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SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36 .
SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI), with IC50 values of 3-20 nM for breast cancer cell death. SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability .
Izalontamab (SI-B001) is a bispecific anti-EGFR/HER3 monoclonal antibody with high selectivity for EGFR/HER3 heterodimer. Izalontamab can be used for the research of cancer .
SI Human Pre-designed siRNA Set A contains three designed siRNAs for SI gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
(rel)-ML-SI3 is the isomer of ML-SI3 (HY-139426). ML-SI3 is a TRPML Channel Inhibitor. ML-SI3 blocks TRPML1 and TRPML2 with IC50s of 4.7 μM and 1.7 μM, respectively. ML-SI3 prevents lysosomal calcium efflux and blocks downstream TRPML1-mediated induction of autophagy .
ML-SI3 is a mixture of cis/trans ML-SI3. ML-SI3 is a TRPML channel modulator. ML-SI3 blocks TRPML1 and TRPML2 with IC50s of 4.7 µM and 1.7 µM, respectively. ML-SI3 is also able to activate TRPML2 and TRPML3 with EC50s of 3.3-9.4 μM and 29 μM, respectively. ML-SI3 also inhibits lysosomal calcium efflux and blocks downstream TRPML1-mediated autophagy.
G12Si-1 is a selective K-Ras(G12S) covalent inhibitor, which can inhibit oncogenic signaling of K-Ras(G12S). G12Si-1 shows good ability to covalently engage recombinant K-Ras(G12S) at the mutant serine residue. G12Si-1 can also affect nucleotide cycling of K-Ras by blocking Sos-catalyzed exchange and decreasing the rate of EDTA promoted exchange .
14,15-EET-SI is a sulfonimide (SI) analog metabolized from 14,15-EET, which is also an effective mitogen. 14,15-EET-SI can stimulate the incorporation of [3H] thymidine, activate pp60c-src and initiate the tyrosine kinase cascade, mediating their mitotic effects. Additionally, 14,15-EET-SI can increase cell proliferation as well as the expression of c-fos and egr-1 mRNA .
(E)-SI-2 is an isomer of SI-2, an inhibitor of the steroid receptor coactivator SRC-3. SI-2 has anticancer activity and increases the number of cytotoxic immune cells in mice with breast cancer .
(1S,2S)-ML-SI3 is the trans-isomer of ML-SI3, a TRPML inhibitor. The (-)-isomer is a potent inhibitor of TRPML1 and TRPML2 (IC50=1.6 μM/2.3 μM) and a weak inhibitor of TRPML3 (IC50=12.5 μM), whereas the (+)-enantiomer is an inhibitor on TRPML1 (IC50=5.9 μM), but an activator on TRPML 2 and 3 (EC50=2.7 μM/10.8 μM) .
Sacrosidase is a yeast-derived enzyme that facilitates sucrose digestion. Sacrosidase has the potential for congenital sucrase-isomaltase (SI) deficiency research .
Gemcitabine-O-Si(di-iso)-O-Mc is a agent-linker conjugate for ADC with potent antitumor activity by using Gemcitabine (a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent; HY-17026), linked via the ADC linker .
EBOV/MARV-IN-1 is a potent inhibitor of Ebola virus (EBOV) and Marburg virus (MARV), with broad-spectrum activity (EC50=0.31, and 0.82 µM, respectively) and low cytotoxicity (SI>100) in HeLa cells .
MMV665916, a quinazolinedione derivative, is an antimalarial agent. MMV665916 displays antiplasmodial activity against P. falciparum FcB1 strain with EC50 value of 0.4 µM and presents the high selectivity index (SI>250) .
HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile .
Antitubercular agent-29 (compound 6xa) is a potent agent resistant (DR) Mycobacterium tuberculosis (Mtb) inhibitor with MIC of 0.03 μg/mL against agent-susceptible (DS)-Mtb strains, MIC of 0.03-0.06 μg/mL against DR-Mtb strains, and favourable selectivity (SI>40) against Vero cells .
