214

Osimertinib

214 Publications Verification

Cat. No.: HY-15772

CAS No.: 1421373-65-0

Purity: 99.92%

Synonyms: AZD-9291; Mereletinib

Target:

EGFR

Research Areas:

Cancer

Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

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214

Osimertinib mesylate

214 Publications Verification

Cat. No.: HY-15772A

CAS No.: 1421373-66-1

Purity: 99.97%

Synonyms: AZD-9291 mesylate; Mereletinib mesylate

Target:

EGFR

Research Areas:

Cancer

Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .

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190

Decitabine

190 Cited Publications

Cat. No.: HY-A0004

CAS No.: 2353-33-5

Synonyms: 5-Aza-2'-deoxycytidine; 5-AZA-CdR; NSC 127716

Target:

DNA Methyltransferase Apoptosis Nucleoside Antimetabolite/Analog

Research Areas:

Infection Inflammation/Immunology Cancer

Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell Apoptosis. Decitabine has potent anticancer activity .

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145

5-Azacytidine

145 Cited Publications

Cat. No.: HY-10586

CAS No.: 320-67-2

Purity: 99.91%

Synonyms: Azacitidine; 5-AzaC; Ladakamycin

Target:

Organoid Nucleoside Antimetabolite/Analog DNA Methyltransferase Bacterial Autophagy Antibiotic

Research Areas:

Infection Cancer

5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes . 5-Azacytidine induces cell autophagy .

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132

C-176

132 Cited Publications

Cat. No.: HY-112906

CAS No.: 314054-00-7

Purity: 99.45%

Target:

STING

Research Areas:

Inflammation/Immunology

C-176 is a selective and blood-brain barrier permeable STING inhibitor. C-176 covalently targets transmembrane cysteine residue 91 and thereby blocking activation-induced palmitoylation of STING .

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130

Sotorasib

130 Cited Publications

Cat. No.: HY-114277

CAS No.: 2296729-00-3

Purity: 99.94%

Synonyms: AMG-510

Target:

Ras

Research Areas:

Cancer

Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .

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97

Avibactam sodium

97 Cited Publications

Cat. No.: HY-14879A

CAS No.: 1192491-61-4

Purity: 99.99%

Synonyms: NXL-104; AVE1330A

Target:

Beta-lactamase Bacterial Antibiotic

Research Areas:

Infection

Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC₅₀s of 8 nM and 5 nM, respectively .

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97

Avibactam sodium hydrate

97 Cited Publications

Cat. No.: HY-14879B

CAS No.: 2938989-90-1

Purity: 98.66%

Synonyms: NXL-104 hydrate; AVE1330A hydrate

Target:

Beta-lactamase Bacterial Antibiotic

Research Areas:

Infection

Avibactam sodium (NXL-104) hydrate is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC₅₀s of 8 nM and 5 nM, respectively .

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97

Avibactam

97 Cited Publications

Cat. No.: HY-14879

CAS No.: 1192500-31-4

Purity: 99.22%

Synonyms: NXL-104 free acid; AVE1330A free acid

Target:

Beta-lactamase Bacterial Antibiotic

Research Areas:

Infection

Avibactam (NXL-104) free acid is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC₅₀s of 8 nM and 5 nM, respectively .

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95

THZ1

95 Cited Publications

Cat. No.: HY-80013

CAS No.: 1604810-83-4

Target:

CDK

Research Areas:

Cancer

THZ1 is a selective and potent covalent CDK7 inhibitor with an IC₅₀ of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression .

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95

THZ1 Hydrochloride

95 Cited Publications

Cat. No.: HY-80013A

Target:

CDK

Research Areas:

Cancer

THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC₅₀ of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression .

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67

Adagrasib

67 Cited Publications

Cat. No.: HY-130149

CAS No.: 2326521-71-3

Purity: 99.81%

Synonyms: MRTX849

Target:

Ras

Research Areas:

Cancer

Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .

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57

Ulixertinib hydrochloride

57 Cited Publications

Cat. No.: HY-15816A

CAS No.: 1956366-10-1

Purity: 99.89%

Synonyms: BVD-523 hydrochloride; VRT752271 hydrochloride

Target:

ERK

Research Areas:

Cancer

Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC₅₀ of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .

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57

Ulixertinib

57 Cited Publications

Cat. No.: HY-15816

CAS No.: 869886-67-9

Purity: 99.95%

Synonyms: BVD-523; VRT752271

Target:

ERK

Research Areas:

Cancer

Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC₅₀ of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .

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43

THZ531

43 Cited Publications

Cat. No.: HY-103618

CAS No.: 1702809-17-3

Purity: 99.57%

Target:

CDK

Research Areas:

Cancer

THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC₅₀s of 158 nM and 69 nM, respectively .

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37

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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36

(-)-DHMEQ

36 Cited Publications

Cat. No.: HY-14645

CAS No.: 287194-40-5

Purity: 99.37%

Synonyms: Dehydroxymethylepoxyquinomicin

Target:

NF-κB

Research Areas:

Inflammation/Immunology Cancer

(-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversible NF-κB inhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation of NF-κB and shows anti-inflammatory and anticancer activity .

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