657

Adezmapimod hydrochloride

657 Publications Verification

Cat. No.: HY-10256A

CAS No.: 869185-85-3

Purity: 99.37%

Synonyms: SB 203580 hydrochloride; RWJ 64809 hydrochloride

Target:

Organoid p38 MAPK Autophagy Mitophagy

Research Areas:

Inflammation/Immunology Cancer

Adezmapimod (SB 203580; RWJ 64809) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC₅₀s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC₅₀s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride does not disrupt JNK activity and is an autophagy and mitophagy activator .

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657

Adezmapimod

657 Publications Verification

Cat. No.: HY-10256

CAS No.: 152121-47-6

Purity: 99.92%

Synonyms: SB 203580; RWJ 64809

Target:

Organoid p38 MAPK Autophagy Mitophagy HSP

Research Areas:

Inflammation/Immunology Cancer

Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC₅₀s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC₅₀s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod can inhibit p38 MAPK and lead to the inhibition of downstream HSP27 phosphorylation. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator ^[3].

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513

MK-2206

513 Cited Publications

Cat. No.: HY-108232

CAS No.: 1032349-77-1

Purity: 99.72%

Target:

Bcl-2 Family Apoptosis mTOR Akt GSK-3

Research Areas:

Metabolic Disease Inflammation/Immunology Cancer

MK-2206 is an orally active pan-AKT inhibitor, with IC₅₀ values of 8 nM, 12 nM and 65 nM against AKT1, AKT2 and AKT3, respectively. MK-2206 inhibits the Akt/mTOR signaling pathway and reduces the levels of downstream GSK3β and Mcl-1 via proteasomal degradation. MK-2206 induces G1-phase cell cycle arrest, apoptosis, epithelial-mesenchymal transition, fibroblast activation and extracellular matrix deposition. MK-2206 causes transient hyperglycemia and hyperinsulinemia in animals. MK-2206 can be used in research related to solid tumors, renal fibrosis and hypercholesterolemia ^[3] .

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513

MK-2206 dihydrochloride

513 Cited Publications

Cat. No.: HY-10358

CAS No.: 1032350-13-2

Purity: 99.94%

Synonyms: MK-2206 (2HCl)

Target:

Bcl-2 Family Apoptosis mTOR Akt GSK-3

Research Areas:

Cardiovascular Disease Inflammation/Immunology Cancer

MK-2206 dihydrochloride (MK-2206 2HCl) is an orally active pan-AKT inhibitor, with IC₅₀ values of 8 nM, 12 nM and 65 nM against AKT1, AKT2 and AKT3, respectively. MK-2206 dihydrochloride inhibits the Akt/mTOR signaling pathway and reduces the levels of downstream GSK3β and Mcl-1 via proteasomal degradation. MK-2206 dihydrochloride induces G1-phase cell cycle arrest, apoptosis, epithelial-mesenchymal transition, fibroblast activation and extracellular matrix deposition. MK-2206 dihydrochloride causes transient hyperglycemia and hyperinsulinemia in animals. MK-2206 dihydrochloride can be used in research related to solid tumors, renal fibrosis and hypercholesterolemia ^[3] .

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154

Erlotinib Hydrochloride

154 Cited Publications

Cat. No.: HY-12008

CAS No.: 183319-69-9

Purity: 99.94%

Synonyms: CP-358774 hydrochloride; NSC 718781 hydrochloride; OSI-774 hydrochloride

Target:

EGFR OAT ERK GSK-3 β-catenin

Research Areas:

Endocrinology Cancer

Erlotinib (CP-358774) Hydrochloride is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib Hydrochloride also acts as a substrate and inhibitor of OATP2B1, with an IC₅₀ of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib Hydrochloride blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib Hydrochloride inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib Hydrochloride is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib Hydrochloride can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis ^[3] .

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154

Erlotinib

154 Cited Publications

Cat. No.: HY-50896

CAS No.: 183321-74-6

Synonyms: CP-358774; NSC 718781; OSI-774

Target:

EGFR OAT ERK GSK-3 β-catenin

Research Areas:

Endocrinology Cancer

Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC₅₀ of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions ^[3] .

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138

Alpelisib

138 Cited Publications

Cat. No.: HY-15244

CAS No.: 1217486-61-7

Purity: 99.88%

Synonyms: BYL-719

Target:

PI3K Apoptosis

Research Areas:

Infection Neurological Disease Metabolic Disease Cancer

Alpelisib (BYL-719) is an orally active PI3Kα-selective inhibitor that blocks the conversion of PIP2 to PIP3, thereby inhibiting pathways including PI3K/AKT/mTOR, MAPK/ERK, Notch and JAK-STAT. Alpelisib also induces apoptosis, G0/G1 phase arrest and senescence; it significantly inhibits the proliferation, self-renewal, stemness and epithelial-mesenchymal transition (EMT) of tumor cells, reduces cancer stem cell populations and decreases the expression of stem cell markers. Alpelisib not only enhances the sensitivity to Eribulin (HY-13442) and exerts a synergistic effect with Paclitaxel (HY-B0015), but may also induce drug resistance by upregulating the SGK3/GSK3β/β-catenin signaling pathway. Alpelisib can be applied to research related to breast cancer, gastric cancer and lipomas associated with PTEN hamartoma tumor syndrome ^[3] .

