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Cat. No.: HY-133616

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JH-XIII-05-01

JH-XIII-05-01 is a cereblon-recruiting PROTAC degrader targeting IRAK1 and IRAK4, with DC₅₀ values of 0.065 μM and 3.63 μM, respectively (TMD8 cells). JH-XIII-05-01 reduces cancer cell viability, induces apoptosis in primary MYD88-mutant WM cells and MYD88-mutant/wild-type lymphoma cells, and selectively degrades additional cereblon neosubstrates and kinases IKZF1, IKZF3, CSNK1A1, CSNK1D, CSNK1E, and PAK4. JH-XIII-05-01 can be used for research on Waldenström macroglobulinemia, diffuse large B-cell lymphoma, and B-cell lymphoma.
(Pink: IRAK1 and IRAK4 ligand (HY-133700); Blue: Cereblon ligand (HY-10984); Black: linker (HY-117104)).

For research use only. We do not sell to patients.

CAS No.: 2374699-35-9
Formula: C₄₆H₅₁N₁₁O₁₀
Molecular Weight:917.96

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

JH-XIII-05-01 Chemical Structure

CAS No.: 2374699-35-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

JH-XIII-05-01 is a cereblon-recruiting PROTAC degrader targeting IRAK1 and IRAK4, with DC₅₀ values of 0.065 μM and 3.63 μM, respectively (TMD8 cells). JH-XIII-05-01 reduces cancer cell viability, induces apoptosis in primary MYD88-mutant WM cells and MYD88-mutant/wild-type lymphoma cells, and selectively degrades additional cereblon neosubstrates and kinases IKZF1, IKZF3, CSNK1A1, CSNK1D, CSNK1E, and PAK4. JH-XIII-05-01 can be used for research on Waldenström macroglobulinemia, diffuse large B-cell lymphoma, and B-cell lymphoma^[1]^[2]. (Pink: IRAK1 and IRAK4 ligand (HY-133700); Blue: Cereblon ligand (HY-10984); Black: linker (HY-117104)).

IC₅₀ & Target

^[2]

IRAK1

IRAK4

IKZF1

IKZF3

PAK4

All PROTACs Isoforms :

All IRAK Isoforms :

All IKZF Family Isoforms :

All PAK Isoforms :

All Casein Kinase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
TMD8	EC50	10 nM	Antiproliferative activity against human TMD8 lymphoma cells assessed as reduction in cell viability. Antiproliferative activity against human TMD8 lymphoma cells assessed as reduction in cell viability.	42741641
HBL1	EC50	30 nM	Antiproliferative activity against human HBL-1 lymphoma cells assessed as reduction in cell viability. Antiproliferative activity against human HBL-1 lymphoma cells assessed as reduction in cell viability.	42741641
OCI-Ly7	EC50	23 nM	Antiproliferative activity against human OCI-Ly7 lymphoma cells assessed as reduction in cell viability. Antiproliferative activity against human OCI-Ly7 lymphoma cells assessed as reduction in cell viability.	42741641
OCI-LY19	EC50	3 nM	Antiproliferative activity against human OCI-Ly19 lymphoma cells assessed as reduction in cell viability. Antiproliferative activity against human OCI-Ly19 lymphoma cells assessed as reduction in cell viability.	42741641
Ramos	EC50	92 nM	Antiproliferative activity against human Ramos lymphoma cells assessed as reduction in cell viability. Antiproliferative activity against human Ramos lymphoma cells assessed as reduction in cell viability.	42741641
TMD8	DC₅₀	0.065 μM	Degradation of IRAK1 in human TMD8 MYD88Mut lymphoma cells assessed by Western blot with densitometric quantification. Degradation of IRAK1 in human TMD8 MYD88Mut lymphoma cells assessed by Western blot with densitometric quantification.	42741641
TMD8	DC₅₀	3.63 μM	Degradation of IRAK4 in human TMD8 MYD88Mut lymphoma cells assessed by Western blot with densitometric quantification. Degradation of IRAK4 in human TMD8 MYD88Mut lymphoma cells assessed by Western blot with densitometric quantification.	42741641

In Vitro

Innate ImmunityAnti-cancerApoptosisOthers

Innate Immunity

JH-XIII-05-01 inhibits IRAK1 and IRAK4 with IC₅₀ values of 43 nM and 16 nM, respectively, and maintains 99.1% inhibition of these two kinases while inhibiting only 8 of 468 kinases^[2].
JH-XIII-05-01 (0.4-10 μM) degrades IRAK1 and IRAK4 in TMD8 cells, with DC₅₀ values of 0.065 μM and 3.63 μM, respectively^[2].

Anti-cancer

JH-XIII-05-01 exhibits anti-proliferative EC₅₀ values of 3 nM and 10 nM in OCI-Ly19 and TMD8 lymphoma cells, respectively, and is active in MYD88^Mut and MYD88^WT lymphoma cell lines^[2].

Apoptosis

Anti-cancer

JH-XIII-05-01 (24 h) induces apoptosis in primary MYD88^Mut WM cells and MYD88^Mut/MYD88^WT lymphoma cells, but does not induce apoptosis in CD3⁺ T cells or CD19⁺ B cells from healthy donors^[2].

Others

JH-XIII-05-01 (1 μM; 6 h) selectively degrades IKZF1, IKZF3, CSNK1A1, CSNK1D, CSNK1E, and PAK4 in TMD8 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_last	T_1/2	MRT_{INF_obs}	CL_{_obs}	V_ss
Mice^[2]	10.0 mg/kg	p.o.	0.0830 h	0.0684 μM	2192 min·ng/mL	/	/	/	/
Mice^[2]	30.0 mg/kg	p.o.	0.0830 h	0.387 μM	13601 min·ng/mL	0.473 h	0.710 h	/	/
Mice^[2]	10.0 mg/kg	s.c.	1.00 h	1.82 μM	331424 min·ng/mL	1.97 h	2.93 h	/	/
Mice^[2]	30.0 mg/kg	s.c.	0.500 h	3.22 μM	823883 min·ng/mL	2.71 h	3.77 h	/	/
Mice^[2]	2.00 mg/kg	i.v.	0.0830 h	1.83 μM	30449 min·ng/mL	0.407 h	0.208 h	65.1 mL/min/kg	0.812 L/kg

Chemical Information

CAS No. 2374699-35-9
Molecular Weight 917.96
Formula C₄₆H₅₁N₁₁O₁₀
SMILES

O=C(C1=NC(C2=CC=NN2)=CC=C1)NC3=CC(C4CCN(C(CCOCCOCCOCCOCCNC5=CC=CC(C(N6C7CCC(NC7=O)=O)=O)=C5C6=O)=O)CC4)=NN3C8=CC=CC=N8
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Nathanael S. Gray, et al. Irak degraders and uses thereof. WO2019160915A1. 2020-08-14.

[2]. Hatcher JM, et al. Discovery of JH-XIII-05-01, a First-in-Class Dual IRAK1/IRAK4 Degrader for MYD88 Mutant Lymphomas. ACS medicinal chemistry letters. 2026 Sep 10;17(9):1977-1988.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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JH-XIII-05-01

All PROTACs Isoforms

All IRAK Isoforms

All IKZF Family Isoforms

All PAK Isoforms

All Casein Kinase Isoforms