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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
102 Results for "
SI
" in MedChemExpress (MCE) Product Catalog:
Products (102)
102 Results for "SI" in MCE Product Catalog:
9
9 Publications Verification
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.
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9 Publications Verification
Synonyms: ML-SI3 (cis/trans mix)
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ML-SI3 is a mixture of cis/trans ML-SI3 (HY-139426A), which is a TRPML1/2 channel inhibitor with IC50s of 4.7 μM and 1.7 μM, respectively. ML-SI3 also inhibits lysosomal calcium efflux and blocks downstream TRPML1-mediated autophagy. The cis/trans ML-SI3 (HY-139426A) components of ML-SI3 are TRPML2 activators with EC50s of 3.3 μM and 9.4 μM, respectively .
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7 Cited Publications
Cat. No.: HY-134818
Purity: 99.80%
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ML-SI1, a racemic mixture of diastereomers, is a TRPML inhibitor with an IC50 value of 15 μM for TRPML1 .
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3 Cited Publications
Synonyms: (-)-trans-ML-SI3
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(1R,2R)-ML-SI3 is an isomer of ML-SI3 and a potent inhibitor of three isoforms of TRPML. (1R,2R)-ML-SI3 inhibits TRPMLs with IC50s of 1.6 μM (TRPML1), 2.3 μM (TRPML2), and 12.5 μM (TRPML3), respectively .
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2 Cited Publications
Synonyms: γ-AminopropyltriethoxySIlane; APTES
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2 Cited Publications
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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 .
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1 Cited Publications
Synonyms: trans-ML-SI3
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(rel)-ML-SI3 is one of the active ingredients of ML-SI3 (HY-139426) (another component is (cis)-ML-SI3) that targets three isoforms of TRPML. (rel)-ML-SI3 is an inhibitor of TRPML1 and TRPML3 (IC50=3.1 μM/28.5 μM), and a potent activator of TRPML2 (EC50=3.3 μM) .
Cat. No.: HY-P99676
CAS No.: 2559704-24-2
Synonyms: SI-B001; BL-B01D1 Antibody
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.
Synonyms: EPH 116 hydrochloride
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SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI). SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability .
Synonyms: (+)-trans-ML-SI3
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(1S,2S)-ML-SI3 is a trans-isomer of ML-SI3 that targets all three isoforms of TRPML. (1S,2S)-ML-SI3 is an activator of TRPML2 and TRPML3 (EC50=2.7 μM/10.8 μM) and a potent inhibitor of TRPML1 (IC50=5.9 μM) .
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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 .
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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) ) .
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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 .
Cat. No.: HY-174066
CAS No.: 2572552-60-2
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SI-W052 is an orally active, brain-penetrant and selective small-molecule inhibitor targeting mTOR and TEX264. SI-W052 activates autophagy by inhibiting mTOR phosphorylation and enhances TEX264 expression to promote ER turnover, suppressing LPS-induced release of inflammatory factors (TNF-α, IL-6). SI-W052 is promising for research of Alzheimer’s disease (AD)-associated neuroinflammation .
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 .
Cat. No.: HY-163469
CAS No.: 3074959-44-4
SRC-3-IN-2 (SI-12 6c)is an orally active steroid receptor coactivator 3 (SRC-3) inhibitor. SRC-3-IN-2 has antitumor activity .
Cat. No.: HY-178970
HDAC11-IN-4 is a potent and selective HDAC11 inhibitor with an IC50 of 13.49 nM and a Ki of 2.2 nM. HDAC11-IN-4 exhibits extremely high selectivity for HDAC11 over other defatty-acylases such as SIRT2, SIRT3, SIRT6, and HDAC8 (SI >10,000). HDAC11-IN-4 can be used for the research of cancer .
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(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.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
