555 Results for "

Pi-binding pocket

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149

SB 202190 hydrochloride

149 Publications Verification

Cat. No.: HY-10295A

CAS No.: 350228-36-3

Purity: 99.66%

Target:

Organoid p38 MAPK Autophagy Apoptosis

Research Areas:

Neurological Disease Cancer

SB 202190 hydrochloride is a selective p38 MAP kinase inhibitor with IC₅₀s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 hydrochloride binds to the ATP pocket of the active recombinant human p38 kinase with a K_d of 38 nM. SB 202190 hydrochloride has anti-cancer activity . SB202190 hydrochloride induces autophagy .

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149

SB 202190

149 Publications Verification

Cat. No.: HY-10295

CAS No.: 152121-30-7

Purity: 99.89%

Target:

Organoid p38 MAPK Autophagy Apoptosis

Research Areas:

Neurological Disease Cancer

SB 202190 is a selective p38 MAP kinase inhibitor with IC₅₀s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a K_d of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits . SB202190 induces autophagy .

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MRTX1133

65 Cited Publications

Cat. No.: HY-134813

CAS No.: 2621928-55-8

Purity: 99.97%

Target:

Ras

Research Areas:

Cancer

MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated K_D against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .

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Acalabrutinib

37 Cited Publications

Cat. No.: HY-17600

CAS No.: 1420477-60-6

Synonyms: Calquence; ACP-196

Target:

Btk

Research Areas:

Infection Inflammation/Immunology Cancer

Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL). Acalabrutinib can be used for CLL research . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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K-975

35 Cited Publications

Cat. No.: HY-138565

CAS No.: 2563855-03-6

Purity: 99.89%

Target:

YAP

Research Areas:

Cancer

K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma .

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Takinib

33 Cited Publications

Cat. No.: HY-103490

CAS No.: 1111556-37-6

Purity: 99.41%

Synonyms: EDHS-206

Target:

MAP3K Apoptosis

Research Areas:

Infection Inflammation/Immunology Cancer

Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC₅₀=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (K_D(app) of 0.46 μM) .

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BMS-309403

31 Cited Publications

Cat. No.: HY-101903

CAS No.: 300657-03-8

Purity: 99.93%

Target:

FABP

Research Areas:

Cardiovascular Disease Metabolic Disease

BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with K_is of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .

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BMS-309403 sodium

31 Cited Publications

Cat. No.: HY-101903A

CAS No.: 2802523-05-1

Purity: 99.93%

Target:

FABP

Research Areas:

Cardiovascular Disease Metabolic Disease

BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with K_is of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .

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KI696

23 Cited Publications

Cat. No.: HY-101140

CAS No.: 1799974-70-1

Purity: 98.67%

Target:

Keap1-Nrf2 Quinone Reductase

Research Areas:

Inflammation/Immunology

KI696 is a selective KEAP1/NRF2 protein-protein interaction inhibitor with a human K_d value of 1.3 nM. KI696 acts by competitively occupying the NRF2-binding pocket of the KEAP1 Kelch domain. KI696 blocks KEAP1-mediated ubiquitination and degradation of NRF2, promotes the translocation of NRF2 to the nucleus, activates the expression of downstream antioxidant genes, increases intracellular glutathione levels, and alleviates oxidative stress-induced cell damage and inflammatory cell infiltration in the lungs. KI696 reduces ozone-induced pulmonary oxidative damage and inflammatory cell accumulation in rats, and upregulates pulmonary antioxidant genes. KI696 can be used in research related to chronic obstructive pulmonary disease, oxidative stress and inflammation .

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EED226

17 Cited Publications

Cat. No.: HY-101117

CAS No.: 2083627-02-3

Purity: 99.56%

Target:

Histone Methyltransferase

Research Areas:

Cancer

EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor . EED226 inhibits PRC2 with an IC₅₀ of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .

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SN-011

16 Cited Publications

Cat. No.: HY-145010

CAS No.: 2249435-90-1

Purity: 99.73%

Target:

STING

Research Areas:

Inflammation/Immunology

SN-011 is a potent and selective mouse and human STING inhibitor, with an IC₅₀ of 76 nM for STING signaling. SN-011 competes with cyclic dinucleotide (CDN) for the binding pocket of the STING dimer, blocking CDN binding and STING activation. SN-011 can be used for the research of STING-driven autoimmune and inflammatory disease .

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Acacetin

16 Cited Publications

Cat. No.: HY-N0451

CAS No.: 480-44-4

Synonyms: 5,7-Dihydroxy-4'-methoxyflavone

Category:

Neurological Disease Anti-aging Flavones 500 - Internal Server Error | MedChemExpress

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