PDE4-IN-12 is a potent pan-PDE4 inhibitor, with IC50s of 3.5 and 15 nM for PDE4 and PDE7, respectively (SI=2.71 and 4.27, respectively). PDE4-IN-12 shows well tolerated, can be used in study of inflammatory bowel diseases (IBDs) .
DENV-IN-4 is a potent DENV inhibitor (DENV EC50=4.79 μM, Vero CC50>100 μM, SI>20.9). DENV-IN-4 can inhibit the expression level of DENV2 with concentration-dependence and reduce RNA-dependent RNA polymerase (RdRp) enzymatic activity. DENV-IN-4 has antiviral effect .
Anti-infective agent 6 (compound 28) is a potent anti-infectious agent. Anti-infective agent 6 shows a good activity against P. falciparum F32-ART (IC50=1.4 μM) with a good selectivity index (SI>36). Anti-infective agent 6 also shows a potency against L. donovani (IC50=3.5 μM) .
N-(5-Hydroxypentyl)maleimide is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs), such as Gemcitabine-O-Si(di-iso)-O-Mc (HY-130812) ) .
Antiviral agent 9 reaches a single-digit picomolar EC50 value (0.006 nM) against HIV-1 and nearly 300-fold higher selectivity index (SI) compared to tenofovir alafenamide fumarate (TAF).
8α,9α-Epoxycoleon-U-quinone (compound 3) is a p-glycoprotein (P-gp) regulator that is selective for cancer cells (SI=2.0). 8α,9α-Epoxycoleon-U-quinone effectively inhibits P-gp activity in NCI-H460/R cells. 8α,9α-Epoxycoleon-U-quinone also reverses the resistance of cancer cells to Doxorubicin (DOX) (HY-15142A) and enhances the anticancer effect of DOX .
D-Glucose- 13C,d-1 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
(2-Chlorophenyl)diphenylmethanol (UCL 1880) is an analog of the metabolite 2-chlorophen-diphenyl-methanol (CBM) of 2-chlorophenyl, The IC50 for sI(AHP) inhibition is 1-2 μM. (2-chlorophenyl)diphenylmethanol is a weak Ca 2+ channel blocker .
D-Glucose- 13C2,d2 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
CP19, a histamine receptor antagonist, is an entry inhibitor against both Ebolavirus (EBOV) and Marburgvirus (MARV) with IC50s of 3.4 μM and 29.5 μM, respectively. CP19 has SI values of 29.4 and 3.4 for EBOV and MARV, respectively. CP19 has antiviral activity .
SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase . SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities .
3-Aminopropyltriethoxysilane (APTES) acts as a strong glue to immobilize biomolecules such as antibodies and enzymes to silicon and silicon derivatives such as silicon nitride (Si3N4 )) on. 3-Aminopropyltriethoxysilane also acts as a spacer, providing biomolecules with more spatial freedom during immobilization for higher specific activity. 3-Aminopropyltriethoxysilane can form a more stable, sensitive, and highly biocompatible bioanalytical platform by immobilizing biomolecules onto some solid materials, electrode materials, nanomaterials, and nanocomposites .
AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells .
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
PI3K-IN-28 (Compound 6c) is a potent inhibitor of PI3K. PI3K-IN-28 displays the most potent activity with lower toxic effects on MCF-10a. PI3K-IN-28 displays half-maximal inhibitory concentration (IC50, μM) values of 5.8, 2.3, and 7.9. PI3K-IN-28 is the most potent one with a selectivity index (SI) of 39 and is considered as a latent lead for further optimization of anticancer agents .
3-Aminopropyltriethoxysilane (APTES) acts as a strong glue to immobilize biomolecules such as antibodies and enzymes to silicon and silicon derivatives such as silicon nitride (Si3N4 )) on. 3-Aminopropyltriethoxysilane also acts as a spacer, providing biomolecules with more spatial freedom during immobilization for higher specific activity. 3-Aminopropyltriethoxysilane can form a more stable, sensitive, and highly biocompatible bioanalytical platform by immobilizing biomolecules onto some solid materials, electrode materials, nanomaterials, and nanocomposites .
Izalontamab (SI-B001) is a bispecific anti-EGFR/HER3 monoclonal antibody with high selectivity for EGFR/HER3 heterodimer. Izalontamab can be used for the research of cancer .
