engagement

By Targets:	Bcl-2 Family (1) CDK (1) Dihydrofolate reductase (DHFR) (2) DNA/RNA Synthesis (11) Epigenetic Reader Domain (1) HIV (1) Oxytocin Receptor (1) P2X Receptor (1) PDI (1) Protein Arginine Deiminase (2) RAR/RXR (1)
By Research Areas:	Cancer (19) Endocrinology (1) Infection (1) Inflammation/Immunology (4) Neurological Disease (1)
Click Chemistry:	Alkynes (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-112088

AZD4573 Maximum Cited Publications 7 Publications Verification	CDK	Cancer
AZD4573 is a potent and highly selective CDK9 inhibitor (IC₅₀ of <4 nM) that enables transient target engagement for the treatment of hematologic malignancies .

HY-148281

TMX-2164	Bcl-2 Family	Cancer
TMX-2164 is a potent, irreversible B-cell lymphoma 6 (BCL6) inhibitor with an IC₅₀ value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells .

HY-157611

DHX9-IN-17

DNA/RNA Synthesis Cancer

DHX9-IN-17 (186) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.161 μM in DHX9 cellular target engagement. Used in cancer research .
HY-157612

DHX9-IN-16

DNA/RNA Synthesis Cancer

DHX9-IN-16 (208) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.125 μM in DHX9 cellular target engagement. Used in cancer research .
HY-157605

DHX9-IN-11

DNA/RNA Synthesis Cancer

DHX9-IN-11 (469) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.0838 μM in DHX9 cellular target engagement. Used in cancer research .
HY-157606

DHX9-IN-13

DNA/RNA Synthesis Cancer

DHX9-IN-13 (389) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 3.4 μM in DHX9 cellular target engagement. Used in cancer research .
HY-157607

DHX9-IN-15

DNA/RNA Synthesis Cancer

DHX9-IN-15 (287) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.232 μM in DHX9 cellular target engagement. Used in cancer research .
HY-157604

DHX9-IN-9

DNA/RNA Synthesis Cancer

DHX9-IN-9 (509) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.0177 μM in DHX9 cellular target engagement. Used in cancer research .
HY-157610

DHX9-IN-14

DNA/RNA Synthesis Cancer

DHX9-IN-14 (161) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 3.4 μM in DHX9 cellular target engagement. Used in cancer research .
HY-157609

DHX9-IN-12

DNA/RNA Synthesis Cancer

DHX9-IN-12 (83) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.917 μM in DHX9 cellular target engagement. Used in cancer research .
HY-157608

DHX9-IN-10

DNA/RNA Synthesis Cancer

DHX9-IN-10 (49) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 9.04 μM in DHX9 cellular target engagement. Used in cancer research .
HY-157603

DHX9-IN-7

DNA/RNA Synthesis Cancer

DHX9-IN-7 (550) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.105 μM in DHX9 cellular target engagement. Used in cancer research .
HY-157602

DHX9-IN-8

DNA/RNA Synthesis Cancer

DHX9-IN-8 (Compound 6) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 3.4 μM in DHX9 cellular target engagement. Used in cancer research .

DHX9-IN-17	DNA/RNA Synthesis	Cancer
DHX9-IN-17 (186) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.161 μM in DHX9 cellular target engagement. Used in cancer research .

DHX9-IN-16	DNA/RNA Synthesis	Cancer
DHX9-IN-16 (208) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.125 μM in DHX9 cellular target engagement. Used in cancer research .

DHX9-IN-11	DNA/RNA Synthesis	Cancer
DHX9-IN-11 (469) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.0838 μM in DHX9 cellular target engagement. Used in cancer research .

DHX9-IN-13	DNA/RNA Synthesis	Cancer
DHX9-IN-13 (389) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 3.4 μM in DHX9 cellular target engagement. Used in cancer research .

DHX9-IN-15	DNA/RNA Synthesis	Cancer
DHX9-IN-15 (287) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.232 μM in DHX9 cellular target engagement. Used in cancer research .

DHX9-IN-9	DNA/RNA Synthesis	Cancer
DHX9-IN-9 (509) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.0177 μM in DHX9 cellular target engagement. Used in cancer research .

DHX9-IN-14	DNA/RNA Synthesis	Cancer
DHX9-IN-14 (161) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 3.4 μM in DHX9 cellular target engagement. Used in cancer research .

DHX9-IN-12	DNA/RNA Synthesis	Cancer
DHX9-IN-12 (83) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.917 μM in DHX9 cellular target engagement. Used in cancer research .

