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144 Results for "

Switch 2 closure

" in MedChemExpress (MCE) Product Catalog:

Products (144)

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MRTX1133

65 Publications Verification

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 ^[2].

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Rimiducid

61 Cited Publications

Cat. No.: HY-16046

CAS No.: 195514-63-7

Synonyms: AP1903

Target:

FKBP Apoptosis

Research Areas:

Cancer

Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains. Rimiducid (AP1903) dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.

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ATP-Red 1

13 Cited Publications

Cat. No.: HY-U00451

CAS No.: 1847485-97-5

ATP-Red 1 is a multisite-binding switchable fluorescent probe, and can selectively and rapidly responds to intracellular concentrations of ATP in living cells (Ex/Em = 510/590 nm).

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p-Aminophenylmercuric acetate

12 Cited Publications

Cat. No.: HY-148905

CAS No.: 6283-24-5

Purity: 99.07%

p-Aminophenylmercuric acetate is an organomercurial activator of matrix metalloproteinases (MMP). P-Aminophenylmercuric acetate participates in the activation and inhibition of MMP-8 by attacking protein sulfhydryl or inducing cysteine switching reaction. p-Aminophenylmercuric acetate promotes the shedding of betacellulin precursor (pro-BTC). p-Aminophenylmercuric acetate influences the binding of agonists and antagonists to the opiate receptor ^[2] .

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Seclidemstat

11 Cited Publications

Cat. No.: HY-103713

CAS No.: 1423715-37-0

Purity: 99.77%

Synonyms: SP-2577

Target:

Histone Demethylase

Research Areas:

Cancer

Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (K_i=31 nM, IC₅₀=13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma ^[2].

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Seclidemstat mesylate

11 Cited Publications

Cat. No.: HY-103713A

CAS No.: 2044953-70-8

Purity: 99.80%

Synonyms: SP-2577 mesylate

Target:

Histone Demethylase

Research Areas:

Cancer

Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (K_i=31 nM, IC₅₀=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma ^[2].

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Ripretinib

9 Cited Publications

Cat. No.: HY-112306

CAS No.: 1442472-39-0

Purity: 98.21%

Synonyms: DCC-2618

Target:

c-Kit PDGFR FLT3 VEGFR Apoptosis

Research Areas:

Cancer

Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) ^[2]. DCC-2618 exerts antineoplastic effect and induces apoptosis .

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