8α,9α-Epoxycoleon-U-quinone (compound 3) is a p-glycoprotein (P-gp) regulator that is selective for cancer cells (SI=2.0). 8α,9α-Epoxycoleon-U-quinone effectively inhibits P-gp activity in NCI-H460/R cells. 8α,9α-Epoxycoleon-U-quinone also reverses the resistance of cancer cells to Doxorubicin (DOX) (HY-15142A) and enhances the anticancer effect of DOX .
AKR1B10; Aldo-keto reductase family 1 member B10; ARL-1; Aldose reductase-like; Aldose reductase-related protein; ARP; hARP; Small intestine reductase; SI reductase
The Aldose-reductase protein reduces carbonyl-containing compounds to alcohols, including retinals. It detoxifies unsaturated carbonyls like crotonaldehyde and 4-hydroxynonenal, but lacks reductase activity towards glucose. Aldose-reductase Protein, Human is the recombinant human-derived Aldose-reductase protein, expressed by E. coli , with tag free. The total length of Aldose-reductase Protein, Human is 316 a.a., .
Citrate Synthase (CS) is a key enzyme in carbohydrate metabolism, specifically in the tricarboxylic acid (TCA) cycle, where it catalyzes the conversion of oxaloacetate and acetyl-CoA to form citrate. This enzymatic process represents the first and crucial step in the TCA cycle, which is fundamental to cellular energy production. By initiating the cycle and facilitating the condensation of acetyl-CoA with oxaloacetate, CS plays a central role in channeling metabolic intermediates towards the production of energy-rich molecules. This step not only generates citrate but also sets the stage for subsequent reactions in the TCA cycle, ultimately contributing to the efficient extraction of energy from carbohydrates and other metabolic substrates. The activity of CS is pivotal in maintaining cellular energy homeostasis and ensuring the proper functioning of aerobic metabolism. Citrate Synthase/CS Protein, Human (sf9, His) is the recombinant human-derived Citrate Synthase/CS protein, expressed by Sf9 insect cells , with C-His labeled tag. The total length of Citrate Synthase/CS Protein, Human (sf9, His) is 439 a.a., with molecular weight of ~46 kDa.
AKR1B10; Aldo-keto reductase family 1 member B10; ARL-1; Aldose reductase-like; Aldose reductase-related protein; ARP; hARP; Small intestine reductase; SI reductase
The Aldose-reductase protein reduces carbonyl-containing compounds to alcohols, including retinals. It detoxifies unsaturated carbonyls like crotonaldehyde and 4-hydroxynonenal, but lacks reductase activity towards glucose. Aldose-reductase Protein, Human (His) is the recombinant human-derived Aldose-reductase protein, expressed by E. coli , with N-6*His labeled tag. The total length of Aldose-reductase Protein, Human (His) is 316 a.a., .
CHID1 Protein, a saccharide- and LPS-binder, implies roles in pathogen sensing and endotoxin neutralization. Its ligand specificity, linked to oligosaccharide length, shows a preference for chitotetraose. CHID1's interaction with STAB1 suggests potential involvement in cellular processes related to STAB1 interactions. CHID1 Protein, Human (His) is the recombinant human-derived CHID1 protein, expressed by E. coli , with N-His labeled tag. The total length of CHID1 Protein, Human (His) is 374 a.a., with molecular weight of ~46.8 kDa.
The sucrase isomaltase (SI) protein plays a vital role in the final stages of carbohydrate digestion, effectively breaking down complex oligosaccharides into simple sugars. The isomaltase activity of SI is specific for α-1,4- and α-1,6-oligosaccharides, emphasizing its critical role in hydrolyzing specific carbohydrate bonds. Sucrase isomaltase/SI Protein, Human (Cell-Free, His) is the recombinant human-derived Sucrase isomaltase/SI protein, expressed by E. coli Cell-free , with C-6*His labeled tag. The total length of Sucrase isomaltase/SI Protein, Human (Cell-Free, His) is 1006 a.a., with molecular weight of 115.2 kDa.
D-Glucose- 13C,d-1 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
D-Glucose- 13C2,d2 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical si
