OX40 Ligand, thereby functioning as a T cell co-stimulatory molecule. The OX40-OX40 Ligand interaction promotes effector T-cell survival and effectively induces memory T-cell generation, as well as enhances the helper function of Tfh for B cells, and also promotes the differentiation and maturation of DCs. OX40/TNFRSF4 Protein, Human (Biotinylated, HEK293, His-Avi) is a recombinant biotinylated human OX40 (L29-A216) with C-terminal Avi and His tag, which is produced in HEK293.
OX40 (TNFRSF4), is a receptor for OX40 Ligand. OX40 is preferentially expressed by T cells. OX40 can be activated by OX40 Ligand, thereby functioning as a T cell co-stimulatory molecule. The OX40-OX40 Ligand interaction promotes effector T-cell survival and effectively induces memory T-cell generation, as well as enhances the helper function of Tfh for B cells, and also promotes the differentiation and maturation of DCs. OX40/TNFRSF4 Protein, Human (Biotinylated, HEK293, Fc) is a biotinylated recombinant human OX40 (L29-A216) with C-terminal hFc tag, which is produced in HEK293.
OX40 (TNFRSF4), is a receptor for OX40 Ligand. OX40 is preferentially expressed by T cells. OX40 can be activated by OX40 Ligand, thereby functioning as a T cell co-stimulatory molecule. The OX40-OX40 Ligand interaction promotes effector T-cell survival and effectively induces memory T-cell generation, as well as enhances the helper function of Tfh for B cells, and also promotes the differentiation and maturation of DCs. OX40/TNFRSF4 Protein, Human (HEK293, His-Avi) is a recombinant human OX40 (L29-A216) with C-terminal Avi and His tag, which is produced in HEK293.
Glutamate carboxypeptidase II type non peptidase homologue; Inactive N acetylated alpha linked acidic dipeptidase like protein 2; Inactive N-acetylated-alpha-linked acidic dipeptidase-like protein 2; N acetylated alpha linked acidic dipeptidase like 2; NAALADase L2; NAALADL 2; NAALADL2
The NAALADL2 protein was identified as catalytically inactive, suggesting a role beyond enzymatic activity. The name implies that non-enzymatic functions contribute to different cellular processes. NAALADL2 Protein, Human (His-SUMO) is the recombinant human-derived NAALADL2 protein, expressed by E. coli , with N-His, N-SUMO labeled tag.
OX40 (TNFRSF4), is a receptor for OX40 Ligand. OX40 is preferentially expressed by T cells. OX40 can be activated by OX40 Ligand, thereby functioning as a T cell co-stimulatory molecule. The OX40-OX40 Ligand interaction promotes effector T-cell survival and effectively induces memory T-cell generation, as well as enhances the helper function of Tfh for B cells, and also promotes the differentiation and maturation of DCs. OX40/TNFRSF4 Protein, Mouse (Biotinylated, HEK293, His-Avi) is a recombinant biotinylated mouse OX40 (V20-P211) with C-terminal Avi and His tag, which is produced in HEK293.
H-HoArg-OH-d4 is a deuterium labeled H-HoArg-OH (HY-W008385). H-HoArg-OH, a homologue arginine, is a strong inhibitor of human bone and liver alkaline phosphatase.
3-Pyridylacetic acid-d4 (hydrochloride) is the deuterium labeled 3-Pyridylacetic acid hydrochloride[1]. 3-Pyridineacetic acid hydrochloride is a higher homologue of nicotinic acid, a breakdown product of nicotine (and other tobacco alkaloids)[2][3].
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