switchable

By Targets:	Akt (1) Apoptosis (3) Bacterial (1) c-Kit (1) Cathepsin (1) Endogenous Metabolite (1) FKBP (1) FLT3 (1) Fluorescent Dye (2) Fungal (1) Histone Demethylase (2) iGluR (1) mTOR (1) NF-κB (1) p38 MAPK (1) PDGFR (1) PI3K (1) Ras (8) VEGFR (1)
By Research Areas:	Cancer (16) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (6) Neurological Disease (2)
Click Chemistry:	Alkynes (2)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-151523

KRas G12R inhibitor 1	Ras	Cancer
KRas G12R inhibitor 1 (compound 3) is a KRas G12R selective covalent inhibitor that exploits the strong nucleophilicity of mutant cysteines and binds irreversibly in the Switch II region of K-Ras. KRas G12R inhibitor 1 can be used in cancer research .

HY-112306

Ripretinib DCC-2618	c-Kit PDGFR FLT3 VEGFR Apoptosis	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) . DCC-2618 exerts antineoplastic effect and induces apoptosis .

HY-W030319

Methyl 2-(7-hydroxy-2-oxo-2H-chromen-4-yl)acetate	Fluorescent Dye	Others
Methyl 2-(7-hydroxy-2-oxo-2H-chromen-4-yl)acetate, a natural coumarins derivative, is exploited for the synthesis of the switchable fluorescent substrates to be used in bacterial enzyme detection .

HY-146116

Antifungal agent 32	Fungal	Infection
Antifungal agent 32 (compound 1a) is a potent antifungal agent. Antifungal agent 32 inhibits Candida albicans filamentation and biofilm formation. Antifungal agent 32 inhibits the morphological switching of Candida albicans and its adherence to epithelial cells. Antifungal agent 32 can be used for Candida albicans infections research .

HY-157261

UNC2383

Others Others

UNC2383 is an oligonucleotide enhancing compound that can enhance effects of antisense oligonucleotides (ASOs), and splice switching oligonucleotides (SSOs) .

UNC2383	Others	Others
UNC2383 is an oligonucleotide enhancing compound that can enhance effects of antisense oligonucleotides (ASOs), and splice switching oligonucleotides (SSOs) .

HY-U00451

ATP-Red 1 1 Publications Verification	Fluorescent Dye	Others
ATP-Red 1 is a multisite-binding switchable fluorescent probe, and can selectively and rapidly responds to intracellular concentrations of ATP in living cells.

HY-160209

KIO-301	Others	Cardiovascular Disease
KIO-301 is a photoswitchable HCN channel blocker, and can be used as the vitreous “light switch” molecule that reactivates retinitis pigmentosa .

HY-19487

Ribocil	Bacterial	Infection
Ribocil is a highly selective chemical regulator that regulates the bacterial riboflavin nuclear switch. Ribocil strongly inhibits GFP expression with an EC50 value of 0.3 μM.

HY-16046

Rimiducid Maximum Cited Publications 33 Publications Verification AP1903	FKBP Apoptosis	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.

HY-126247

BI-2852	Ras	Cancer
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.

HY-161066

KRAS G13D-IN-1	Ras	Cancer
KRAS G13D-IN-1 (compound 41) is a selective and covalently reversible inhibitor of KRAS ^G13D (IC₅₀: 0.41 nM). The selectivity for KRAS ^G13D is 29-fold against KRAS wild type. KRAS G13D-IN-1 is an inhibitor of the GDP state and targets the SWII binding pocket of KRAS ^G13D. KRAS G13D-IN-1 inhibits KRAS binding to GDP and turns on/off downstream signaling cascades .

HY-126247B

(R)-BI-2852	Others	Cancer
(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.

HY-120897

NS-3-008 hydrochloride	Others	Inflammation/Immunology
NS-3-008 hydrochloride is an orally active transcriptional inhibitor of *G0/G1 switch* 2 (G0s2) with an IC₅₀** of 2.25 μM. NS-3-008 hydrochloride can be used for chronic kidney disease .

HY-145928

Divarasib 1 Publications Verification GDC-6036	Ras	Cancer
Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC₅₀ of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.

HY-P99313

Quilizumab Anti-Human NGcGM3 Recombinant Antibody	Apoptosis	Inflammation/Immunology
Quilizumab (Anti-Human NGcGM3 Recombinant Antibody) is a humanized IgG1κ monoclonal antibody. Quilizumab targets the M1-prime segment of membrane-expressed IgE, leading to depletion of IgE-switched and memory B cells. Quilizumab has the potantial for the asthma research .

HY-145928B

Divarasib adipate GDC-6036 adipate	Ras	Cancer
Divarasib (GDC-6036) adipate is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC₅₀ of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state .

HY-W010970

5'-Guanylic acid disodium salt 1 Publications Verification 5'-GMP disodium salt; 5'-guanosine monophosphate disodium salt	Endogenous Metabolite	Others
5'-Guanylic acid disodium salt (5'-GMP disodium salt) is composed of guanine, ribose, and phosphate moieties and it is a nucleotide monomer in messenger RNA. Guanosine derivatives are involved in intracellular signal transduction and have been identified in repetitive genomic sequences in telomeres, in ribosomal DNA, immunoglobulin heavy‐chain switch regions, and in the control regions of proto-oncogenes .

HY-148905

p-Aminophenylmercuric acetate	Cathepsin	Infection
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 .

HY-N0284

Esculetin 3 Publications Verification	PI3K Akt	Inflammation/Immunology Cancer
Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities .