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138

Alpelisib hydrochloride

138 Cited Publications

Cat. No.: HY-15244A

CAS No.: 1584128-91-5

Synonyms: BYL-719 hydrochloride

Target:

PI3K Apoptosis

Research Areas:

Infection Neurological Disease Metabolic Disease Cancer

Alpelisib (BYL-719) hydrochloride is an orally active PI3Kα-selective inhibitor that blocks the conversion of PIP2 to PIP3, thereby inhibiting pathways including PI3K/AKT/mTOR, MAPK/ERK, Notch and JAK-STAT. Alpelisib hydrochloride also induces apoptosis, G0/G1 phase arrest and senescence; it significantly inhibits the proliferation, self-renewal, stemness and epithelial-mesenchymal transition (EMT) of tumor cells, reduces cancer stem cell populations and decreases the expression of stem cell markers. Alpelisib hydrochloride not only enhances the sensitivity to Eribulin (HY-13442) and exerts a synergistic effect with Paclitaxel (HY-B0015), but may also induce drug resistance by upregulating the SGK3/GSK3β/β-catenin signaling pathway. Alpelisib hydrochloride can be applied to research related to breast cancer, gastric cancer and lipomas associated with PTEN hamartoma tumor syndrome ^[3] .

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50

SB 216763

50 Cited Publications

Cat. No.: HY-12012

CAS No.: 280744-09-4

Purity: 99.37%

Target:

GSK-3 Autophagy

Research Areas:

Neurological Disease Cancer

SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC₅₀s of 34.3 nM for both GSK-3α and GSK-3β.

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42

BX795

42 Cited Publications

Cat. No.: HY-10514

CAS No.: 702675-74-9

Purity: 99.84%

Target:

PDK-1 IKK Autophagy

Research Areas:

Cancer

BX795 is a potent and selective inhibitor of PDK1, with an IC₅₀ of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC₅₀ of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy ^[3] .

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36

TWS119

36 Cited Publications

Cat. No.: HY-10590

CAS No.: 601514-19-6

Purity: 99.20%

Target:

Wnt GSK-3 Autophagy

Research Areas:

Neurological Disease Cancer

TWS119 is an inhibitor of GSK-3β, with an IC₅₀ of 30 nM, and activates the wnt/β-catenin pathway.

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23

LY2090314

23 Cited Publications

Cat. No.: HY-16294

CAS No.: 603288-22-8

Target:

GSK-3

Research Areas:

Cancer

LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC₅₀ values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.

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23

Ceftriaxone

23 Cited Publications

Cat. No.: HY-B0712

CAS No.: 73384-59-5

Synonyms: Ro 13-9904 free acid

Target:

Bacterial Antibiotic GSK-3 Aurora Kinase

Research Areas:

Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer

Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC₅₀ value of 0.78 μM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis ^[3] .

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23

Ceftriaxone sodium hydrate

23 Cited Publications

Cat. No.: HY-B0712A

CAS No.: 104376-79-6

Synonyms: Ro 13-9904 sodium hydrate

Target:

Bacterial Antibiotic GSK-3 Aurora Kinase

Research Areas:

Infection Cancer

Ceftriaxone sodium hydrate (Ro 13-9904 sodium hydrate) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium hydrate is a covalent inhibitor of GSK3β with IC₅₀ value of 0.78 μM. Ceftriaxone sodium hydrate is an inhibitor of Aurora B. Ceftriaxone sodium hydrate has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium hydrate can be used in the study of bacterial infections and meningitis ^[3] .

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23

Ceftriaxone sodium salt

23 Cited Publications

Cat. No.: HY-B0712B

CAS No.: 74578-69-1

Synonyms: Ro 13-9904

Target:

Antibiotic GSK-3 Bacterial Aurora Kinase

Research Areas:

Infection Inflammation/Immunology Cancer

Ceftriaxone sodium salt (Ro 13-9904) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium salt is a covalent inhibitor of GSK3β with IC₅₀ value of 0.78 μM. Ceftriaxone sodium salt is an inhibitor of Aurora B. Ceftriaxone sodium salt has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium salt can be used in the study of bacterial infections and meningitis ^[3] .

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