DHX9-IN-10	DNA/RNA Synthesis	Cancer
DHX9-IN-10 (49) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 9.04 μM in DHX9 cellular target engagement. Used in cancer research .

DHX9-IN-7	DNA/RNA Synthesis	Cancer
DHX9-IN-7 (550) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 0.105 μM in DHX9 cellular target engagement. Used in cancer research .

DHX9-IN-8	DNA/RNA Synthesis	Cancer
DHX9-IN-8 (Compound 6) is a RNA helicase DHX9 inhibitor, with an EC₅₀ of 3.4 μM in DHX9 cellular target engagement. Used in cancer research .

HY-141550

BPK-25	Others	Inflammation/Immunology
BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP .

HY-P5017

(Val3,Pro8)-Oxytocin	Oxytocin Receptor	Endocrinology
(Val3,Pro8)-Oxytocin is the Gq-dependent pathway agonist. (Val3,Pro8)-Oxytocin is also a weaker agonist for the β-arrestin engagement and endocytosis toward the oxytocin receptor (OXTR) .

HY-136521

AZ13824374	Epigenetic Reader Domain	Cancer
AZ13824374 is a highly potent and selective ATAD2 bromodomain inhibitor which shows cellular target engagement and antiproliferative activity in a range of breast cancer models. AZ13824374 inhibits ATAD2 with pIC₅₀s of 8.2 and 6.2 in ATAD2 FRET assay and ATAD2 NanoBRET assay, respectively .

HY-136557

AFM32a PAD2-IN-1	Protein Arginine Deiminase	Inflammation/Immunology Cancer
AFM32a (PAD2-IN-1), a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. AFM32a shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold) .

HY-136557A

AFM32a hydrochloride 1 Publications Verification PAD2-IN-1 hydrochloride	Protein Arginine Deiminase	Inflammation/Immunology Cancer
AFM32a (PAD2-IN-1) hydrochloride, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. AFM32a hydrochloride shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold) .

HY-111573

KCL-286

RAR/RXR Others

Anticancer agent 168 is an orally active retinoic acid receptor (RAR/RXR) beta2 agonist with ameliorating effects on spinal cord injury (SCI) .

KCL-286	RAR/RXR	Others
Anticancer agent 168 is an orally active retinoic acid receptor (RAR/RXR) beta2 agonist with ameliorating effects on spinal cord injury (SCI) .

HY-D0976

NF279	P2X Receptor HIV	Infection
NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC₅₀ of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC₅₀=1.62 μM), P2X4 (IC₅₀>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env .

HY-117570

KSC-34	PDI	Neurological Disease
KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC₅₀ of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family . KSC-34 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-161063

DHFR-IN-14	Dihydrofolate reductase (DHFR)	Cancer
DHFR-IN-14 (compound 32) is a pyrimethamine (Pyr)-type, dihydrofolate reductase (DHFR) inhibitor with potential anticancer activity .

HY-161064

DHFR-IN-15	Dihydrofolate reductase (DHFR)	Cancer
DHFR-IN-15 (compound 34) is a dihydrofolate reductase (DHFR) inhibitor with potential anticancer activity. DHFR-IN-15 effectively binds to DHFR in cells, reducing DHFR levels to 10 nM .

Cat. No.	Product Name	Target	Research Area

HY-P5017

(Val3,Pro8)-Oxytocin	Oxytocin Receptor	Endocrinology
(Val3,Pro8)-Oxytocin is the Gq-dependent pathway agonist. (Val3,Pro8)-Oxytocin is also a weaker agonist for the β-arrestin engagement and endocytosis toward the oxytocin receptor (OXTR) .

Cat. No.	Product Name	Target	Research Area

HY-P99431

KY-1044 Alomfilimab; SAR 445256	Inhibitory Antibodies	Inflammation/Immunology Cancer
KY-1044 (Alomfilimab; SAR 445256) is a fully human IgG1 antibody targeting inducible costimulatory receptor (ICOS). KY-1044 depletes ICOS ^high cells via antibody-dependent cellular cytotoxicity (ADCC) through the engagement of FcgRIIIa. KY-1044 act as a costimulatory molecule on cells expressing lower ICOS levels, such as CD8 ⁺ T_Eff cells (through FcgR-dependent clustering). KY-1044 exploit the differential expression of ICOS on T-cell subtypes to improve the intratumoral immune contexture and restore an antitumor immune response .

Cat. No.	Product Name		Classification

HY-117570

KSC-34		Alkynes
KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC₅₀ of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family . KSC-34 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Click Chemistry

Name
Email *

	Sorry, but the email address you supplied was invalid.