HY-100825

OABK hydrochloride
OABK hydrochloride is a small-molecule switch that can be used to control protein activity. OABK (hydrochloride) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

HY-P3031

Mitogen-activated protein kinase 1 MAPK1	p38 MAPK NF-κB	Inflammation/Immunology
Mitogen-activated protein kinase 1 (MAPK1) can activate the downstream p38/NF-κB pathway. Mitogen-activated protein kinase 1 can regulate cellular processes in various sepsis-associated diseases. MAPK-catalyzed phosphorylation of substrate proteins functions as a switch to turn on or off the activity of the substrate protein .

HY-107712

TCN 213	iGluR	Neurological Disease
TCN 213 is a selective, surmountable, glycine-dependentlly GluN1/GluN2A NMDAR antagonist with IC₅₀s of 0.55, 3.5, 40 μM in the presence of 75, 750, 7500 nM glycine, respectively. TCN 213 can be used to monitor, pharmacologically, the switch in NMDAR expression in developing cortical neurones .

HY-162112

KRB-456	Ras	Cancer
KRB-456 is a small molecule that binds a dynamic allosteric binding pocket within the switch-I/II region of KRAS G12D. KRB-456 inhibits P-MEK, P-AKT, and P-S6 levels in vivo and inhibits the growth of cancer. KRB-456 can be used for the research of pancreatic cancer .

HY-103713

Seclidemstat 4 Publications Verification SP-2577	Histone Demethylase	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 .

HY-128522

ARS-1323-alkyne	Ras	Cancer
ARS-1323-alkyne, a switch-II pocket (S-IIP) inhibitor, is a conformational specific chemical reporter of KRAS ^G12C nucleotide state in living cells . ARS-1323-alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-103713A

Seclidemstat mesylate 4 Publications Verification SP-2577 mesylate	Histone Demethylase	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 .

HY-124798

Rheb inhibitor NR1 1 Publications Verification	mTOR	Neurological Disease Inflammation/Immunology Cancer
Rheb inhibitor NR1 is a Rheb inhibitor with an IC₅₀ of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven ^T389pS6K1 and increases the phosphorylation of ^S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity . ^{(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)}

HY-134813

MRTX1133 3 Publications Verification	Ras	Cancer
MRTX1133 is a noncovalent, potent, and selective 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 .

Cat. No.	Product Name	Type

HY-U00451

ATP-Red 1 1 Publications Verification	Fluorescent Dyes/Probes
ATP-Red 1 is a multisite-binding switchable fluorescent probe, and can selectively and rapidly responds to intracellular concentrations of ATP in living cells.

Cat. No.	Product Name	Type

HY-148905

p-Aminophenylmercuric acetate	Biochemical Assay Reagents
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 .

p-Aminophenylmercuric acetate

Biochemical Assay Reagents

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 .

Cat. No.	Product Name	Target	Research Area

HY-P3031

Mitogen-activated protein kinase 1 MAPK1	p38 MAPK NF-κB	Inflammation/Immunology
Mitogen-activated protein kinase 1 (MAPK1) can activate the downstream p38/NF-κB pathway. Mitogen-activated protein kinase 1 can regulate cellular processes in various sepsis-associated diseases. MAPK-catalyzed phosphorylation of substrate proteins functions as a switch to turn on or off the activity of the substrate protein .

Cat. No.	Product Name	Target	Research Area

HY-P99313

Quilizumab Anti-Human NGcGM3 Recombinant Antibody	Apoptosis	Inflammation/Immunology
Quilizumab (Anti-Human NGcGM3 Recombinant Antibody) is a humanized IgG1κ monoclonal antibody. Quilizumab targets the M1-prime segment of membrane-expressed IgE, leading to depletion of IgE-switched and memory B cells. Quilizumab has the potantial for the asthma research .

HY-P99236

Bexmarilimab FP-1305	Inhibitory Antibodies	Inflammation/Immunology Cancer
Bexmarilimab (FP-1305) is a potent humanized anti-CLEVER-1 IgG4-antibody with an IC₅₀ value of 4.51 nM. Bexmarilimab is capable of inducing a phenotypic M2 to M1 immune switch of tumor-associated macrophages. Bexmarilimab can be used in research of cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-W010970

5'-Guanylic acid disodium salt 1 Publications Verification 5'-GMP disodium salt; 5'-guanosine monophosphate disodium salt	Classification of Application Fields Ketones, Aldehydes, Acids Source classification Other Diseases Endogenous metabolite Disease Research Fields	Endogenous Metabolite
5'-Guanylic acid disodium salt (5'-GMP disodium salt) is composed of guanine, ribose, and phosphate moieties and it is a nucleotide monomer in messenger RNA. Guanosine derivatives are involved in intracellular signal transduction and have been identified in repetitive genomic sequences in telomeres, in ribosomal DNA, immunoglobulin heavy‐chain switch regions, and in the control regions of proto-oncogenes .

HY-N0284

Esculetin 3 Publications Verification	Structural Classification Classification of Application Fields Oleaceae Source classification Fraxinus rhynchophylla Hance Coumarins Phenols Polyphenols Phenylpropanoids Plants Inflammation/Immunology Disease Research Fields	PI3K Akt
Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities .

Cat. No.	Product Name		Classification

HY-128522

ARS-1323-alkyne		Alkynes
ARS-1323-alkyne, a switch-II pocket (S-IIP) inhibitor, is a conformational specific chemical reporter of KRAS ^G12C nucleotide state in living cells . ARS-1323-alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-134813

MRTX1133 3 Publications Verification		Alkynes
MRTX1133 is a noncovalent, potent, and selective 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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Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Inhibitory Antibodies

Natural
Products

Click Chemistry

switchable

Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Inhibitory Antibodies

NaturalProducts

Click Chemistry

Natural
Products